Literature DB >> 31047748

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

Scott D Edmondson1, Bin Yang2, Charlene Fallan3.   

Abstract

Proteolysis targeting chimeras (PROTACs) are heterobifunctional compounds with molecular weights and other properties that lie outside the classic 'rule-of-five' space. Consequently, PROTACs have unique challenges associated with their development as potential therapeutic agents. This review summarizes and analyzes a representative set of recent PROTACs and highlights some of the potential future challenges facing this promising modality.
Copyright © 2019 Elsevier Ltd. All rights reserved.

Keywords:  Absorption; Beyond rule-of-five; Degradation; Oral bioavailability; PROTACs; Proteolysis targeting chimeras; bRo5

Year:  2019        PMID： 31047748     DOI： 10.1016/j.bmcl.2019.04.030

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  47 in total

Review 1.  Methods to identify and optimize small molecules interacting with RNA (SMIRNAs).

Authors:  Andrei Ursu; Simon Vézina-Dawod; Matthew D Disney
Journal:  Drug Discov Today       Date:  2019-07-26       Impact factor: 7.851

Review 2.  PROTACs: great opportunities for academia and industry.

Authors:  Xiuyun Sun; Hongying Gao; Yiqing Yang; Ming He; Yue Wu; Yugang Song; Yan Tong; Yu Rao
Journal:  Signal Transduct Target Ther       Date:  2019-12-24

3.  A kinetic proofreading model for bispecific protein degraders.

Authors:  Derek W Bartlett; Adam M Gilbert
Journal:  J Pharmacokinet Pharmacodyn       Date:  2020-10-22       Impact factor: 2.745

Review 4.  Proteolysis-targeting chimeras in drug development: A safety perspective.

Authors:  Kevin Moreau; Muireann Coen; Andrew X Zhang; Fiona Pachl; M Paola Castaldi; Goran Dahl; Helen Boyd; Clay Scott; Pete Newham
Journal:  Br J Pharmacol       Date:  2020-02-25       Impact factor: 8.739

5.  The Evolving Druggability and Developability Space: Chemically Modified New Modalities and Emerging Small Molecules.

Authors:  Wenzhan Yang; Prajakta Gadgil; Venkata R Krishnamurthy; Margaret Landis; Pankajini Mallick; Dipal Patel; Phenil J Patel; Darren L Reid; Manuel Sanchez-Felix
Journal:  AAPS J       Date:  2020-01-03       Impact factor: 4.009

6.  Evolution of Cereblon-Mediated Protein Degradation as a Therapeutic Modality.

Authors:  Philip P Chamberlain; Laura A D'Agostino; J Michael Ellis; Joshua D Hansen; Mary E Matyskiela; Joseph J McDonald; Jennifer R Riggs; Lawrence G Hamann
Journal:  ACS Med Chem Lett       Date:  2019-11-12       Impact factor: 4.345

7.  bioPROTACs as versatile modulators of intracellular therapeutic targets including proliferating cell nuclear antigen (PCNA).

Authors:  Shuhui Lim; Regina Khoo; Khong Ming Peh; Jinkai Teo; Shih Chieh Chang; Simon Ng; Greg L Beilhartz; Roman A Melnyk; Charles W Johannes; Christopher J Brown; David P Lane; Brian Henry; Anthony W Partridge
Journal:  Proc Natl Acad Sci U S A       Date:  2020-03-02       Impact factor: 11.205

Review 8.  Critical Assessment of Targeted Protein Degradation as a Research Tool and Pharmacological Modality.

Authors:  Milka Kostic; Lyn H Jones
Journal:  Trends Pharmacol Sci       Date:  2020-03-26       Impact factor: 14.819

Review 9.  Avoid the trap: Targeting PARP1 beyond human malignancy.

Authors:  Chiho Kim; Chuo Chen; Yonghao Yu
Journal:  Cell Chem Biol       Date:  2021-03-02       Impact factor: 8.116

Review 10.  Advancing targeted protein degradation for cancer therapy.

Authors:  Brandon Dale; Meng Cheng; Kwang-Su Park; H Ümit Kaniskan; Yue Xiong; Jian Jin
Journal:  Nat Rev Cancer       Date:  2021-06-15       Impact factor: 60.716
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