PROTAC degraders as chemical probes for studying target biology and target validation

Selective inhibition of BET bromodomains

Filippakopoulos, P., Qi, J., Picaud, S., Shen, Y., Smith, W. B., Fedorov, O., Morse, E. M., Keates, T., Hickman, T. T., Felletar, I., et al. (2010) · Nature · doi:10.1038/nature09504 · Cited by 4,262 · see citing works

Protacs: Chimeric molecules that target proteins to the Skp1–Cullin–F box complex for ubiquitination and degradation

Sakamoto, K. M., Kim, K. B., Kumagai, A., Mercurio, F., Crews, C. M., & Deshaies, R. J. (2001) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.141230798 · Cited by 2,609 · see citing works

Targeting bromodomains: epigenetic readers of lysine acetylation

Filippakopoulos, P., & Knapp, S. (2014) · Nature Reviews Drug Discovery · doi:10.1038/nrd4286 · Cited by 1,274 · see citing works

Structural basis of PROTAC cooperative recognition for selective protein degradation

Gadd, M. S., Testa, A., Lucas, X., Chan, K.-H., Chen, W., Lamont, D. J., Zengerle, M., & Ciulli, A. (2017) · Nature Chemical Biology · doi:10.1038/nchembio.2329 · Cited by 1,242 · see citing works

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4

Zengerle, M., Chan, K.-H., & Ciulli, A. (2015) · ACS Chemical Biology · doi:10.1021/acschembio.5b00216 · Cited by 1,056 · see citing works

Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

Bondeson, D. P., Smith, B. E., Burslem, G. M., Buhimschi, A. D., Hines, J., Jaime-Figueroa, S., Wang, J., Hamman, B. D., Ishchenko, A., & Crews, C. M. (2018) · Cell Chemical Biology · doi:10.1016/j.chembiol.2017.09.010 · Cited by 923 · see citing works

The promise and peril of chemical probes

Arrowsmith, C. H., Audia, J. E., Austin, C., Baell, J., Bennett, J., Blagg, J., Bountra, C., Brennan, P. E., Brown, P. J., Bunnage, M. E., et al. (2015) · Nature Chemical Biology · doi:10.1038/nchembio.1867 · Cited by 839 · see citing works

PROteolysis TArgeting Chimeras (PROTACs) — Past, present and future

Pettersson, M., & Crews, C. M. (2019) · Drug Discovery Today Technologies · doi:10.1016/j.ddtec.2019.01.002 · Cited by 818 · see citing works

Trends in kinase drug discovery: targets, indications and inhibitor design

Attwood, M. M., Fabbro, D., Sokolov, A. V., Knapp, S., & Schiöth, H. B. (2021) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00252-y · Cited by 807 · see citing works

A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity

Khan, S., Zhang, X., Lv, D., Zhang, Q., He, Y., Zhang, P., Liu, X., Thummuri, D., Yuan, Y., Wiegand, J. S., et al. (2019) · Nature Medicine · doi:10.1038/s41591-019-0668-z · Cited by 688 · see citing works

Small‐Molecule PROTACS: New Approaches to Protein Degradation

Toure, M., & Crews, C. M. (2016) · Angewandte Chemie International Edition · doi:10.1002/anie.201507978 · Cited by 674 · see citing works

Plasticity in binding confers selectivity in ligand-induced protein degradation

Nowak, R. P., DeAngelo, S. L., Buckley, D., He, Z., Donovan, K. A., An, J., Safaee, N., Jedrychowski, M. P., Ponthier, C. M., Ishoey, M., et al. (2018) · Nature Chemical Biology · doi:10.1038/s41589-018-0055-y · Cited by 615 · see citing works

RING-type E3 ligases: Master manipulators of E2 ubiquitin-conjugating enzymes and ubiquitination

Metzger, M. B., Pruneda, J. N., Klevit, R. E., & Weissman, A. M. (2013) · Biochimica et Biophysica Acta (BBA) - Molecular Cell Research · doi:10.1016/j.bbamcr.2013.05.026 · Cited by 608 · see citing works

Caco-2 cell permeability assays to measure drug absorption

van Breemen, R. B., & Li, Y. (2005) · Expert Opinion on Drug Metabolism & Toxicology · doi:10.1517/17425255.1.2.175 · Cited by 602 · see citing works

BAF complex vulnerabilities in cancer demonstrated via structure-based PROTAC design

Farnaby, W., Koegl, M., Roy, M. J., Whitworth, C., Diers, E., Trainor, N., Zollman, D., Steurer, S., Karolyi-Oezguer, J., Riedmueller, C., et al. (2019) · Nature Chemical Biology · doi:10.1038/s41589-019-0294-6 · Cited by 562 · see citing works

UBCH7 reactivity profile reveals parkin and HHARI to be RING/HECT hybrids

Wenzel, D. M., Lissounov, A., Brzović, P. S., & Klevit, R. E. (2011) · Nature · doi:10.1038/nature09966 · Cited by 560 · see citing works

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation

Olson, C. M., Jiang, B., Erb, M. A., Liang, Y., Doctor, Z. M., Zhang, Z., Zhang, T., Kwiatkowski, N., Boukhali, M., Green, J. L., et al. (2018) · Nature Chemical Biology · doi:10.1038/nchembio.2538 · Cited by 552 · see citing works

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

Smith, B. E., Wang, S. L., Jaime-Figueroa, S., Harbin, A., Wang, J., Hamman, B. D., & Crews, C. M. (2019) · Nature Communications · doi:10.1038/s41467-018-08027-7 · Cited by 517 · see citing works

Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

Zhang, X., Crowley, V. M., Wucherpfennig, T. G., Dix, M. M., & Cravatt, B. F. (2019) · Nature Chemical Biology · doi:10.1038/s41589-019-0279-5 · Cited by 487 · see citing works

BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment

Winter, G. E., Mayer, A., Buckley, D. L., Erb, M. A., Roderick, J. E., Vittori, S., Reyes, J. M., di Iulio, J., Souza, A., Ott, C. J., et al. (2017) · Molecular Cell · doi:10.1016/j.molcel.2017.06.004 · Cited by 465 · see citing works

Targeted Degradation of Oncogenic KRAS ^G12C by VHL-Recruiting PROTACs

Bond, M. J., Chu, L., Nalawansha, D. A., Li, K., & Crews, C. M. (2020) · ACS Central Science · doi:10.1021/acscentsci.0c00411 · Cited by 450 · see citing works

