In vitro and in vivo degradation of programmed cell death ligand 1 (PD-L1) by a proteolysis targeting chimera (PROTAC)

Nivolumab plus Ipilimumab in Advanced Melanoma

Wolchok, J. D., Kluger, H., Callahan, M. K., Postow, M. A., Rizvi, N. A., Lesokhin, A. M., Segal, N. H., Ariyan, C. E., Gordon, R.-A., Reed, K., et al. (2013) · New England Journal of Medicine · doi:10.1056/nejmoa1302369 · Cited by 4,230 · see citing works

Immune Checkpoint Blockade: A Common Denominator Approach to Cancer Therapy

Topalian, S. L., Drake, C. G., & Pardoll, D. M. (2015) · Cancer Cell · doi:10.1016/j.ccell.2015.03.001 · Cited by 4,229 · see citing works

Immune checkpoint targeting in cancer therapy: toward combination strategies with curative potential

Sharma, P., & Allison, J. P. (2015) · Cell · doi:10.1016/j.cell.2015.03.030 · Cited by 2,345 · see citing works

Combination cancer immunotherapy and new immunomodulatory targets

Mahoney, K. M., Rennert, P. D., & Freeman, G. J. (2015) · Nature Reviews Drug Discovery · doi:10.1038/nrd4591 · Cited by 1,294 · see citing works

Cancer immunotherapy: the beginning of the end of cancer?

Farkona, S., Diamandis, E. P., & Blasutig, I. M. (2016) · BMC Medicine · doi:10.1186/s12916-016-0623-5 · Cited by 1,192 · see citing works

The future of cancer treatment: immunomodulation, CARs and combination immunotherapy

Khalil, D. N., Smith, E. L., Brentjens, R. J., & Wolchok, J. D. (2016) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2016.25 · Cited by 1,151 · see citing works

CMTM6 maintains the expression of PD-L1 and regulates anti-tumour immunity

Burr, M. L., Sparbier, C. E., Chan, Y.-C., Williamson, J. C., Woods, K., Beavis, P. A., Lam, E. Y. N., Henderson, M. A., Bell, C. C., Stolzenburg, S., et al. (2017) · Nature · doi:10.1038/nature23643 · Cited by 946 · see citing works

Combination cancer immunotherapies tailored to the tumour microenvironment

Smyth, M. J., Ngiow, S. F., Ribas, A., & Teng, M. W. L. (2016) · Nature Reviews Clinical Oncology · doi:10.1038/nrclinonc.2015.209 · Cited by 944 · see citing works

Coinhibitory Pathways in Immunotherapy for Cancer

Baumeister, S. H. C., Freeman, G. J., Dranoff, G., & Sharpe, A. H. (2016) · Annual Review of Immunology · doi:10.1146/annurev-immunol-032414-112049 · Cited by 912 · see citing works

Cancer and fertility preservation: international recommendations from an expert meeting

Lambertini, M., Mastro, L. D., Pescio, M. C., Andersen, C. Y., Azim, H. A., Peccatori, F. A., Costa, M., Revelli, A., Salvagno, F., Gennari, A., et al. (2016) · BMC Medicine · doi:10.1186/s12916-015-0545-7 · Cited by 787 · see citing works

Evolving synergistic combinations of targeted immunotherapies to combat cancer

Melero, I., Berman, D. M., Aznar, M. A., Korman, A. J., Perez‐Gracia, J. L., & Haanen, J. B. A. G. (2015) · Nature reviews. Cancer · doi:10.1038/nrc3973 · Cited by 633 · see citing works

Development of immuno-oncology drugs — from CTLA4 to PD1 to the next generations

Hoos, A. (2016) · Nature Reviews Drug Discovery · doi:10.1038/nrd.2015.35 · Cited by 601 · see citing works

Structural basis for small molecule targeting of the programmed death ligand 1 (PD-L1)

Żak, K. M., Grudnik, P., Guzik, K., Zieba, B. J., Musielak, B., Dömling, A. S. S., Dubin, G., & Holak, T. A. (2016) · Oncotarget · doi:10.18632/oncotarget.8730 · Cited by 443 · 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

Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1

Guzik, K., Żak, K. M., Grudnik, P., Magiera‐Mularz, K., Musielak, B., Törner, R., Skalniak, Ł., Dömling, A. S. S., Dubin, G., & Holak, T. A. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00293 · Cited by 380 · see citing works

The evolution of checkpoint blockade as a cancer therapy: what's here, what's next?

Shin, D. S., & Ribas, A. (2015) · Current Opinion in Immunology · doi:10.1016/j.coi.2015.01.006 · Cited by 344 · 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

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

Li, Y., Yang, J., Aguilar, A., McEachern, D., Przybranowski, S., Liu, L., Yang, C.-Y., Wang, M., Han, X., & Wang, S. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00909 · Cited by 312 · 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

Waste disposal—An attractive strategy for cancer therapy

Salami, J., & Crews, C. M. (2017) · Science · doi:10.1126/science.aam7340 · Cited by 279 · see citing works

Small-Molecule Modulation of Protein Homeostasis.

