Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 2: Improvement of In Vitro Antiproliferation Activity and In Vivo Antitumor Efficacy

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

Strategies and challenges for the next generation of antibody–drug conjugates

Beck, A., Goetsch, L., Dumontet, C., & Corvaïa, N. (2017) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2016.268 · Cited by 2,271 · see citing works

Phthalimide conjugation as a strategy for in vivo target protein degradation

Winter, G. E., Buckley, D. L., Paulk, J., Roberts, J. M., Souza, A., Dhe-Paganon, S., & Bradner, J. E. (2015) · Science · doi:10.1126/science.aab1433 · Cited by 1,760 · 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

DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1

Ogitani, Y., Aida, T., Hagihara, K., Yamaguchi, J., Ishii, C., Harada, N., Soma, M., Okamoto, H., Oitate, M., Arakawa, S., et al. (2016) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-15-2822 · Cited by 1,214 · 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

Targeted protein degradation: expanding the toolbox

Schapira, M., Calabrese, M. F., Bullock, A. N., & Crews, C. M. (2019) · Nature Reviews Drug Discovery · doi:10.1038/s41573-019-0047-y · Cited by 960 · see citing works

Antibody–Drug Conjugates: An Emerging Concept in Cancer Therapy

Chari, R. V. J., Miller, M. L., & Widdison, W. C. (2014) · Angewandte Chemie International Edition · doi:10.1002/anie.201307628 · Cited by 930 · 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 COVALENT STRUCTURE OF AN ENTIRE γG IMMUNOGLOBULIN MOLECULE

Edelman, G. M., Cunningham, B. A., Gall, W. E., Gottlieb, P. D., Rutishauser, U. S., & Waxdal, M. J. (1969) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.63.1.78 · Cited by 903 · see citing works

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

Raina, K., Lu, J., Qian, Y., Altieri, M., Gordon, D., Rossi, A. M. K., Wang, J., Chen, X., Dong, H., Siu, K., et al. (2016) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.1521738113 · Cited by 852 · 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

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

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

PROTACs: An Emerging Therapeutic Modality in Precision Medicine

Nalawansha, D. A., & Crews, C. M. (2020) · Cell chemical biology · doi:10.1016/j.chembiol.2020.07.020 · Cited by 514 · 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

Two Decades under the Influence of the Rule of Five and the Changing Properties of Approved Oral Drugs

Shultz, M. D. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00686 · Cited by 456 · see citing works

Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation

Gilan, O., Rioja, I., Knezevic, K., Bell, M. J., Yeung, M. M., Harker, N., Lam, E. Y. N., Chung, C., Bamborough, P., Petretich, M., et al. (2020) · Science · doi:10.1126/science.aaz8455 · Cited by 446 · see citing works

Bromodomain inhibitor OTX015 in patients with acute leukaemia: a dose-escalation, phase 1 study

Berthon, C., Raffoux, E., Thomas, X., Vey, N., Gomez‐Roca, C., Yee, K. W. L., Taussig, D. C., Rezaï, K., Roumier, C., Herait, P., et al. (2016) · The Lancet Haematology · doi:10.1016/s2352-3026(15)00247-1 · Cited by 423 · see citing works

Bromodomain inhibitor OTX015 in patients with lymphoma or multiple myeloma: a dose-escalation, open-label, pharmacokinetic, phase 1 study

Amorim, S., Stathis, A., Gleeson, M., Iyengar, S., Magarotto, V., Leleu, X. P., Morschhauser, F., Karlin, L., Broussais, F., Rezaï, K., et al. (2016) · The Lancet Haematology · doi:10.1016/s2352-3026(16)00021-1 · Cited by 422 · 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

Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer

Faivre, E. J., McDaniel, K. F., Albert, D. H., Mantena, S. R., Plotnik, J. P., Wilcox, D., Zhang, L., Bui, M. H., Sheppard, G. S., Wang, L., et al. (2020) · Nature · doi:10.1038/s41586-020-1930-8 · Cited by 408 · see citing works