A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader

Huang, H.-T., Dobrovolsky, D., Paulk, J., Yang, G., Weisberg, E. L., Doctor, Z. M., Buckley, D. L., Cho, J.-H., Ko, E., Jang, J., et al. (2018) · Cell Chemical Biology · doi:10.1016/j.chembiol.2017.10.005 · Cited by 437 · see citing works

CRISPR-Mediated Tagging of Endogenous Proteins with a Luminescent Peptide

Schwinn, M. K., Machleidt, T., Zimmerman, K., Eggers, C. T., Dixon, A. S., Hurst, R., Hall, M. P., Encell, L. P., Binkowski, B. F., & Wood, K. V. (2018) · ACS Chemical Biology · doi:10.1021/acschembio.7b00549 · Cited by 434 · see citing works

Proteolysis targeting chimeras (PROTACs) in ‘beyond rule-of-five’ chemical space: Recent progress and future challenges

Edmondson, S. D., Yang, B., & Fallan, C. (2019) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2019.04.030 · Cited by 422 · see citing works

SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate

Roy, M. J., Winkler, S., Hughes, S. J., Whitworth, C., Galant, M., Farnaby, W., Rumpel, K., & Ciulli, A. (2019) · ACS Chemical Biology · doi:10.1021/acschembio.9b00092 · Cited by 386 · see citing works

Dual kinase-bromodomain inhibitors for rationally designed polypharmacology

Ciceri, P., Müller, S., O’Mahony, A., Fedorov, O., Filippakopoulos, P., Hunt, J. P., Lasater, E. A., Pallares, G., Picaud, S., Wells, C. D., et al. (2014) · Nature Chemical Biology · doi:10.1038/nchembio.1471 · Cited by 345 · see citing works

Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel–Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7

Zoppi, V., Hughes, S. J., Maniaci, C., Testa, A., Gmaschitz, T., Wieshofer, C., Koegl, M., Riching, K. M., Daniels, D. L., Spallarossa, A., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01413 · Cited by 336 · see citing works

Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications

Ward, C. C., Kleinman, J. I., Brittain, S. M., Lee, P. S., Chung, C. Y. S., Kim, K., Petri, Y., Thomas, J. R., Tallarico, J. A., McKenna, J. M., et al. (2019) · ACS Chemical Biology · doi:10.1021/acschembio.8b01083 · Cited by 336 · see citing works

WD40 repeat domain proteins: a novel target class?

Schapira, M., Tyers, M., Torrent, M., & Arrowsmith, C. H. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2017.179 · Cited by 335 · see citing works

Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action

Riching, K. M., Mahan, S. D., Corona, C. R., McDougall, M. G., Vasta, J. D., Robers, M. B., Urh, M., & Daniels, D. L. (2018) · ACS Chemical Biology · doi:10.1021/acschembio.8b00692 · Cited by 307 · see citing works

Probing the Probes: Fitness Factors For Small Molecule Tools

Workman, P., & Collins, I. (2010) · Chemistry & Biology · doi:10.1016/j.chembiol.2010.05.013 · Cited by 300 · see citing works

Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands

Remillard, D., Buckley, D. L., Paulk, J., Brien, G. L., Sonnett, M., Seo, H., Dastjerdi, S., Wühr, M., Dhe‐Paganon, S., Armstrong, S. A., et al. (2017) · Angewandte Chemie International Edition · doi:10.1002/anie.201611281 · Cited by 294 · see citing works

Targeted protein degradation: A promise for undruggable proteins

Samarasinghe, K. T. G., & Crews, C. M. (2021) · Cell chemical biology · doi:10.1016/j.chembiol.2021.04.011 · Cited by 291 · see citing works

The SMARCA2/4 ATPase Domain Surpasses the Bromodomain as a Drug Target in SWI/SNF-Mutant Cancers: Insights from cDNA Rescue and PFI-3 Inhibitor Studies

Vangamudi, B., Paul, T. A., Shah, P. K., Kost-Alimova, M., Nottebaum, L., Shi, X., Zhan, Y., Leo, E., Mahadeshwar, H. S., Protopopov, A., et al. (2015) · Cancer Research · doi:10.1158/0008-5472.can-14-3798 · Cited by 281 · see citing works

The ins and outs of selective kinase inhibitor development

Müller, S., Chaikuad, A., Gray, N. S., & Knapp, S. (2015) · Nature Chemical Biology · doi:10.1038/nchembio.1938 · Cited by 276 · see citing works

The PROTACtable genome

Schneider, M., Radoux, C. J., Hercules, A., Ochoa, D., Dunham, I., Zalmas, L.-P., Hessler, G., Ruf, S., Shanmugasundaram, V., Hann, M. M., et al. (2021) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00245-x · Cited by 273 · see citing works

Homolog-Selective Degradation as a Strategy to Probe the Function of CDK6 in AML

Brand, M., Jiang, B., Bauer, S., Donovan, K. A., Liang, Y., Wang, E. S., Nowak, R. P., Yuan, J. C., Zhang, T., Kwiatkowski, N., et al. (2019) · Cell Chemical Biology · doi:10.1016/j.chembiol.2018.11.006 · Cited by 258 · see citing works

Structure‐Based Design of a Macrocyclic PROTAC

Testa, A., Hughes, S. J., Lucas, X., Wright, J. E., & Ciulli, A. (2019) · Angewandte Chemie International Edition · doi:10.1002/anie.201914396 · Cited by 251 · see citing works

Triterpenoid CDDO-Me Blocks the NF-κB Pathway by Direct Inhibition of IKKβ on Cys-179

Ahmad, R., Raina, D. B., Meyer, C. J., Kharbanda, S. M., & Kufe, D. W. (2006) · Journal of Biological Chemistry · doi:10.1074/jbc.m607160200 · Cited by 238 · see citing works

Multiubiquitylation by E4 enzymes: ‘one size’ doesn't fit all

Hoppe, T. (2005) · Trends in Biochemical Sciences · doi:10.1016/j.tibs.2005.02.004 · Cited by 237 · see citing works

The Cysteinome of Protein Kinases as a Target in Drug Development

Chaikuad, A., Koch, P., Laufer, S., & Knapp, S. (2017) · Angewandte Chemie International Edition · doi:10.1002/anie.201707875 · Cited by 237 · see citing works

Extended pharmacodynamic responses observed upon PROTAC-mediated degradation of RIPK2

Mares, A., Miah, A. H., Smith, I. E. D., Rackham, M., Thawani, A. R., Cryan, J., Haile, P. A., Votta, B. J., Beal, A. M., Capriotti, C., et al. (2020) · Communications Biology · doi:10.1038/s42003-020-0868-6 · Cited by 232 · see citing works