Burslem, G., & Crews, C. (2017) · Chemical Reviews · doi:10.1021/acs.chemrev.7b00077 · Cited by 256 · see citing works

Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC)

Robb, C. M., Contreras, J. I., Kour, S., Taylor, M., Abid, M., Sonawane, Y. A., Zahid, M., Murry, D. J., Natarajan, A., & Rana, S. (2017) · Chemical Communications · doi:10.1039/c7cc03879h · Cited by 221 · see citing works

From monoclonal antibodies to small molecules: the development of inhibitors targeting the PD-1/PD-L1 pathway

Zhan, M., Hu, X., Liu, X.-X., Ruan, B., Xu, J., & Liao, C. (2016) · Drug Discovery Today · doi:10.1016/j.drudis.2016.04.011 · Cited by 192 · see citing works

Induction of apoptosis in MDA-MB-231 breast cancer cells by a PARP1-targeting PROTAC small molecule

Zhao, Q., Lan, T., Su, S., & Rao, Y. (2018) · Chemical Communications · doi:10.1039/c8cc07813k · Cited by 185 · see citing works

Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion

Burslem, G. M., Song, J., Chen, X., Hines, J., & Crews, C. M. (2018) · Journal of the American Chemical Society · doi:10.1021/jacs.8b10320 · Cited by 176 · see citing works

Drug Discovery Targeting Anaplastic Lymphoma Kinase (ALK)

Kong, X., Pan, P., Sun, H., Xia, H., Wang, X., Li, Y., & Hou, T. (2019) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.9b00446 · Cited by 134 · see citing works

Discovery of novel resorcinol diphenyl ether-based PROTAC-like molecules as dual inhibitors and degraders of PD-L1

Cheng, B., Ren, Y., Cao, H., & Chen, J. (2020) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2020.112377 · Cited by 123 · see citing works

Cancer Immunotherapy: Selected Targets and Small‐Molecule Modulators

Weinmann, H. (2016) · ChemMedChem · doi:10.1002/cmdc.201500566 · Cited by 122 · see citing works

Inhibitors of programmed cell death 1 (PD-1): a patent review (2010-2015)

Zarganes‐Tzitzikas, T., Konstantinidou, M., Gao, Y., Krzemień, D., Żak, K. M., Dubin, G., Holak, T. A., & Dömling, A. S. S. (2016) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2016.1206527 · Cited by 102 · see citing works

Identification of a neo-epitope dominating endogenous CD8 T cell responses to MC-38 colorectal cancer

Hos, B. J., Camps, M. G. M., van den Bulk, J., Tondini, E., van den Ende, T. C., Ruano, D., Franken, K. L. M. C., Janssen, G. M. C., de Ru, A. H., Filippov, D. V., et al. (2019) · OncoImmunology · doi:10.1080/2162402x.2019.1673125 · Cited by 93 · see citing works

Membrane-Active Hydantoin Derivatives as Antibiotic Agents

Su, M., Xia, D., Teng, P., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b00847 · Cited by 91 · see citing works

Azetidine and Piperidine Carbamates as Efficient, Covalent Inhibitors of Monoacylglycerol Lipase

Butler, C. R., Beck, E. M., Harris, A. R., Huang, Z., McAllister, L. A., Ende, C. W. A., Fennell, K. F., Foley, T. L., Fonseca, K. R., Hawrylik, S. J., et al. (2017) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.7b01531 · Cited by 76 · see citing works

Targeted Degradation of MDM2 as a New Approach to Improve the Efficacy of MDM2-p53 Inhibitors

Wurz, R. P., & Cee, V. J. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b01945 · Cited by 75 · 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

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

Targeted protein modification as a paradigm shift in drug discovery

Amirian, R., Azadi Badrbani, M., Izadi, Z., Samadian, H., Bahrami, G., Sarvari, S., Abdolmaleki, S., Nabavi, S. M., Derakhshankhah, H., & Jaymand, M. (2023) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2023.115765 · Cited by 18 · see citing works

Dissecting Intracellular Proteolysis Using Small Molecule Inhibitors and Molecular Probes

Ovaa, H., Overkleeft, H. S., Kessler, B. M., & Ploegh, H. L. (2005) · doi:10.1002/9783527620210.ch3 · Cited by 2 · see citing works

Dissecting Intracellular Proteolysis Using Small Molecule Inhibitors and Molecular Probes

Ovaa, H., Overkleeft, H. S., Kessler, B. M., & Ploegh, H. L. (2007) · doi:10.1002/9783527619320.ch3a

Regulation of proteolysis

Attaix, D., Combaret, L., Pouch-Pélissier, M.-N., & Taillandier, D. (2001) · Current Opinion in Clinical Nutrition & Metabolic Care · doi:10.1097/00075197-200101000-00009 · Cited by 74 · see citing works

Proteasomes: protein degradation machines of the cell

Peters, J. (1994) · Trends in Biochemical Sciences · doi:10.1016/0968-0004(94)90115-5 · Cited by 311 · see citing works

Regulation of Protein Degradation by Proteasomes in Cancer

Jang, H. H. (2018) · Journal of Cancer Prevention · doi:10.15430/jcp.2018.23.4.153 · Cited by 101 · see citing works