Discovery of ARD-69 as a Highly Potent Proteolysis Targeting Chimera (PROTAC) Degrader of Androgen Receptor (AR) for the Treatment of Prostate Cancer

Han, X., Wang, C., Qin, C., Xiang, W., Fernández‐Salas, E., Yang, C., Wang, M., Zhao, L., Xu, T., Chinnaswamy, K., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01631 · Cited by 404 · 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

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression

Zhou, B. N., Hu, J., Xu, F., Chen, Z., Bai, L., Fernández‐Salas, E., Lin, M., Liu, L., Yang, C., Zhao, Y., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01816 · Cited by 373 · see citing works

Antibody–PROTAC Conjugates Enable HER2-Dependent Targeted Protein Degradation of BRD4

Maneiro, M., Forte, N., Shchepinova, M. M., Kounde, C. S., Chudasama, V., Baker, J. R., & Tate, E. W. (2020) · ACS Chemical Biology · doi:10.1021/acschembio.0c00285 · Cited by 350 · see citing works

Drug Discovery Targeting Bromodomain-Containing Protein 4

Liu, Z., Wang, P., Chen, H., Wold, E. A., Tian, B., Brasier, A. R., & Zhou, J. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01761 · Cited by 325 · 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

Small-Molecule Modulation of Protein Homeostasis

Burslem, G. M., & Crews, C. M. (2017) · Chemical Reviews · doi:10.1021/acs.chemrev.7b00077 · Cited by 294 · see citing works

Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tumor Regression

Qin, C., Hu, Y., Zhou, B., Fernandez-Salas, E., Yang, C.-Y., Liu, L., McEachern, D., Przybranowski, S., Wang, M., Stuckey, J., et al. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00506 · Cited by 281 · see citing works

Using proteolysis-targeting chimera technology to reduce navitoclax platelet toxicity and improve its senolytic activity

He, Y., Zhang, X., Chang, J., Kim, H.-N., Zhang, P., Wang, Y., Khan, S., Liu, X., Zhang, X., Lv, D., et al. (2020) · Nature Communications · doi:10.1038/s41467-020-15838-0 · Cited by 280 · 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

Optimising proteolysis-targeting chimeras (PROTACs) for oral drug delivery: a drug metabolism and pharmacokinetics perspective

Pike, A., Williamson, B., Harlfinger, S., Martin, S. W., & McGinnity, D. F. (2020) · Drug Discovery Today · doi:10.1016/j.drudis.2020.07.013 · Cited by 247 · see citing works

In Vivo Knockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)

Ohoka, N., Okuhira, K., Ito, M., Nagai, K., Shibata, N., Hattori, T., Ujikawa, O., Shimokawa, K., Sano, O., Koyama, R., et al. (2017) · Journal of Biological Chemistry · doi:10.1074/jbc.m116.768853 · Cited by 240 · see citing works

Inhibition of BET bromodomains as a therapeutic strategy for cancer drug discovery

Fu, L., Tian, M., Li, X., Li, J., Huang, J. M., Ouyang, L., Zhang, Y., & Liu, B. (2015) · Oncotarget · doi:10.18632/oncotarget.3551 · Cited by 223 · see citing works

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

Chan, K.-H., Zengerle, M., Testa, A., & Ciulli, A. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.6b01912 · Cited by 222 · see citing works

Antibody Conjugation of a Chimeric BET Degrader Enables <i>in vivo</i> Activity

Pillow, T. H., Adhikari, P., Blake, R. A., Chen, J., Del Rosario, G., Deshmukh, G., Figueroa, I., Gascoigne, K. E., Kamath, A. V., Kaufman, S., et al. (2020) · ChemMedChem · doi:10.1002/cmdc.201900497 · Cited by 216 · see citing works