Recent Developments in PROTAC‐Mediated Protein Degradation: From Bench to Clinic

Hu, Z., & Crews, C. M. (2022) · ChemBioChem · doi:10.1002/cbic.202100270 · Cited by 231 · see citing works

A ubiquitin ligase transfers preformed polyubiquitin chains from a conjugating enzyme to a substrate

Li, W., Tu, D., Brünger, A. T., & Ye, Y. (2007) · Nature · doi:10.1038/nature05542 · Cited by 227 · see citing works

Detection of sequential polyubiquitylation on a millisecond timescale

Pierce, N. W., Kleiger, G., Shan, S., & Deshaies, R. J. (2009) · Nature · doi:10.1038/nature08595 · Cited by 225 · see citing works

PRosettaC: Rosetta Based Modeling of PROTAC Mediated Ternary Complexes

Zaidman, D., Prilusky, J., & London, N. (2020) · Journal of Chemical Information and Modeling · doi:10.1021/acs.jcim.0c00589 · Cited by 224 · see citing works

Functional TRIM24 degrader via conjugation of ineffectual bromodomain and VHL ligands

Gechijian, L. N., Buckley, D. L., Lawlor, M. A., Reyes, J. M., Paulk, J., Ott, C. J., Winter, G. E., Erb, M. A., Scott, T. G., Xu, M., et al. (2018) · Nature Chemical Biology · doi:10.1038/s41589-018-0010-y · Cited by 222 · see citing works

Discovery of a Covalent FEM1B Recruiter for Targeted Protein Degradation Applications

Henning, N. J., Manford, A. G., Spradlin, J. N., Brittain, S. M., Zhang, E., McKenna, J. M., Tallarico, J. A., Schirle, M., Rape, M., & Nomura, D. K. (2022) · Journal of the American Chemical Society · doi:10.1021/jacs.1c03980 · Cited by 221 · see citing works

Enhancing intracellular accumulation and target engagement of PROTACs with reversible covalent chemistry

Guo, W., Qi, X., Yu, X., Liu, Y., Chung, C.-I., Bai, F., Lin, X., Lu, D., Wang, L., Chen, J., et al. (2020) · Nature Communications · doi:10.1038/s41467-020-17997-6 · Cited by 220 · see citing works

PROTAC-DB: an online database of PROTACs

Weng, G., Shen, C., Cao, D., Gao, J., Dong, X., He, Q., Yang, B., Li, D., Wu, J., & Hou, T. (2021) · Nucleic Acids Research · doi:10.1093/nar/gkaa807 · Cited by 219 · see citing works

Efficient targeted degradation via reversible and irreversible covalent PROTACs

Gabizon, R., Shraga, A., Gehrtz, P., Livnah, E., Gurwicz, N., Avram, L., Unger, T., Albeck, S., Shulman, Z., & London, N. (2020) · doi:10.26434/chemrxiv.11494398.v1 · Cited by 213 · see citing works

Targeting BCR-ABL1 in Chronic Myeloid Leukemia by PROTAC-Mediated Targeted Protein Degradation

Burslem, G. M., Schultz, A. R., Bondeson, D. P., Eide, C. A., Savage Stevens, S. L., Druker, B. J., & Crews, C. M. (2019) · Cancer Research · doi:10.1158/0008-5472.can-19-1236 · Cited by 212 · see citing works

The Ascension of Targeted Covalent Inhibitors

Singh, J. (2022) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c02134 · Cited by 210 · see citing works

Solution Conformations Shed Light on PROTAC Cell Permeability

Atilaw, Y., Poongavanam, V., Svensson Nilsson, C., Nguyen, D., Giese, A., Meibom, D., Erdelyi, M., & Kihlberg, J. (2021) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.0c00556 · Cited by 208 · see citing works

Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders

Su, S., Yang, Z., Gao, H., Yang, H., Zhu, S., An, Z., Wang, J., Li, Q., Chandarlapaty, S., Deng, H., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00871 · Cited by 208 · see citing works

Rational Design and Synthesis of Novel Dual PROTACs for Simultaneous Degradation of EGFR and PARP

Zheng, M., Huo, J., Gu, X., Wang, Y., Wu, C., Zhang, Q., Wang, W., Liu, Y., Liu, Y., Zhou, X., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c00649 · Cited by 206 · see citing works

Choose and Use Your Chemical Probe Wisely to Explore Cancer Biology

Blagg, J., & Workman, P. (2017) · Cancer Cell · doi:10.1016/j.ccell.2017.06.005 · Cited by 203 · see citing works

DCAF11 Supports Targeted Protein Degradation by Electrophilic Proteolysis-Targeting Chimeras

Zhang, X., Luukkonen, L. M., Eissler, C. L., Crowley, V. M., Yamashita, Y., Schafroth, M. A., Kikuchi, S., Weinstein, D. S., Symons, K. T., Nordin, B. E., et al. (2021) · Journal of the American Chemical Society · doi:10.1021/jacs.1c00990 · Cited by 199 · see citing works

From Conception to Development: Investigating PROTACs Features for Improved Cell Permeability and Successful Protein Degradation

Cecchini, C., Pannilunghi, S., Tardy, S., & Scapozza, L. (2021) · Frontiers in Chemistry · doi:10.3389/fchem.2021.672267 · Cited by 198 · see citing works

PROTAC-Mediated Degradation of Bruton’s Tyrosine Kinase Is Inhibited by Covalent Binding

Tinworth, C. P., Lithgow, H., Dittus, L., Bassi, Z. I., Hughes, S. E., Muelbaier, M., Dai, H., Smith, I. E. D., Kerr, W. J., Burley, G. A., et al. (2019) · ACS Chemical Biology · doi:10.1021/acschembio.8b01094 · Cited by 195 · see citing works

Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach

Bassi, Z. I., Fillmore, M. C., Miah, A. H., Chapman, T. D., Maller, C., Roberts, E. J., Davis, L. C., Lewis, D. E., Galwey, N. W., Waddington, K. E., et al. (2018) · ACS Chemical Biology · doi:10.1021/acschembio.8b00705 · Cited by 186 · see citing works

Chemoproteomics-enabled discovery of covalent RNF114-based degraders that mimic natural product function

Luo, M., Spradlin, J. N., Boike, L., Tong, B., Brittain, S. M., McKenna, J. M., Tallarico, J. A., Schirle, M., Maimone, T. J., & Nomura, D. K. (2021) · Cell Chemical Biology · doi:10.1016/j.chembiol.2021.01.005 · Cited by 186 · see citing works

