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Year Number of Results
1950 1
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1972 3
1973 4
1974 2
1975 8
1976 4
1977 7
1978 7
1979 7
1980 11
1981 20
1982 23
1983 32
1984 36
1985 57
1986 61
1987 56
1988 69
1989 100
1990 74
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1992 97
1993 82
1994 95
1995 77
1996 106
1997 98
1998 100
1999 104
2000 103
2001 113
2002 98
2003 125
2004 125
2005 153
2006 182
2007 194
2008 194
2009 200
2010 226
2011 205
2012 221
2013 197
2014 184
2015 207
2016 174
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5,350 results

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Page 1
Targeted protein degradation: mechanisms, strategies and application.
Zhao L, Zhao J, Zhong K, Tong A, Jia D. Zhao L, et al. Signal Transduct Target Ther. 2022 Apr 4;7(1):113. doi: 10.1038/s41392-022-00966-4. Signal Transduct Target Ther. 2022. PMID: 35379777 Free PMC article. Review.
Traditional drug discovery mainly focuses on direct regulation of protein activity. The development and application of protein activity modulators, particularly inhibitors, has been the mainstream in drug development. In recent years, PROteolysis TArgeting Chimeras …
Traditional drug discovery mainly focuses on direct regulation of protein activity. The development and application of protein …
Molecular Glues: The Adhesive Connecting Targeted Protein Degradation to the Clinic.
Sasso JM, Tenchov R, Wang D, Johnson LS, Wang X, Zhou QA. Sasso JM, et al. Biochemistry. 2023 Feb 7;62(3):601-623. doi: 10.1021/acs.biochem.2c00245. Epub 2022 Jul 20. Biochemistry. 2023. PMID: 35856839 Free PMC article. Review.
Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin-proteasome pathway. It shows great potential for treating diseases such as cancer …
Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small molecules to recruit disease-causing p …
Molecular Glues for Targeted Protein Degradation: From Serendipity to Rational Discovery.
Dong G, Ding Y, He S, Sheng C. Dong G, et al. J Med Chem. 2021 Aug 12;64(15):10606-10620. doi: 10.1021/acs.jmedchem.1c00895. Epub 2021 Jul 28. J Med Chem. 2021. PMID: 34319094 Review.
Targeted protein degradation is a promising area in the discovery and development of innovative therapeutics. ...Classical molecular glue degraders have been identified serendipitously, but rational discovery and design strategies are emerging rapidly. ...
Targeted protein degradation is a promising area in the discovery and development of innovative therapeutics. ...Classical molecular …
Chasing molecular glue degraders: screening approaches.
Domostegui A, Nieto-Barrado L, Perez-Lopez C, Mayor-Ruiz C. Domostegui A, et al. Chem Soc Rev. 2022 Jul 4;51(13):5498-5517. doi: 10.1039/d2cs00197g. Chem Soc Rev. 2022. PMID: 35723413 Review.
Protein-protein interactions (PPIs) govern all biological processes. Some small molecules modulate PPIs through induced protein proximity. In particular, molecular glue degraders are monovalent compounds that orchestrate interactions between a target …
Protein-protein interactions (PPIs) govern all biological processes. Some small molecules modulate PPIs through induced pro …
The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K.
Słabicki M, Kozicka Z, Petzold G, Li YD, Manojkumar M, Bunker RD, Donovan KA, Sievers QL, Koeppel J, Suchyta D, Sperling AS, Fink EC, Gasser JA, Wang LR, Corsello SM, Sellar RS, Jan M, Gillingham D, Scholl C, Fröhling S, Golub TR, Fischer ES, Thomä NH, Ebert BL. Słabicki M, et al. Nature. 2020 Sep;585(7824):293-297. doi: 10.1038/s41586-020-2374-x. Epub 2020 Jun 3. Nature. 2020. PMID: 32494016 Free PMC article.
