Literature DB >> 30783496

Evolution of Small Molecule Kinase Drugs.

Helen L Lightfoot1, Frederick W Goldberg2, Joerg Sedelmeier3.   

Abstract

The development of small molecule kinase drugs is a rapidly evolving field and represents one of the most important research areas within oncology. This innovation letter provides an overview and analysis of approved kinase drugs according to their WHO registration (INN) dates, primary biological targets, and selectivity and structural similarities, which are also depicted in an associated poster. It also discusses new trends in kinase drug discovery programs such as new kinase targets, novel mechanisms of action, and diverse indications.

Entities:  

Year:  2018        PMID: 30783496      PMCID: PMC6378673          DOI: 10.1021/acsmedchemlett.8b00445

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


  4 in total

1.  Identification of Potent Reverse Indazole Inhibitors for HPK1.

Authors:  Elsie C Yu; Joey L Methot; Xavier Fradera; Charles A Lesburg; Brian M Lacey; Phieng Siliphaivanh; Ping Liu; Dustin M Smith; Zangwei Xu; Jennifer A Piesvaux; Shuhei Kawamura; Haiyan Xu; J Richard Miller; Mark Bittinger; Alexander Pasternak
Journal:  ACS Med Chem Lett       Date:  2021-03-01       Impact factor: 4.345

2.  Discovery of Diaminopyrimidine Carboxamide HPK1 Inhibitors as Preclinical Immunotherapy Tool Compounds.

Authors:  Brandon A Vara; Samuel M Levi; Abdelghani Achab; David A Candito; Xavier Fradera; Charles A Lesburg; Shuhei Kawamura; Brian M Lacey; Jongwon Lim; Joey L Methot; Zangwei Xu; Haiyan Xu; Dustin M Smith; Jennifer A Piesvaux; J Richard Miller; Mark Bittinger; Sheila H Ranganath; David J Bennett; Erin F DiMauro; Alexander Pasternak
Journal:  ACS Med Chem Lett       Date:  2021-03-19       Impact factor: 4.345

3.  GCN2 kinase activation by ATP-competitive kinase inhibitors.

Authors:  Colin P Tang; Owen Clark; John R Ferrarone; Carl Campos; Alshad S Lalani; John D Chodera; Andrew M Intlekofer; Olivier Elemento; Ingo K Mellinghoff
Journal:  Nat Chem Biol       Date:  2021-12-23       Impact factor: 16.174

4.  Structural Basis for Targeting the Folded P-Loop Conformation of c-MET.

Authors:  Gavin W Collie; Iacovos N Michaelides; Kevin Embrey; Christopher J Stubbs; Ulf Börjesson; Ian L Dale; Arjan Snijder; Louise Barlind; Kun Song; Puneet Khurana; Christopher Phillips; R Ian Storer
Journal:  ACS Med Chem Lett       Date:  2020-12-08       Impact factor: 4.345

  4 in total

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