Kinase Inhibitor Selectivity Profiling Using Differential Scanning Fluorimetry

Fedorov, O., Niesen, F., & Knapp, S. (2011) · Methods in molecular biology · doi:10.1007/978-1-61779-337-0_7 · Cited by 183 · see citing works

PROTAC-mediated degradation reveals a non-catalytic function of AURORA-A kinase

Adhikari, B., Božilović, J., Diebold, M., Schwarz, J. D., Hofstetter, J., Schröder, M., Wanior, M., Narain, A., Vogt, M., Stanković, N. D., et al. (2020) · Nature Chemical Biology · doi:10.1038/s41589-020-00652-y · Cited by 175 · see citing works

PROTACs– a game-changing technology

Konstantinidou, M., Li, J., Zhang, B., Wang, Z., Shaabani, S., ter Brake, F., Essa, K., & Dömling, A. S. S. (2019) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2019.1659242 · Cited by 167 · see citing works

A selective WDR5 degrader inhibits acute myeloid leukemia in patient-derived mouse models

Yu, X., Li, D., Kottur, J., Shen, Y., Kim, H. S., Park, K., Tsai, Y., Gong, W., Wang, J., Suzuki, K., et al. (2021) · Science Translational Medicine · doi:10.1126/scitranslmed.abj1578 · Cited by 154 · see citing works

Understanding and Improving the Membrane Permeability of VH032-Based PROTACs

Klein, V. G., Townsend, C. E., Testa, A., Zengerle, M., Maniaci, C., Hughes, S. J., Chan, K.-H., Ciulli, A., & Lokey, R. S. (2020) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.0c00265 · Cited by 153 · see citing works

Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity

Klein, V. G., Bond, A. G., Craigon, C., Lokey, R. S., & Ciulli, A. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01496 · Cited by 152 · see citing works

Bardoxolone conjugation enables targeted protein degradation of BRD4

Tong, B., Luo, M., Xie, Y., Spradlin, J. N., Tallarico, J. A., McKenna, J. M., Schirle, M., Maimone, T. J., & Nomura, D. K. (2020) · Scientific Reports · doi:10.1038/s41598-020-72491-9 · Cited by 149 · see citing works

Improving on Nature: Making a Cyclic Heptapeptide Orally Bioavailable

Nielsen, D. S., Hoang, H. N., Lohman, R., Hill, T. A., Lucke, A. J., Craik, D. J., Edmonds, D. J., Griffith, D. A., Rotter, C. J., Ruggeri, R. B., et al. (2014) · Angewandte Chemie International Edition · doi:10.1002/anie.201405364 · Cited by 144 · see citing works

Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance

Fedorov, O., Castex, J., Tallant, C., Owen, D. R., Martin, S., Aldeghi, M., Monteiro, O., Filippakopoulos, P., Picaud, S., Trzupek, J. D., et al. (2015) · Science Advances · doi:10.1126/sciadv.1500723 · Cited by 144 · see citing works

Genomic insights into the causes of type 2 diabetes

Langenberg, C., & Lotta, L. A. (2018) · The Lancet · doi:10.1016/s0140-6736(18)31132-2 · Cited by 142 · see citing works

Chemical approaches to targeted protein degradation through modulation of the ubiquitin–proteasome pathway

Collins, I., Wang, H., Caldwell, J., & Chopra, R. (2017) · Biochemical Journal · doi:10.1042/bcj20160762 · Cited by 135 · see citing works

Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket

Förster, M., Chaikuad, A., Bauer, S. M., Holstein, J., Robers, M. B., Corona, C. R., Gehringer, M., Pfaffenrot, E., Ghoreschi, K., Knapp, S., et al. (2016) · Cell chemical biology · doi:10.1016/j.chembiol.2016.10.008 · Cited by 132 · see citing works

Targetable BET proteins- and E2F1-dependent transcriptional program maintains the malignancy of glioblastoma

Xu, L., Chen, Y., Mayakonda, A., Koh, L., Chong, Y. K., Buckley, D. L., Sandanaraj, E., Lim, S. W., Lin, R. Y., Ke, X., et al. (2018) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1712363115 · Cited by 112 · see citing works

Development of BromoTag: A “Bump-and-Hole”–PROTAC System to Induce Potent, Rapid, and Selective Degradation of Tagged Target Proteins

Bond, A. G., Craigon, C., Chan, K.-H., Testa, A., Karapetsas, A., Fasimoye, R. Y., Macartney, T., Blow, J. J., Alessi, D. R., & Ciulli, A. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01532 · Cited by 111 · see citing works

Protein degradation through covalent inhibitor-based PROTACs

Xue, G., Chen, J., Liu, L., Zhou, D., Zuo, Y., Fu, T., & Pan, Z. (2020) · Chemical Communications · doi:10.1039/c9cc08238g · Cited by 109 · see citing works

Donated chemical probes for open science

Müller, S., Ackloo, S. Z., Arrowsmith, C. H., Bauser, M., Baryza, J. L., Blagg, J., Böttcher, J., Bountra, C., Brown, P. J., Bunnage, M. E., et al. (2018) · eLife · doi:10.7554/elife.34311 · Cited by 107 · see citing works

Enzymatic Logic of Ubiquitin Chain Assembly

Deol, K. K., Lorenz, S., & Strieter, E. R. (2019) · Frontiers in Physiology · doi:10.3389/fphys.2019.00835 · Cited by 107 · see citing works

Mechanistic and Structural Features of PROTAC Ternary Complexes

Casement, R., Bond, A. G., Craigon, C., & Ciulli, A. (2021) · Methods in molecular biology · doi:10.1007/978-1-0716-1665-9_5 · Cited by 105 · see citing works

Critical Assessment of Targeted Protein Degradation as a Research Tool and Pharmacological Modality

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Structure-Based Optimization of a Small Molecule Antagonist of the Interaction Between WD Repeat-Containing Protein 5 (WDR5) and Mixed-Lineage Leukemia 1 (MLL1)

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Protein targeting chimeric molecules specific for bromodomain and extra-terminal motif family proteins are active against pre-clinical models of multiple myeloma

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Fluorescent and Bioluminescent Calcium Indicators with Tuneable Colors and Affinities

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Selective targeting of non-centrosomal AURKA functions through use of a targeted protein degradation tool

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Discovery of a dual WDR5 and Ikaros PROTAC degrader as an anti-cancer therapeutic

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Targeting epigenetic modulators using PROTAC degraders: Current status and future perspective

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Assessing histone demethylase inhibitors in cells: lessons learned

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Advances in Genomics for Drug Development

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Covalent PROTACs: the best of both worlds?

