| 1 |
PROTAC targeted protein degraders: the past is prologue
Miklós Békés, David R. Langley, Craig M. Crews · Nature Reviews Drug Discovery
ReviewOpen access |
18 Jan 2022 |
3,294 |
| 2 |
Catalytic in vivo protein knockdown by small-molecule PROTACs
Daniel P. Bondeson et al. · Nature Chemical Biology
Open access |
10 Jun 2015 |
1,365 |
| 3 |
Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4
Jing Lü, Yimin Qian, Martha Altieri et al. · Chemistry & Biology
Open access |
Jun 2015 |
1,162 |
| 4 |
Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead
Daniel P. Bondeson, Blake E. Smith, George M. Burslem et al. · Cell chemical biology
Open access |
9 Nov 2017 |
938 |
| 5 |
PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer
Kanak Raina, Jing Lü, Yimin Qian et al. · Proceedings of the National Academy of Sciences
Open access |
6 Jun 2016 |
855 |
| 6 |
The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study
George M. Burslem, Blake E. Smith, Ashton C. Lai et al. · Cell chemical biology
Open access |
9 Nov 2017 |
699 |
| 7 |
Protein degraders enter the clinic — a new approach to cancer therapy
Deborah Chirnomas, Keith R. Hornberger, Craig M. Crews · Nature Reviews Clinical Oncology
ReviewOpen access |
13 Feb 2023 |
637 |
| 8 |
Targeted protein degradation by PROTACs
Taavi K. Neklesa, James D. Winkler, Craig M. Crews · Pharmacology & Therapeutics
|
14 Feb 2017 |
589 |
| 9 |
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
Blake E. Smith, Stephen L. Wang, Saul Jaime‐Figueroa et al. · Nature Communications
Open access |
4 Jan 2019 |
532 |
| 10 |
Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance
Jemilat Salami, Shanique B. Alabi, Ryan R. Willard et al. · Communications Biology
Open access |
27 Jul 2018 |
353 |
| 11 |
MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53
John F. Hines, Schan Lartigue, Hanqing Dong et al. · Cancer Research
Open access |
Nov 2018 |
348 |
| 12 |
Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1
Andrew P. A. Crew, Kanak Raina, Hanqing Dong et al. · Journal of Medicinal Chemistry
Open access |
10 Jul 2017 |
256 |
| 13 |
Oral Estrogen Receptor PROTAC Vepdegestrant (ARV-471) Is Highly Efficacious as Monotherapy and in Combination with CDK4/6 or PI3K/mTOR Pathway Inhibitors in Preclinical ER+ Breast Cancer Models
Sheryl M. Gough et al. · Clinical Cancer Research
Open access |
31 May 2024 |
191 |
| 14 |
Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells
Dyana T. Saenz et al. · Leukemia
Open access |
2 Jan 2017 |
190 |
| 15 |
BET protein proteolysis targeting chimera (PROTAC) exerts potent lethal activity against mantle cell lymphoma cells
Baohua Sun, Warren C. Fiskus, Yimin Qian et al. · Leukemia
Open access |
30 Jun 2017 |
182 |
| 16 |
Enhancing Antiproliferative Activity and Selectivity of a FLT-3 Inhibitor by Proteolysis Targeting Chimera Conversion
George M. Burslem, Jayoung Song, Xin Chen et al. · Journal of the American Chemical Society
|
14 Nov 2018 |
178 |
| 17 |
Physicochemical Property Determinants of Oral Absorption for PROTAC Protein Degraders
Keith R. Hornberger, Erika M. V. Araujo · Journal of Medicinal Chemistry
Open access |
6 Jun 2023 |
173 |
| 18 |
Vepdegestrant, a PROTAC Estrogen Receptor Degrader, in Advanced Breast Cancer
Mario Campone et al. · New England Journal of Medicine
|
31 May 2025 |
150 |
| 19 |
Selective PROTAC-mediated degradation of SMARCA2 is efficacious in SMARCA4 mutant cancers