Disrupting Acetyl-Lysine Recognition: Progress in the Development of Bromodomain Inhibitors

Romero, F. A., Taylor, A. M., Crawford, T. D., Tsui, V., Côté, A., & Magnuson, S. R. (2015) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.5b01514 · Cited by 194 · see citing works

Covalent Inhibition of Bacterial Quorum Sensing

Amara, N., Mashiach, R., Amar, D., Krief, P., Spieser, S. A. H., Bottomley, M. J., Aharoni, A., & Meijler, M. M. (2009) · Journal of the American Chemical Society · doi:10.1021/ja903292v · Cited by 190 · see citing works

Advances in antibody–drug conjugates: A new era of targeted cancer therapy

Sau, S., Alsaab, H. O., Kashaw, S. K., Tatiparti, K., & Iyer, A. K. (2017) · Drug Discovery Today · doi:10.1016/j.drudis.2017.05.011 · Cited by 177 · see citing works

First-in-human phase I study of ARV-110, an androgen receptor (AR) PROTAC degrader in patients (pts) with metastatic castrate-resistant prostate cancer (mCRPC) following enzalutamide (ENZ) and/or abiraterone (ABI).

Petrylak, D. P., Gao, X., Vogelzang, N. J., Garfield, M. H., Taylor, I., Dougan Moore, M., Peck, R. A., & Burris, H. A. (2020) · Journal of Clinical Oncology · doi:10.1200/jco.2020.38.15_suppl.3500 · Cited by 169 · see citing works

Fundamental aspects of DMPK optimization of targeted protein degraders

Cantrill, C., Chaturvedi, P., Rynn, C., Schaffland, J. P., Walter, I., & Wittwer, M. (2020) · Drug Discovery Today · doi:10.1016/j.drudis.2020.03.012 · Cited by 169 · see citing works

Targeting Brd4 for cancer therapy: inhibitors and degraders

Duan, Y., Guan, Y., Qin, W., Zhai, X., Yu, B., & Liu, H. (2018) · MedChemComm · doi:10.1039/c8md00198g · Cited by 165 · see citing works

Developing degraders: principles and perspectives on design and chemical space

Maple, H. J., Clayden, N., Baron, A., Stacey, C., & Felix, R. L. (2019) · MedChemComm · doi:10.1039/c9md00272c · Cited by 159 · see citing works

Development of Protein Degradation Inducers of Androgen Receptor by Conjugation of Androgen Receptor Ligands and Inhibitor of Apoptosis Protein Ligands

Shibata, N., Nagai, K., Morita, Y., Ujikawa, O., Ohoka, N., Hattori, T., Koyama, R., Sano, O., Imaeda, Y., Nara, H., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00168 · Cited by 147 · see citing works

Discovery of Pyrophosphate Diesters as Tunable, Soluble, and Bioorthogonal Linkers for Site-Specific Antibody–Drug Conjugates

Kern, J. C., Cancilla, M. T., Dooney, D., Kwasnjuk, K., Zhang, R., Beaumont, M., Figueroa, I., Hsieh, S., Liang, L. A., Tomazela, D. M., et al. (2016) · Journal of the American Chemical Society · doi:10.1021/jacs.5b12547 · Cited by 143 · see citing works

Decoupling stability and release in disulfide bonds with antibody-small molecule conjugates

Pillow, T. H., Sadowsky, J., Zhang, D., Yu, S., Rosario, G. D., Xu, K., He, J., Bhakta, S., Ohri, R. V., Kozak, K. R., et al. (2016) · Chemical Science · doi:10.1039/c6sc01831a · Cited by 142 · see citing works

Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain

Sheppard, G. S., Wang, L., Fidanze, S. D., Hasvold, L. A., Liu, D., Pratt, J. K., Park, C. H., Longenecker, K. L., Qiu, W., Torrent, M., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00628 · Cited by 139 · see citing works