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Mapping Proteome-Wide Targets of Environmental Chemicals Using Reactivity-Based Chemoproteomic Platforms

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Open Access Chemical Probes for Epigenetic Targets

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The Promise and Peril of Chemical Probe Negative Controls

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Pan-SMARCA/PB1 Bromodomain Inhibitors and Their Role in Regulating Adipogenesis

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Public Resources for Chemical Probes: The Journey so Far and the Road Ahead

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Small molecule targeting of chromatin writers in cancer

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Prediction of Chameleonic Efficiency

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Discovery of a Highly Potent and Selective Degrader Targeting Hematopoietic Prostaglandin D Synthase via In Silico Design

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Image-Based Annotation of Chemogenomic Libraries for Phenotypic Screening

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Aurora-A: a potential DNA repair modulator

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A High-Throughput Method to Prioritize PROTAC Intracellular Target Engagement and Cell Permeability Using NanoBRET

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Engineering Single Pan-Specific Ubiquibodies for Targeted Degradation of All Forms of Endogenous ERK Protein Kinase

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Novel, highly potent PROTACs targeting AURORA-A kinase

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Chemical probes targeting epigenetic proteins: Applications beyond oncology

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A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing Proteins

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Genomics-driven drug discovery based on disease-susceptibility genes

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A Method for Determining the Kinetics of Small-Molecule-Induced Ubiquitination

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Chemical Inactivation of the E3 Ubiquitin Ligase Cereblon by Pomalidomide-based Homo-PROTACs

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Expanding the Degradable Proteome: Designing PROTACs by the Book

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Methods for Quantitative Assessment of Protein Degradation

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Linker length affects photostability of protein-targeted sensor of cellular microviscosity

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Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes

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Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization

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Overview of epigenetic degraders based on PROTAC, molecular glue, and hydrophobic tagging technologies

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Small-molecule probes from bench to bedside: advancing molecular analysis of drug–target interactions toward precision medicine

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Small-molecule PROTAC mediates targeted protein degradation to treat STAT3-dependent epithelial cancer

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Targeted Protein Degradation for Infectious Diseases: from Basic Biology to Drug Discovery

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Leveraging aptamers for targeted protein degradation

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Revolutionizing Drug Targeting Strategies: Integrating Artificial Intelligence and Structure-Based Methods in PROTAC Development

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How many kinases are druggable? A review of our current understanding

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The impact of E3 ligase choice on PROTAC effectiveness in protein kinase degradation

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Application of Novel Degraders Employing Autophagy for Expediting Medicinal Research

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Antibody-Proteolysis Targeting Chimera Conjugate Enables Selective Degradation of Receptor-Interacting Serine/Threonine-Protein Kinase 2 in HER2+ Cell Lines

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Tumor microenvironment responsive nano-PROTAC for BRD4 degradation enhanced cancer photo-immunotherapy

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Pharmacological inhibition of HDAC6 suppresses NLRP3 inflammasome-mediated IL-1β release

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Single amino acid–based PROTACs trigger degradation of the oncogenic kinase BCR–ABL in chronic myeloid leukemia (CML)

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The most common linkers in bioactive molecules and their bioisosteric replacement network

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Discovery of a Potent Proteolysis Targeting Chimera Enables Targeting the Scaffolding Functions of FK506‐Binding Protein 51 (FKBP51)

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Luciferase- and HaloTag-based reporter assays to measure small-molecule-induced degradation pathway in living cells

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Expanding the ligand spaces for E3 ligases for the design of protein degraders

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Which Small Molecule? Selecting Chemical Probes for Use in Cancer Research and Target Validation

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Characterizing the Cooperative Effect of PROTAC Systems with End-Point Binding Free Energy Calculation

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Critical assessment of LC3/GABARAP ligands used for degrader development and ligandability of LC3/GABARAP binding pockets

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Workflow for E3 Ligase Ligand Validation for PROTAC Development

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PROTAC chemical probes for histone deacetylase enzymes

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Interplay of PROTAC Complex Dynamics for Undruggable Targets: Insights into Ternary Complex Behavior and Linker Design

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Rational Proteolysis Targeting Chimera Design Driven by Molecular Modeling and Machine Learning

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Application of PROTACs in target identification and validation

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Auto-RapTAC: A Versatile and Sustainable Platform for the Automated Rapid Synthesis and Evaluation of PROTAC

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Discovery and Functional Characterization of a Potent, Selective, and Metabolically Stable PROTAC of the Protein Kinases DYRK1A and DYRK1B

Wilms, G., Schofield, K., Maddern, S., Foley, C., Shaw, Y., Smith, B. E., Basantes, L. E., Schwandt, K., Babendreyer, A., Chavez, T., et al. (2024) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.4c01130 · Cited by 17 · see citing works

Identification of a Highly Cooperative PROTAC Degrader Targeting GTP-Loaded KRAS(On) Alleles

Vetma, V., Puoti, I., Karolak, N. K., Chakraborti, S., Diers, E., Girardi, E., Khan, S., Kidd, G., Kropatsch, K., McLennan, R., et al. (2025) · Journal of the American Chemical Society · doi:10.1021/jacs.5c10354 · Cited by 16 · see citing works

Functional Characterization of Pathway Inhibitors for the Ubiquitin-Proteasome System (UPS) as Tool Compounds for CRBN and VHL-Mediated Targeted Protein Degradation

Schwalm, M. P., Menge, A., Elson, L., Greco, F., Robers, M. B., Müller, S., & Knapp, S. (2025) · ACS Chemical Biology · doi:10.1021/acschembio.4c00450 · Cited by 15 · see citing works

Potential of the nanoplatform and PROTAC interface to achieve targeted protein degradation through the Ubiquitin–Proteasome system

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Stereochemical inversion at a 1,4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity

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Extrapolating Lessons from Targeted Protein Degradation to Other Proximity-Inducing Drugs

Winter, G. E. (2024) · ACS Chemical Biology · doi:10.1021/acschembio.4c00191 · Cited by 12 · see citing works

Bifunctional robots inducing targeted protein degradation

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From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors

Koravović, M., Mayasundari, A., Tasić, G., Keramatnia, F., Stachowski, T. R., Cui, H., Chai, S. C., Jonchère, B., Yang, L., Li, Y., et al. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115246 · Cited by 10 · see citing works

Epigenetic therapy meets targeted protein degradation: HDAC-PROTACs in cancer treatment

Hussain, M. S., Zhang, L., Rana, A. J., Maqbool, M., Ashique, S., Khan, Y., Jakhmola, V., Hanbashi, A., Mawkili, W., & Khan, G. (2025) · Future Medicinal Chemistry · doi:10.1080/17568919.2025.2533113 · Cited by 9 · see citing works