Molecular glue compounds induce protein-protein interactions that, in the context of a ubiquitin ligase, lead to protein degradation(1). Unlike traditional enzyme inhibitors, these molecular glue degraders act substoichiometrically to catalyse t …
Molecular glue compounds induce protein-protein interactions that, in the context of a ubiquitin ligase, lead to pro …
Catalytic Protein Inhibitors.
Kodadek T. Kodadek T. Angew Chem Int Ed Engl. 2024 Mar 11;63(11):e202316726. doi: 10.1002/anie.202316726. Epub 2024 Jan 12. Angew Chem Int Ed Engl. 2024. PMID: 38064411 Review.
Many of the highest priority targets in a wide range of disease states are difficult-to-drug proteins. The development of reversible small molecule inhibitors for the active sites of these proteins with sufficient affinity and residence time on-target is an enormous …
Many of the highest priority targets in a wide range of disease states are difficult-to-drug proteins. The development of reversible …
Clinical Translation of Targeted Protein Degraders.
Kong NR, Jones LH. Kong NR, et al. Clin Pharmacol Ther. 2023 Sep;114(3):558-568. doi: 10.1002/cpt.2985. Epub 2023 Jul 17. Clin Pharmacol Ther. 2023. PMID: 37399310 Review.
Targeted protein degradation (TPD) has emerged as a potentially transformational therapeutic modality with considerable promise. Molecular glue degraders remodel the surface of E3 ligases inducing interactions with neosubstrates resulting in their polyubiquitination …
Targeted protein degradation (TPD) has emerged as a potentially transformational therapeutic modality with considerable promise. Mole …
ATTEC: a potential new approach to target proteinopathies.
Li Z, Zhu C, Ding Y, Fei Y, Lu B. Li Z, et al. Autophagy. 2020 Jan;16(1):185-187. doi: 10.1080/15548627.2019.1688556. Epub 2019 Nov 7. Autophagy. 2020. PMID: 31690177 Free PMC article. Review.
Many diseases are caused by aberrant accumulation of certain proteins that are misfolded and cytotoxic, and lowering the level of these proteins provides promising treatment strategies for these diseases. We hypothesized that compounds that interact with both the di …
Many diseases are caused by aberrant accumulation of certain proteins that are misfolded and cytotoxic, and lowering the level of the …
Discovery of a molecular glue promoting CDK12-DDB1 interaction to trigger cyclin K degradation.
Lv L, Chen P, Cao L, Li Y, Zeng Z, Cui Y, Wu Q, Li J, Wang JH, Dong MQ, Qi X, Han T. Lv L, et al. Elife. 2020 Aug 17;9:e59994. doi: 10.7554/eLife.59994. Elife. 2020. PMID: 32804079 Free PMC article.
Molecular-glue degraders mediate interactions between target proteins and components of the ubiquitin-proteasome system to cause selective protein degradation. ...Structure-activity relationship analysis of HQ461 revealed the importance of a 5-methylthiazol-2 …
Molecular-glue degraders mediate interactions between target proteins and components of the ubiquitin-proteasome system to cau …
Atypical E3 ligase ZFP91 promotes small-molecule-induced E2F2 transcription factor degradation for cancer therapy.
Liu TT, Yang H, Zhuo FF, Yang Z, Zhao MM, Guo Q, Liu Y, Liu D, Zeng KW, Tu PF. Liu TT, et al. EBioMedicine. 2022 Dec;86:104353. doi: 10.1016/j.ebiom.2022.104353. Epub 2022 Nov 11. EBioMedicine. 2022. PMID: 36375317 Free PMC article.
Unlike canonical small-molecule therapeutics, molecular glues mediate new E3 ligase-protein interactions to induce selective proteasomal degradation, which represents an attractive option to overcome these limitations. ...FINDINGS: In this study, we identified a molecular …
Unlike canonical small-molecule therapeutics, molecular glues mediate new E3 ligase-protein interactions to induce selective proteaso …
5,350 results