Highly Selective PTK2 Proteolysis Targeting Chimeras to Probe Focal Adhesion Kinase Scaffolding Functions

Popow, J., Arnhof, H., Bader, G., Berger, H., Ciulli, A., Covini, D., Dank, C., Gmaschitz, T., Greb, P., Karolyi-Özguer, J., et al. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01826 · Cited by 138 · see citing works

Discovery of PROTAC BCL-XL degraders as potent anticancer agents with low on-target platelet toxicity

Zhang, X., Thummuri, D., Liu, X., Hu, W., Zhang, P., Khan, S., Yuan, Y., Zhou, D., & Zheng, G. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112186 · Cited by 123 · see citing works

Antibody-mediated delivery of chimeric protein degraders which target estrogen receptor alpha (ERα)

Dragovich, P. S., Adhikari, P., Blake, R. A., Blaquiere, N., Chen, J., Cheng, Y.-X., den Besten, W., Han, J., Hartman, S. J., He, J., et al. (2020) · Bioorganic &amp; Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2019.126907 · Cited by 120 · see citing works

A chemical approach for global protein knockdown from mice to non-human primates

Sun, X., Wang, J., Yao, X., Zheng, W., Mao, Y., Lan, T., Wang, L., Sun, Y., Zhang, X., Zhao, Q., et al. (2019) · Cell Discovery · doi:10.1038/s41421-018-0079-1 · Cited by 118 · see citing works

Discovery of Peptidomimetic Antibody–Drug Conjugate Linkers with Enhanced Protease Specificity

Wei, B. Q., Gunzner, J. L., Yao, H., Wang, T., Wang, J., Xu, Z., Chen, J., Wai, J. S. M., Nonomiya, J., Tsai, S. P., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01430 · Cited by 109 · see citing works

High-Throughput Cysteine Scanning To Identify Stable Antibody Conjugation Sites for Maleimide- and Disulfide-Based Linkers

Ohri, R. V., Bhakta, S., Fourie-O’Donohue, A., Cruz-Chuh, J. D., Tsai, S. P., Cook, R., Wei, B. Q., Ng, C., Wong, A. W., Bos, A. B., et al. (2018) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.7b00791 · Cited by 109 · see citing works

Monodisperse polysarcosine-based highly-loaded antibody-drug conjugates

Viricel, W., Fournet, G., Beaumel, S., Cros‐Perrial, E., Papot, S., Dumontet, C., & Joseph, B. (2019) · Chemical Science · doi:10.1039/c9sc00285e · Cited by 101 · see citing works

GSK789: A Selective Inhibitor of the First Bromodomains (BD1) of the Bromo and Extra Terminal Domain (BET) Proteins

Watson, R. J., Bamborough, P., Barnett, H., Chung, C., Davis, R. P., Gordon, L. J., Grandi, P., Petretich, M., Phillipou, A., Prinjha, R. K., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00614 · Cited by 98 · see citing works

Immobilized liposome and biomembrane partitioning chromatography of drugs for prediction of drug transport

Beigi, F., Gottschalk, I., Hägglund, C. L., et al. (1998) · International Journal of Pharmaceutics · doi:10.1016/s0378-5173(97)00398-0 · Cited by 97 · see citing works

A Novel Anti-HER2 Antibody–Drug Conjugate XMT-1522 for HER2-Positive Breast and Gastric Cancers Resistant to Trastuzumab Emtansine

Joncour, V. L., Martins, A., Puhka, M., Isola, J. J., Salmikangas, M., Laakkonen, P., Joensuu, H., & Barok, M. (2019) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-19-0207 · Cited by 86 · see citing works

Efficient synthesis of γ-methyl-capped guanosine 5′-triphosphate as a 5′-terminal unique structure of U6 RNA via a new triphosphate bond formation involving activation of methyl phosphorimidazolidate using ZnCl2 as a catalyst in DMF under anhydrous conditions