Click. Screen. Degrade. A Miniaturized D2B Workflow for Rapid PROTAC Discovery

Mitrovic, M., Greco, F., Cruz-Garcia, Y., Lučić, A., Hoffmann, L., Chander, R., Schönfeld, J., Liebisch, N., Sivashanmugam, S. A., Schwalm, M. P., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5c02543 · Cited by 8 · see citing works

Synthesis, SAR, and application of JQ1 analogs as PROTACs for cancer therapy

De, S., Sahu, R., Palei, S., & Nanda, L. N. (2024) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2024.117875 · Cited by 8 · see citing works

Advances in BRET probes for intracellular target engagement studies

Capener, J. L., Schwalm, M. P., Vasta, J. D., Michaud, A., Teske, K. A., Marsiglia, W. M., Huber, K., Dar, A. C., Knapp, S., Axtman, A. D., et al. (2026) · Nature Chemical Biology · doi:10.1038/s41589-025-02103-y · Cited by 8 · see citing works

Toward effective Atg8‐based ATTECs: Approaches and perspectives

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Targeting LC3/GABARAP for degrader development and autophagy modulationPreprint

Schwalm, M. P., Dopfer, J., Kumar, A. M., Greco, F., Bauer, N., Löhr, F., Heering, J., Cano, S., Lechner, S., Hanke, T., et al. (2023) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2023.10.05.560930 · Cited by 7 · see citing works

Targeted Protein Degradation of NUDT5 Reveals an Unexpected Non-Enzymatic Role in 6-Thioguanine-Mediated ToxicityPreprint

Marques, A.-S. M. C., Bauer, L. G., Nguyen, T. A., Orta, A. G., Venne, J. L., Cheng, L., Balıkçı, E., Tivon, B., London, N., Kubicek, S., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.03.16.643557 · Cited by 7 · see citing works

Inhibition of bromodomain and extra-terminal proteins targets constitutively active NFκB and STAT signaling in lymphoma and influences the expression of the antiapoptotic proteins BCL2A1 and c-MYC

Pieper, N. M., Schnell, J., Brücher, D., Knapp, S., & Vogler, M. (2024) · Cell Communication and Signaling · doi:10.1186/s12964-024-01782-9 · Cited by 5 · see citing works

Direct degradation and stabilization of proteins: New horizons in treatment of nonalcoholic steatohepatitis

Wang, Y., Zheng, J., Long, Y., Wu, W., & Zhu, Y. (2023) · Biochemical Pharmacology · doi:10.1016/j.bcp.2023.115989 · Cited by 5 · see citing works

High-Throughput Screening for LC3/GABARAP Binders Utilizing the Fluorescence Polarization Assay

Schwalm, M. P., Dopfer, J., Knapp, S., & Rogov, V. V. (2024) · Methods in molecular biology · doi:10.1007/978-1-0716-4067-8_17 · Cited by 5 · see citing works

Selective steroid receptor modulators, degraders and PROTACs: Therapeutic strategies in management of endocrine-related cancers

Tripathi, A., Chhabra, A., Rizvi, S., & Tyagi, R. K. (2025) · Molecular and Cellular Endocrinology · doi:10.1016/j.mce.2025.112569 · Cited by 4 · see citing works

Dynamic characteristics of proteolysis-targeting chimera systems revealed by in silico computations

Xu, K., Ge, J., Tang, R., Hou, T., & Sun, H. (2025) · Current Opinion in Structural Biology · doi:10.1016/j.sbi.2025.103151 · Cited by 5 · see citing works

Targeted degradation of BRD4 by PROTACs: advances in cancer therapy

Hong, Y., Liu, X., Li, Y., Yu, M., Wang, C., Nie, C., & Xu, S. (2026) · Chemical Communications · doi:10.1039/d5cc05563f · Cited by 4 · see citing works

Target Engagement Studies and Kinetic Live-Cell Degradation Assays Enable the Systematic Characterization of Histone Deacetylase 6 Degraders

Hanl, M., Feller, F., Honin, I., Tan, K., Miranda, M., Schäker‐Hübner, L., Bückreiß, N., Schiedel, M., Gütschow, M., Bendas, G., et al. (2025) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.5c00247 · Cited by 3 · see citing works

Ginsenoside Rh2- functionalized liposomes enhanced BRD4-PROTAC delivery and antitumor efficacy via improved tumor targeting and ECM remodeling

Wen, L., Rao, J., Chen, J., Li, F., Chen, X., Guo, S., Cui, B., 邱财生, & Chen, W. (2026) · Materials Today Bio · doi:10.1016/j.mtbio.2026.102767 · Cited by 3 · see citing works

Effects of Biguanide-PROTACs in Pancreatic Cancer Cells

Vatté, J., Bourdeau, V., Ferbeyre, G., & Schmitzer, A. R. (2024) · Molecules · doi:10.3390/molecules29225329 · Cited by 3 · see citing works

Application of mass spectrometry for the advancement of PROTACs

Hao, Y., Zhang, B., & Chen, R. (2025) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2025.116829 · Cited by 3 · see citing works

Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators

Liu, Y., Nowak, R. P., Che, J., Donovan, K. A., Huerta, F., Liu, H., Metivier, R. J., Fischer, E. S., & Jones, L. H. (2024) · RSC Medicinal Chemistry · doi:10.1039/d3md00652b · Cited by 3 · see citing works

Predicting PROTAC-targeted Degradation and Designing Androgen Receptor Degraders with AiPROTACPreprint

Zhang, L., Sun, R., Li, X., Ren, C., Long, Y., Tan, W., Wang, X., Zou, K., Yang, X., Wu, M., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.02.26.640266 · Cited by 3 · see citing works

Biochemical investigation of LC3/GABARAP-ligand interaction as an important quality measure for LC3/GABARAP-targeting small molecules: addendum to the guidelines (4th edition)

Schwalm, M. P., Lenz, C., Saxena, K., Klionsky, D. J., Proschak, E., & Knapp, S. (2025) · Autophagy · doi:10.1080/15548627.2025.2498506 · Cited by 2 · see citing works

Multitargeted protein degradation: Integrating small-molecule, biomacromolecular, and nano-PROTACs for paradigm shifts in drug discovery

Yang, J., Zhang, Y., Zhang, M., Xing, D., & Wang, C. (2025) · Materials Today Advances · doi:10.1016/j.mtadv.2025.100644 · Cited by 3 · see citing works

Emerging pharmacology of targeted protein degraders

Barghout, S. H., & Eldeeb, M. A. (2025) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/j.jpet.2025.103694 · Cited by 2 · see citing works