Jennifer L. Cantley et al. · Nature Communications
Open access |
10 Nov 2022 |
138 |
| 20 |
Activity profiling and structures of inhibitor-bound SARS-CoV-2-PLpro protease provides a framework for anti-COVID-19 drug design
Wioletta Rut, Zongyang Lv, Mikolaj Zmudzinski et al. · bioRxiv (Cold Spring Harbor Laboratory)
PreprintOpen access |
29 Apr 2020 |
123 |
| 21 |
Targeted protein knockdown using small molecule degraders
Kanak Raina, Craig M. Crews · Current Opinion in Chemical Biology
ReviewOpen access |
10 Jun 2017 |
112 |
| 22 |
Molecular Characterization of a Neutralizing Domain of the Japanese Encephalitis Virus Structural Glycoprotein
Peter W. Mason, Joel M. Dalrymple, Mary Kay Gentry et al. · Journal of General Virology
|
Aug 1989 |
109 |
| 23 |
THE ISOLATION OF A BLUETONGUE VIRUS FROM CULICOIDES COLLECTED IN THE NORTHERN TERRITORY OF AUSTRALIA
T. D. St. George, H. A. Standfast, D. H. Cybinski et al. · Australian Veterinary Journal
|
Mar 1978 |
105 |
| 24 |
VERITAC-2: a Phase III study of vepdegestrant, a PROTAC ER degrader, versus fulvestrant in ER+/HER2- advanced breast cancer
Erika Paige Hamilton, Cynthia X. Ma, Michelino De Laurentiis et al. · Future Oncology
Open access |
29 Jul 2024 |
104 |
| 25 |
RUNX1-targeted therapy for AML expressing somatic or germline mutation in RUNX1
Christopher Peter Mill, Warren C. Fiskus, Courtney Denton Dinardo et al. · Blood
Open access |
25 Apr 2019 |
100 |
| 26 |
Targeting Nuclear Receptors with PROTAC degraders
John J. Flanagan, Taavi K. Neklesa · Molecular and Cellular Endocrinology
|
21 May 2019 |
96 |
| 27 |
Safety and efficacy of eculizumab for the prevention of antibody-mediated rejection after deceased-donor kidney transplantation in patients with preformed donor-specific antibodies
Denis Glotz, Graeme R. Russ, Lionel P. E. Rostaing et al. · American Journal of Transplantation
Open access |
23 Apr 2019 |
93 |
| 28 |
Preclinical Evaluation of Bavdegalutamide (ARV-110), a Novel PROteolysis TArgeting Chimera Androgen Receptor Degrader
Lawrence B. Snyder, Taavi K. Neklesa, Ryan R. Willard et al. · Molecular Cancer Therapeutics
Open access |
13 Dec 2024 |
87 |
| 29 |
A first-in-human phase I study to evaluate the MEK1/2 inhibitor, cobimetinib, administered daily in patients with advanced solid tumors
Lee S. Rosen, Patricia Mucci LoRusso, Wen Wee Ma et al. · Investigational New Drugs
Open access |
16 Jul 2016 |
85 |
| 30 |
A MYC and RAS co-activation signature in localized prostate cancer drives bone metastasis and castration resistance
Juan Martín Arriaga et al. · Nature Cancer
Open access |
19 Oct 2020 |
83 |
| 31 |
Protein targeting chimeric molecules specific for bromodomain and extra-terminal motif family proteins are active against pre-clinical models of multiple myeloma
Xiaohui Zhang et al. · Leukemia
Open access |
26 Mar 2018 |
83 |
| 32 |
Current directions in tau research: Highlights from Tau 2020
Claire E. Sexton et al. · Alzheimer s & Dementia
Open access |
28 Sep 2021 |
79 |
| 33 |
BETP degradation simultaneously targets acute myelogenous leukemic stem cells and the microenvironment
Sujan Piya, Hong Hua Mu, Seemana Bhattacharya et al. · Journal of Clinical Investigation
Open access |
21 Feb 2019 |
73 |
| 34 |
Proteolysis-Targeting Chimeras: Harnessing the Ubiquitin-Proteasome System to Induce Degradation of Specific Target Proteins
Kevin G. Coleman, Craig M. Crews · Annual Review of Cancer Biology
Review |
30 Oct 2017 |
68 |
| 35 |