Kadokura, M., Wada, T., Urashima, C., et al. (1997) · Tetrahedron Letters · doi:10.1016/s0040-4039(97)10263-5 · Cited by 78 · see citing works

The Optimization of a Novel, Weak Bromo and Extra Terminal Domain (BET) Bromodomain Fragment Ligand to a Potent and Selective Second Bromodomain (BD2) Inhibitor

Seal, J. T., Atkinson, S. J., Aylott, H. E., Bamborough, P., Chung, C., Copley, R. C. B., Gordon, L. J., Grandi, P., Gray, J. R., Harrison, L. A., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00796 · Cited by 76 · see citing works

A Self-Immolative Spacer That Enables Tunable Controlled Release of Phenols under Neutral Conditions

Schmid, K. M., Jensen, L., & Phillips, S. T. (2012) · The Journal of Organic Chemistry · doi:10.1021/jo300400q · Cited by 74 · see citing works

Modulating Therapeutic Activity and Toxicity of Pyrrolobenzodiazepine Antibody–Drug Conjugates with Self-Immolative Disulfide Linkers

Pillow, T. H., Schutten, M. M., Yu, S., Ohri, R. V., Sadowsky, J., Poon, K. A., Solis, W. A., Zhong, F., Rosario, G. D., Go, M. A. T., et al. (2017) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-16-0641 · Cited by 72 · see citing works

Direct Measurement of Intracellular Compound Concentration by RapidFire Mass Spectrometry Offers Insights into Cell Permeability

Gordon, L. J., Allen, M., Artursson, P., et al. (2015) · SLAS DISCOVERY · doi:10.1177/1087057115604141 · Cited by 66 · see citing works

An Anti–CLL-1 Antibody–Drug Conjugate for the Treatment of Acute Myeloid Leukemia

Zheng, B., Yu, S., Rosario, G. D., Leong, S. R., Lee, G. Y., Vij, R., Chiu, C., Liang, W., Wu, Y. P., Chalouni, C. M., et al. (2018) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-18-0333 · Cited by 66 · see citing works

Design and Synthesis of a Highly Selective and In Vivo -Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins

Preston, A. G. S., Atkinson, S. J., Bamborough, P., Chung, C., Craggs, P. D., Gordon, L. J., Grandi, P., Gray, J. R., Jones, E. J., Lindon, M. J., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00605 · Cited by 64 · see citing works

Development of Efficient Chemistry to Generate Site-Specific Disulfide-Linked Protein– and Peptide–Payload Conjugates: Application to THIOMAB Antibody–Drug Conjugates

Sadowsky, J., Pillow, T. H., Chen, J., Fan, F., He, C., Wang, Y., Yan, G., Yao, H., Xu, Z., Martin, S. A., et al. (2017) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.7b00258 · Cited by 58 · see citing works

Development of Anti-CD74 Antibody–Drug Conjugates to Target Glucocorticoids to Immune Cells

Brandish, P. E., Palmieri, A., Antonenko, S. V., et al. (2018) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.8b00312 · Cited by 57 · see citing works

Structure-Based Design of a Bromodomain and Extraterminal Domain (BET) Inhibitor Selective for the N-Terminal Bromodomains That Retains an Anti-inflammatory and Antiproliferative Phenotype

Wellaway, C. R., Bamborough, P., Bernard, S. G., Chung, C., Craggs, P. D., Cutler, L., Demont, E. H., Evans, J. P., Gordon, L. J., Karamshi, B., et al. (2020) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c00566 · Cited by 57 · see citing works

Targeted Delivery of Cytotoxic NAMPT Inhibitors Using Antibody–Drug Conjugates

Neumann, C. S., Olivas, K. C., Anderson, M. E., Cochran, J. H., Jin, S., Li, F., Loftus, L. V., Meyer, D. W., Neale, J. R., Nix, J. C., et al. (2018) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-18-0643 · Cited by 51 · see citing works

