Literature DB >> 29174540

Small-Molecule Kinase Downregulators.

Lyn H Jones1.   

Abstract

New opportunities to advance small-molecule kinase ligands that downregulate their cognate target binding proteins are discussed. Rationally designed heterobifunctional kinase degraders are compared with ATP site ligands that were serendipitously found to cause kinase downregulation. These approaches could be particularly useful in the treatment of cancers since many kinases are known to remodel pro-oncogenic protein-protein interactions, which could be destroyed by small-molecule-mediated kinase depletion.
Copyright © 2017 Elsevier Ltd. All rights reserved.

Entities:  

Keywords:  PROTAC; chemical probe; downregulation; kinase; non-canonical signaling; target degradation; transcriptional modulation

Mesh：

Substances：

Year:  2017        PMID： 29174540     DOI： 10.1016/j.chembiol.2017.10.011

Source DB:  PubMed          Journal:  Cell Chem Biol        ISSN： 2451-9448            Impact factor:   8.116


  12 in total

Review 1.  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

2.  DNA Barcoding a Complete Matrix of Stereoisomeric Small Molecules.

Authors:  Christopher J Gerry; Mathias J Wawer; Paul A Clemons; Stuart L Schreiber
Journal:  J Am Chem Soc       Date:  2019-06-25       Impact factor: 15.419

Review 3.  Emerging modes-of-action in drug discovery.

Authors:  Eric Valeur; Frank Narjes; Christian Ottmann; Alleyn T Plowright
Journal:  Medchemcomm       Date:  2019-06-25       Impact factor: 3.597

4.  An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells.

Authors:  Ekaterina V Vinogradova; Xiaoyu Zhang; David Remillard; Daniel C Lazar; Radu M Suciu; Yujia Wang; Giulia Bianco; Yu Yamashita; Vincent M Crowley; Michael A Schafroth; Minoru Yokoyama; David B Konrad; Kenneth M Lum; Gabriel M Simon; Esther K Kemper; Michael R Lazear; Sifei Yin; Megan M Blewett; Melissa M Dix; Nhan Nguyen; Maxim N Shokhirev; Emily N Chin; Luke L Lairson; Bruno Melillo; Stuart L Schreiber; Stefano Forli; John R Teijaro; Benjamin F Cravatt
Journal:  Cell       Date:  2020-07-29       Impact factor: 41.582

Review 5.  Unifying principles of bifunctional, proximity-inducing small molecules.

Authors:  Christopher J Gerry; Stuart L Schreiber
Journal:  Nat Chem Biol       Date:  2020-03-20       Impact factor: 15.040

6.  Covalent inhibitors of EGFR family protein kinases induce degradation of human Tribbles 2 (TRIB2) pseudokinase in cancer cells.

Authors:  Daniel M Foulkes; Dominic P Byrne; Wayland Yeung; Safal Shrestha; Fiona P Bailey; Samantha Ferries; Claire E Eyers; Karen Keeshan; Carrow Wells; David H Drewry; William J Zuercher; Natarajan Kannan; Patrick A Eyers
Journal:  Sci Signal       Date:  2018-09-25       Impact factor: 8.192

7.  Salt-inducible kinase inhibition suppresses acute myeloid leukemia progression in vivo.

Authors:  Yusuke Tarumoto; Shan Lin; Jinhua Wang; Joseph P Milazzo; Yali Xu; Bin Lu; Zhaolin Yang; Yiliang Wei; Sofya Polyanskaya; Mark Wunderlich; Nathanael S Gray; Kimberly Stegmaier; Christopher R Vakoc
Journal:  Blood       Date:  2020-01-02       Impact factor: 25.476

8.  The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K.

Authors:  Mikołaj Słabicki; Zuzanna Kozicka; Georg Petzold; Yen-Der Li; Manisha Manojkumar; Richard D Bunker; Katherine A Donovan; Quinlan L Sievers; Jonas Koeppel; Dakota Suchyta; Adam S Sperling; Emma C Fink; Jessica A Gasser; Li R Wang; Steven M Corsello; Rob S Sellar; Max Jan; Dennis Gillingham; Claudia Scholl; Stefan Fröhling; Todd R Golub; Eric S Fischer; Nicolas H Thomä; Benjamin L Ebert
Journal:  Nature       Date:  2020-06-03       Impact factor: 49.962

Review 9.  Bivalent Ligands for Protein Degradation in Drug Discovery.

Authors:  Marcel Scheepstra; Koen F W Hekking; Luc van Hijfte; Rutger H A Folmer
Journal:  Comput Struct Biotechnol J       Date:  2019-01-25       Impact factor: 7.271

Review 10.  The PROTAC technology in drug development.

Authors:  Yutian Zou; Danhui Ma; Yinyin Wang
Journal:  Cell Biochem Funct       Date:  2019-01-02       Impact factor: 3.685
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