Antibody-PROTAC Conjugate Enables Selective Degradation of Receptor-Interacting Serine/Threonine-Protein Kinase 2 (RIPK2) in HER+ Cell LinesPreprint

Chan, K., Sathyamurthi, P. S., Queisser, M. A., Mullin, M. J., Shrives, H. J., Coe, D. M., & Burley, G. A. (2023) · ChemRxiv · doi:10.26434/chemrxiv-2023-97zdb · Cited by 2 · see citing works

Rapid proteasomal degradation of mutant feline McDonough sarcoma-like tyrosine kinase-3 overcomes tyrosine kinase inhibitor resistance of acute myeloid leukemia cellsPreprint

Halilovic, M., Abdelsalam, M. A. M., Mieland, A. O., Neuroth, S., Ashry, R., Zabkiewicz, J., Lazenby, M., Alvares, C. L., Schmidt, M., Brenner, W., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.06.20.660791 · Cited by 2 · see citing works

Targeting Epigenetic Readers Using Small Molecule Binders and PROTAC Degraders

Boccia, E., Gazzillo, E., Chini, M. G., Bifulco, G., & Lauro, G. (2024) · Interdisciplinary cancer research · doi:10.1007/16833_2024_240 · Cited by 1 · see citing works

High-Quality In Vivo Chemical Probes for Protein Kinases Disclosed in 2024

Serafim, R. A. M., & Gehringer, M. (2025) · ACS Pharmacology & Translational Science · doi:10.1021/acsptsci.5c00293 · Cited by 1 · see citing works

Protacs in oral cancer: degrading oncogenic drivers for next-generation therapy

Prasad, P., Maslamani, M. J. M. A., Dinislam, K., Syed, T., & Shamsi, A. (2026) · Frontiers in Oral Health · doi:10.3389/froh.2026.1691816 · Cited by 1 · see citing works

PROTAC-based protein degradation: a window of opportunity for melanoma therapy

Gentile, G., D’Aguanno, S., Martile, M. D., Petricca, A., Valentini, E., Scalera, S., & Bufalo, D. D. (2026) · Journal of Biomedical Science · doi:10.1186/s12929-026-01225-2 · Cited by 1 · see citing works

Discovery of a Selective Histone Deacetylase 6 Degrader (HDAC6 PROTAC) with a Short and Rigid Linker Demonstrating Sustained Knockdown of HDAC6 In Vivo

Ripa, L., Cassani, C., Hughes, G. A., Ranieri, B., Ullah, V., Zambelloni, R., Andreasson, T., Collins, M., Lindberg, B., Llinàs, A., et al. (2026) · ACS Medicinal Chemistry Letters · doi:10.1021/acsmedchemlett.6c00086 · Cited by 1 · see citing works

On the Scope of DCAF1-Recruiting PROTACs Degrading Protein Kinases

Weckesser, J., Miletić, N., Sivashanmugam, S. A., Ohmayer, U., Steger, M., Shashikadze, B., Gehrtz, P., Lopez, A. U., Wegener, A. A., Dietz, T. J., et al. (2026) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6c00383 · Cited by 1 · see citing works

Next-generation strategies for PROTAC formulation: mechanistic insights and advanced formulation technologies

Maurya, A. K., Padrela, L., Agrawal, A. K., Kumar, A., & Kumar, D. M. (2026) · Expert Opinion on Drug Delivery · doi:10.1080/17425247.2026.2697992 · Cited by 1 · see citing works

Entdeckung eines potenten PROTAC ermöglicht die gezielte Ausschaltung der Gerüstfunktionen von FKBP51

Geiger, T. M., Walz, M., Meyners, C., Kuehn, A., Dreizler, J. K., Sugiarto, W. O., Maciel, E. V. S., Zheng, M., Lermyte, F., & Hausch, F. (2023) · Angewandte Chemie · doi:10.1002/ange.202309706 · Cited by 1 · see citing works

Bivalent ligands as a new universal chemotype of BCL6 degrader by inducing aggregationPreprint

Hu, R., Hu, X.-T., Yang, Y.-Y., Luo, P., Li, C., Liu, Z., Yu, L., & Wang, N. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.02.25.638777 · Cited by 1 · see citing works

Cellular selectivity and kinetics of clinical kinase inhibitors

Berger, L. M. (2023) · doi:10.21248/gups.72279

Biguanide-PROTACs: Modulating Mitochondrial Proteins in Pancreatic Cancer CellsPreprint

Vatté, J., Bourdeau, V., Ferbeyre, G., & Schmitzer, A. R. (2024) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2024.03.17.585436

Covalency in PROTACs: Mechanisms and applications

Geiger, T. M., & Nowak, R. P. (2024) · Annual reports in medicinal chemistry · doi:10.1016/bs.armc.2024.10.001

Target engagement studies and kinetic live-cell degradation assays enable the systematic characterization of HDAC6 PROTACsPreprint

Hanl, M., Feller, F., Honin, I., Tan, K., Miranda, M., Schäker-Hübner, L., Bückreiß, N., Schiedel, M., Gütschow, M., Bendas, G., et al. (2025) · bioRxiv (Cold Spring Harbor Laboratory) · doi:10.1101/2025.03.31.646177

Integrating PROTAC technology with natural product research: A new frontier in target identification

Wei, B., Dong, J., Liang, Y., Qin, J., & Kai, G. (2025) · Elsevier eBooks · doi:10.1016/b978-0-443-21816-3.00003-8

Protease-mediated degradation

Yang, L., Duan, H., Mao, X., Li, B., Che, J., & Dong, X. (2025) · Elsevier eBooks · doi:10.1016/b978-0-443-21816-3.00004-x

Advancing cancer immunotherapy: Small-Molecule, biomacromolecular, and nanoscale PROTACs targeting PD-L1 for degradation

Meng, Y., Zhang, Y., Yu, W., Xing, D., & Wang, C. (2025) · Materials Today Advances · doi:10.1016/j.mtadv.2025.100606

Additional file 2 of Inhibition of bromodomain and extra-terminal proteins targets constitutively active NFκB and STAT signaling in lymphoma and influences the expression of the antiapoptotic proteins BCL2A1 and c-MYC

Pieper, N. M., Schnell, J., Brücher, D., Knapp, S., & Vogler, M. (2024) · Figshare · doi:10.6084/m9.figshare.26860681

Additional file 1 of Inhibition of bromodomain and extra-terminal proteins targets constitutively active NFκB and STAT signaling in lymphoma and influences the expression of the antiapoptotic proteins BCL2A1 and c-MYC

