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Literature DB >> 32184950

PROTAC Technology: Opportunities and Challenges.

Hongying Gao^1,2, Xiuyun Sun^1,2, Yu Rao¹.

Abstract

PROTACs-induced targeted protein degradation has emerged as a novel therapeutic strategy in drug development and attracted the favor of academic institutions, large pharmaceutical enterprises (e.g., AstraZeneca, Bayer, Novartis, Amgen, Pfizer, GlaxoSmithKline, Merck, and Boehringer Ingelheim, etc.), and biotechnology companies. PROTACs opened a new chapter for novel drug development. However, any new technology will face many new problems and challenges. Perspectives on the potential opportunities and challenges of PROTACs will contribute to the research and development of new protein degradation drugs and degrader tools.

Year: 2020 PMID： 32184950 PMCID： PMC7073876 DOI： 10.1021/acsmedchemlett.9b00597

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

21 in total

Review 1. Small-molecule stabilization of protein-protein interactions: an underestimated concept in drug discovery?

Authors: Philipp Thiel; Markus Kaiser; Christian Ottmann
Journal: Angew Chem Int Ed Engl Date: 2012-02-03 Impact factor: 15.336

Review 2. Reaching for high-hanging fruit in drug discovery at protein-protein interfaces.

Authors: James A Wells; Christopher L McClendon
Journal: Nature Date: 2007-12-13 Impact factor: 49.962

3. Acquired Resistance to BET-PROTACs (Proteolysis-Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 Ligase Complexes.

Authors: Lu Zhang; Bridget Riley-Gillis; Priyanka Vijay; Yu Shen
Journal: Mol Cancer Ther Date: 2019-05-07 Impact factor: 6.261

4. Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders.

Authors: Jiuling Yang; Yangbing Li; Angelo Aguilar; Zhaomin Liu; Chao-Yie Yang; Shaomeng Wang
Journal: J Med Chem Date: 2019-10-21 Impact factor: 7.446

5. 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

6. Catalytic in vivo protein knockdown by small-molecule PROTACs.

Authors: Daniel P Bondeson; Alina Mares; Ian E D Smith; Eunhwa Ko; Sebastien Campos; Afjal H Miah; Katie E Mulholland; Natasha Routly; Dennis L Buckley; Jeffrey L Gustafson; Nico Zinn; Paola Grandi; Satoko Shimamura; Giovanna Bergamini; Maria Faelth-Savitski; Marcus Bantscheff; Carly Cox; Deborah A Gordon; Ryan R Willard; John J Flanagan; Linda N Casillas; Bartholomew J Votta; Willem den Besten; Kristoffer Famm; Laurens Kruidenier; Paul S Carter; John D Harling; Ian Churcher; Craig M Crews
Journal: Nat Chem Biol Date: 2015-06-10 Impact factor: 15.040

7. Delineating the role of cooperativity in the design of potent PROTACs for BTK.

Authors: Adelajda Zorba; Chuong Nguyen; Yingrong Xu; Jeremy Starr; Kris Borzilleri; James Smith; Hongyao Zhu; Kathleen A Farley; WeiDong Ding; James Schiemer; Xidong Feng; Jeanne S Chang; Daniel P Uccello; Jennifer A Young; Carmen N Garcia-Irrizary; Lara Czabaniuk; Brandon Schuff; Robert Oliver; Justin Montgomery; Matthew M Hayward; Jotham Coe; Jinshan Chen; Mark Niosi; Suman Luthra; Jaymin C Shah; Ayman El-Kattan; Xiayang Qiu; Graham M West; Mark C Noe; Veerabahu Shanmugasundaram; Adam M Gilbert; Matthew F Brown; Matthew F Calabrese
Journal: Proc Natl Acad Sci U S A Date: 2018-07-16 Impact factor: 11.205

8. Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6.

Authors: William McCoull; Tony Cheung; Erica Anderson; Peter Barton; Jonathan Burgess; Kate Byth; Qing Cao; M Paola Castaldi; Huawei Chen; Elisabetta Chiarparin; Rodrigo J Carbajo; Erin Code; Suzanna Cowan; Paul R Davey; Andrew D Ferguson; Shaun Fillery; Nathan O Fuller; Ning Gao; David Hargreaves; Martin R Howard; Jun Hu; Aarti Kawatkar; Paul D Kemmitt; Elisabetta Leo; Daniel M Molina; Nichole O'Connell; Philip Petteruti; Timothy Rasmusson; Piotr Raubo; Philip B Rawlins; Piero Ricchiuto; Graeme R Robb; Monica Schenone; Michael J Waring; Michael Zinda; Stephen Fawell; David M Wilson
Journal: ACS Chem Biol Date: 2018-10-17 Impact factor: 5.100

9. Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach.

Authors: Zuni I Bassi; Martin C Fillmore; Afjal H Miah; Trevor D Chapman; Claire Maller; Emma J Roberts; Lauren C Davis; Darcy E Lewis; Nicholas W Galwey; Kirsty E Waddington; Valentino Parravicini; Abigail L Macmillan-Jones; Celine Gongora; Philip G Humphreys; Ian Churcher; Rab K Prinjha; David F Tough
Journal: ACS Chem Biol Date: 2018-09-18 Impact factor: 5.100

PROTAC Technology: Opportunities and Challenges.

Review 1. Small-molecule stabilization of protein-protein interactions: an underestimated concept in drug discovery?

Review 2. Reaching for high-hanging fruit in drug discovery at protein-protein interfaces.

3. Acquired Resistance to BET-PROTACs (Proteolysis-Targeting Chimeras) Caused by Genomic Alterations in Core Components of E3 Ligase Complexes.

4. Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders.

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

6. Catalytic in vivo protein knockdown by small-molecule PROTACs.

7. Delineating the role of cooperativity in the design of potent PROTACs for BTK.

8. Development of a Novel B-Cell Lymphoma 6 (BCL6) PROTAC To Provide Insight into Small Molecule Targeting of BCL6.

9. Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach.

Review 10. Molecular genetics and cellular events of K-Ras-driven tumorigenesis.

1. Ligand Design for Cereblon Based Immunomodulatory Therapy.

Review 2. The role of PI3'-lipid signalling in melanoma initiation, progression and maintenance.

Review 3. Targeted degradation of immune checkpoint proteins: emerging strategies for cancer immunotherapy.

4. A new genre of fluorescence recovery assay to evaluate polo-like kinase 1 ATP-competitive inhibitors.

5. Discovery of First-in-Class Protein Arginine Methyltransferase 5 (PRMT5) Degraders.

Review 6. PROTACs to address the challenges facing small molecule inhibitors.

7. Design, Synthesis, and Biological Evaluation of IRAK4-Targeting PROTACs.

Review 8. Protein arginine methyltransferases: promising targets for cancer therapy.

9. Homo-PROTAC mediated suicide of MDM2 to treat non-small cell lung cancer.

Review 10. Opportunities and Challenges of Small Molecule Induced Targeted Protein Degradation.