Attachment Site Cysteine Thiol pKa Is a Key Driver for Site-Dependent Stability of THIOMAB Antibody–Drug Conjugates

Vollmar, B. S., Wei, B. Q., Ohri, R. V., Zhou, J., He, J., Yu, S., Leipold, D. D., Cosino, E., Yee, S. F., Fourie-O’Donohue, A., et al. (2017) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.7b00365 · Cited by 46 · see citing works

Immolation of p-Aminobenzyl Ether Linker and Payload Potency and Stability Determine the Cell-Killing Activity of Antibody–Drug Conjugates with Phenol-Containing Payloads

Zhang, D., Le, H., Cruz-Chuh, J. D., et al. (2018) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.7b00576 · Cited by 33 · see citing works

Preclinical models of nicotinamide phosphoribosyltransferase inhibitor-mediated hematotoxicity and mitigation by co-treatment with nicotinic acid

Tarrant, J. M., Dhawan, P., Singh, J., Zabka, T. S., Clarke, E., DosSantos, G., Dragovich, P. S., Sampath, D., Lin, T., McCray, B., et al. (2015) · Toxicology Mechanisms and Methods · doi:10.3109/15376516.2015.1014080 · Cited by 31 · see citing works

Application of human CFU-Mk assay to predict potential thrombocytotoxicity of drugs

Pessina, A., Parent‐Massin, D., Albella, B., et al. (2008) · Toxicology in Vitro · doi:10.1016/j.tiv.2008.11.006 · Cited by 29 · see citing works

Improved Methodology for the Synthesis of a Cathepsin B Cleavable Dipeptide Linker, Widely Used in Antibody-Drug Conjugate Research

(2018) · doi:10.1016/j.tetlet.2018.08.021 · Cited by 26 · see citing works

Application of in Situ Silylation for Improved, Convenient Preparation of Fluorenylmethoxycarbonyl (Fmoc)-Protected Phosphinate Amino Acids

Li, Whitehead, J. K., & Hammer, R. P. (2007) · The Journal of Organic Chemistry · doi:10.1021/jo070266p · Cited by 24 · see citing works

Translational Modeling of Drug-Induced Myelosuppression and Effect of Pretreatment Myelosuppression for AZD5153, a Selective BRD4 Inhibitor

Collins, T., Hattersley, M. M., Yates, J., et al. (2017) · CPT Pharmacometrics & Systems Pharmacology · doi:10.1002/psp4.12194 · Cited by 24 · see citing works

Improved translation of stability for conjugated antibodies using an in vitro whole blood assay

Fourie-O’Donohue, A., Chu, P. Y., Chuh, J., et al. (2020) · mAbs · doi:10.1080/19420862.2020.1715705 · Cited by 23 · see citing works

Glucuronide-Linked Antibody–Tubulysin Conjugates Display Activity in MDR+ and Heterogeneous Tumor Models

Burke, P., Hamilton, J. Z., Pires, T. A., Lai, H. W. H., Leiske, C. I., Emmerton, K. K., Waight, A. B., Senter, P. D., Lyon, R. P., & Jeffrey, S. C. (2018) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-18-0073 · Cited by 21 · see citing works

Antibody–Drug Conjugates Derived from Cytotoxic seco-CBI-Dimer Payloads Are Highly Efficacious in Xenograft Models and Form Protein Adducts In Vivo

Su, D., Chen, J., Cosino, E., et al. (2019) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.9b00133 · Cited by 21 · see citing works

Preclinical pharmacokinetics and pharmacodynamics of DCLL9718A: An antibody-drug conjugate for the treatment of acute myeloid leukemia

Leipold, D. D., Figueroa, I., Masih, S., Latifi, B., Yip, V., Shen, B., Dere, R. C., Carrasco‐Triguero, M., Lee, M. V., Saad, O. M., et al. (2018) · mAbs · doi:10.1080/19420862.2018.1517565 · Cited by 17 · see citing works

Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors

Fidanze, S. D., Liu, D., Mantei, R. A., Hasvold, L. A., Pratt, J. K., Sheppard, G. S., Wang, L., Holms, J. H., Dai, Y., Aguirre, A. L., et al. (2018) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2018.04.020 · Cited by 13 · see citing works

Conjugation of Indoles to Antibodies through a Novel Self‐Immolating Linker

Dragovich, P. S., Blake, R. A., Chen, C., et al. (2018) · Chemistry - A European Journal · doi:10.1002/chem.201800859 · Cited by 9 · see citing works

Abstract LB-097: Targeted degradation of the androgen receptor in prostate cancer

Jin, M., Winkler, J. D., Coleman, K. G., et al. (2015) · Cancer Research · doi:10.1158/1538-7445.am2015-lb-097 · Cited by 2 · see citing works

PROTAC targeted protein degraders: the past is prologue

Békés, M., Langley, D. R., & Crews, C. M. (2022) · Nature Reviews Drug Discovery · doi:10.1038/s41573-021-00371-6 · Cited by 3,395 · see citing works

Exploring the next generation of antibody–drug conjugates

Tsuchikama, K., Anami, Y., Ha, S. Y. Y., & Yamazaki, C. M. (2024) · Nature Reviews Clinical Oncology · doi:10.1038/s41571-023-00850-2 · Cited by 659 · see citing works

PROTACs: great opportunities for academia and industry (an update from 2020 to 2021)

He, M., Cao, C., Ni, Z., Liu, Y., Song, P., Hao, S., He, Y., Sun, X., & Rao, Y. (2022) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-022-00999-9 · Cited by 283 · 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

Targeting cancer with small-molecule pan-KRAS degraders

Popow, J., Farnaby, W., Gollner, A., Kofink, C., Fischer, G., Wurm, M., Zollman, D., Wijaya, A., Mischerikow, N., Hasenoehrl, C., et al. (2024) · Science · doi:10.1126/science.adm8684 · Cited by 198 · see citing works

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

Dragovich, P. S., Pillow, T. H., Blake, R. A., Sadowsky, J. D., Adaligil, E., Adhikari, P., Bhakta, S., Blaquiere, N., Chen, J., dela Cruz-Chuh, J., et al. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.0c01845 · Cited by 152 · see citing works

Integrative Modeling of PROTAC-Mediated Ternary Complexes

Weng, G., Li, D., Kang, Y., & Hou, T. (2021) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.1c01576 · Cited by 130 · see citing works

Modeling the CRL4A ligase complex to predict target protein ubiquitination induced by cereblon-recruiting PROTACs

Bai, N., Riching, K. M., Makaju, A., Wu, H., Acker, T. M., Ou, S.-C., Zhang, Y., Shen, X., Bulloch, D. N., Rui, H., et al. (2022) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2022.101653 · Cited by 77 · see citing works

Analysis and Control of Proteolysis of Recombinant Proteins in Escherichia coli

Rozkov, A., & Enfors, S. (2004) · Advances in biochemical engineering, biotechnology · doi:10.1007/b95567 · Cited by 62 · see citing works

Proteolysis in alfalfa silage and its inhibiting method

Guo, X., He, Z., & Liu, G. (2005) · Caoye kexue

Progress on Proteolysis in Bacterial Cells

Wang, H. (2008) · Letters in Biotechnology

Proteolysis Associated with Thymidine-Induced Selective Cell Death in L-Cell Cultures

Amenta, J. S., Mehta, J., & Baccino, F. M. (1988) · Springer eBooks · doi:10.1007/978-1-4757-9640-7_59 · Cited by 5 · see citing works

Proteolysis in the storage of beef

Locker, R. H. (1960) · Journal of the Science of Food and Agriculture · doi:10.1002/jsfa.2740110906 · Cited by 47 · see citing works