Pieper, N. M., Schnell, J., Brücher, D., Knapp, S., & Vogler, M. (2024) · Figshare · doi:10.6084/m9.figshare.26860616

Advancing precision oncology through hNQO1-activatable NIR-II probes: Integrating molecular imaging with artificial intelligence

Egbewole, B. I., Oisakede, E. O., Egbon, E., Bello, O. J., Analikwu, C. C., & Olawade, D. B. (2026) · Intelligent Oncology · doi:10.1016/j.intonc.2026.100053

Analogues et outils moléculaires de composés naturels ciblant la protéine OSBP : synthèse et validation biologique

Guimard, C. (2023) · doi:10.70675/4cf5ceadz24a5z4e83zaaccz10a4bf56eb61

Targeted Protein Degradation of NUDT5 Dissociates Catalytic Inhibition from Protein Loss in 6-Thioguanine Response

Marques, A.-S. M. C., Bauer, L. G., Nguyen, T., Orta, A. G., Venne, J. L., Cheng, C., Balıkçı, E., Liu, Y., Tivon, B., Kroupova, A., et al. (2026) · Nature Communications · doi:10.1038/s41467-026-74489-9

Atomic degradation: chemical design strategies and immunotherapeutic mechanisms of radio-PROTACs

Varol, T. Ö., & Varol, M. (2026) · Annals of Nuclear Medicine · doi:10.1007/s12149-026-02254-5

The role of E3 ubiquitin ligases in selective types of macroautophagy

Müller, M., Winklhofer, K. F., & Reggiori, F. (2026) · EMBO Reports · doi:10.1038/s44319-026-00887-1

Sprayable androgen receptor PROTAC degrader for immunomodulation and accelerated skin regeneration

Jang, S. Y., Park, B., Ko, E., 신동원, Jang, Y., Lee, W. S., Lee, J.-H., Lee, A., Park, J., Lee, S. P., et al. (2026) · Chemical Engineering Journal · doi:10.1016/j.cej.2026.179954

T-type calcium channel blockers: a review of recent advances (2018–2025)

Tamboli, Y., Ferron, L., & Zamponi, G. W. (2026) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2026.2713553

Pocket-PROTACs: an interpretable pocket-aware deep learning framework for predicting PROTAC-induced protein degradation

Chen, K., Huang, Z., Wang, Y., Shen, S., Song, J.-P., & Deng, L. (2026) · Bioinformatics · doi:10.1093/bioinformatics/btag431

Proteolysis Targeting Chimeras (PROTACs): Design and Mechanism

Lin, X., Zhang, Y., & Wang, C. (2026) · Handbook of experimental pharmacology · doi:10.1007/164_2026_838

Expanding the chemical biology toolbox: cyclic peptides emerging as versatile chemical probes

Pebody, K. H., & Kawamura, A. (2026) · Essays in Biochemistry · doi:10.1042/ebc20260008

Fitness criteria for PROTACs as chemical probes: principles and applications

Sturbaut, M., & Ciulli, A. (2026) · Essays in Biochemistry · doi:10.1042/ebc20260006

BindingDB Entry 50022943: Synthesis, SAR, and application of JQ1 analogs as PROTACs for cancer therapy.

BindingDB (2026) · UC San Diego · doi:10.7270/q2xg9wzj

BindingDB Entry 50019841: From PROTAC to inhibitor: Structure-guided discovery of potent and orally bioavailable BET inhibitors.

BindingDB (2024) · UC San Diego · doi:10.7270/q2k93cxs

BindingDB Entry 50020602: Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators.

BindingDB (2024) · UC San Diego · doi:10.7270/q2cv4p64

BindingDB Entry 50021782: Expanding the ligand spaces for E3 ligases for the design of protein degraders.

BindingDB (2025) · UC San Diego · doi:10.7270/q2b85dsn

BindingDB Entry 50023383: Discovery and Functional Characterization of a Potent, Selective, and Metabolically Stable PROTAC of the Protein Kinases DYRK1A and DYRK1B.

BindingDB (2026) · UC San Diego · doi:10.7270/q2348r93

BindingDB Entry 50019872: Expanding Chemical Probe Space: Quality Criteria for Covalent and Degrader Probes.

BindingDB (2024) · UC San Diego · doi:10.7270/q2gb28f9

BindingDB Entry 50022043: Stereochemical inversion at a 1,4-cyclohexyl PROTAC linker fine-tunes conformation and binding affinity.

BindingDB (2025) · UC San Diego · doi:10.7270/q2891bkb

BindingDB Entry 50020617: Application of Novel Degraders Employing Autophagy for Expediting Medicinal Research.

BindingDB (2024) · UC San Diego · doi:10.7270/q23b64kj

Rapid proteasomal degradation of mutant feline McDonough sarcoma-like tyrosine kinase-3 overcomes inhibitor resistance mechanisms of acute myeloid leukemia cells

Halilovic, M., Abdelsalam, M. A. M., Mieland, A. O., Neuroth, S., Ashry, R., Schwarting, M. E. S., Zabkiewicz, J., Lazenby, M., Alvares, C. L., Schmidt, M., et al. (2026) · Leukemia · doi:10.1038/s41375-026-03168-x

Fitness criteria for PROTACs as chemical probes: principles and applications

Sturbaut, M., & Ciulli, A. (2026) · Essays in Biochemistry · doi:10.1042/ebc20260006

Quantitative Live-Cell Kinetic Degradation and Mechanistic Profiling of PROTAC Mode of Action

Riching, K. M., Mahan, S. D., Corona, C. R., McDougall, M. G., Vasta, J. D., Robers, M. B., Urh, M., & Daniels, D. L. (2018) · ACS Chemical Biology · doi:10.1021/acschembio.8b00692 · Cited by 307 · see citing works

Assays and Technologies for Developing Proteolysis Targeting Chimera Degraders

Liu, X., Zhang, X., Lv, D., Yuan, Y., Zheng, G., & Zhou, D. (2020) · Future Medicinal Chemistry · doi:10.4155/fmc-2020-0073 · Cited by 73 · see citing works

Targeted protein degradation: elements of PROTAC design

Paiva, S.-L., & Crews, C. M. (2019) · Current Opinion in Chemical Biology · doi:10.1016/j.cbpa.2019.02.022 · Cited by 586 · see citing works

Monitoring and deciphering protein degradation pathways inside cells

Daniels, D. L., Riching, K. M., & Urh, M. (2018) · Drug Discovery Today Technologies · doi:10.1016/j.ddtec.2018.12.001 · Cited by 68 · see citing works