Oral Migalastat HCl Leads to Greater Systemic Exposure and Tissue Levels of Active α-Galactosidase A in Fabry Patients when Co-Administered with Infused Agalsidase
David G. Warnock, Daniel Georges Bichet, Myrl D. Holida et al. · PLoS ONE
Open access |
7 Aug 2015 |
63 |
| 36 |
Co-opting the E3 ligase KLHDC2 for targeted protein degradation by small molecules
Christopher M. Hickey, Katherine Marie Digianantonio, Kurt Zimmermann et al. · Nature Structural & Molecular Biology
|
4 Jan 2024 |
62 |
| 37 |
Efficient Synthesis of Immunomodulatory Drug Analogues Enables Exploration of Structure–Degradation Relationships
George M. Burslem, Philipp Ottis, Saul Jaime‐Figueroa et al. · ChemMedChem
Open access |
5 Jun 2018 |
58 |
| 38 |
A highly accurate metadynamics-based Dissociation Free Energy method to calculate protein–protein and protein–ligand binding potencies
Jing Wang, Alexey V. Ishchenko, Wei Zhang et al. · Scientific Reports
Open access |
7 Feb 2022 |
54 |
| 39 |
Duvoglustat HCl Increases Systemic and Tissue Exposure of Active Acid α-Glucosidase in Pompe Patients Co-administered with Alglucosidase α
Priya Sunil Kishnani et al. · Molecular Therapy
Open access |
22 Mar 2017 |
46 |
| 40 |
Targeting nuclear β-catenin as therapy for post-myeloproliferative neoplasm secondary AML
Dyana T. Saenz et al. · Leukemia
Open access |
21 Dec 2018 |
42 |
| 41 |
Arbovirus infections in Sarawak: The isolation of Kunjin virus from mosquitoes of theCulex pseudovishnuigroup
E. T. W. Bowen, David I. H. Simpson, G. S. Platt et al. · Annals of Tropical Medicine and Parasitology
|
Sep 1970 |
41 |
| 42 |
New therapies on the horizon: Targeted protein degradation in neuroscience
James A Gregory, Christopher M. Hickey, Juan D. Chavez et al. · Cell chemical biology
Open access |
Sep 2024 |
38 |
| 43 |
SEROLOGICAL RELATION BETWEEN RIFT VALLEY FEVER VIRUS AND VIRUSES OF PHLEBOTOMUS FEVER SEROGROUP
RobertE. Shope, ClarenceJ. Peters, J.S. Walker · The Lancet
|
Apr 1980 |
35 |
| 44 |
PROTACs Targeting BRM (SMARCA2) Afford Selective In Vivo Degradation over BRG1 (SMARCA4) and Are Active in BRG1 Mutant Xenograft Tumor Models
Michael Y. Berlin et al. · Journal of Medicinal Chemistry
Open access |
5 Jan 2024 |
34 |
| 45 |
Integration of Affinity Selection–Mass Spectrometry and Functional Cell-Based Assays to Rapidly Triage Druggable Target Space within the NF-κB Pathway
Victoria D. Kutilek et al. · SLAS DISCOVERY
Open access |
11 Mar 2016 |
33 |
| 46 |
Reversion analysis reveals the in vivo immunogenicity of a poorly MHC I-binding cancer neoepitope
Hakimeh Ebrahimi-Nik, Marmar R. Moussa, Ryan P. Englander et al. · Nature Communications
Open access |
5 Nov 2021 |
32 |
| 47 |
Highly Enantioselective Rhodium-Catalyzed Cross-Addition of Silylacetylenes to Cyclohexadienone-Tethered Internal Alkynes
Chang-Lin Duan, Yun‐Xuan Tan, Junli Zhang et al. · Organic Letters
|
Mar 2019 |
32 |
| 48 |
Immunopathologic Aspects of Infection with Lagos Bat Virus of the Rabies Serogroup
Gregory H. Tignor, Robert E. Shope, Richard K. Gershon et al. · The Journal of Immunology
|
1974 |
30 |
| 49 |
MONOCLONAL ANTIBODIES TO IDENTIFY ZINGA VIRUS AS RIFT VALLEY FEVER VIRUS
James M. Meegan, J.P. Digoutte, Clarence J. Peters et al. · The Lancet
|
Mar 1983 |
30 |
| 50 |
Development of Liposome Systems for Enhancing the PK Properties of Bivalent PROTACs
Ponien Kou, Elizabeth S. Levy, An D. Nguyen et al. · Pharmaceutics
Open access |
8 Aug 2023 |
25 |