Literature DB >> 33429995

The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification.

Carrow I Wells1, Hassan Al-Ali2,3, David M Andrews4, Christopher R M Asquith1, Alison D Axtman1, Ivan Dikic5,6,7, Daniel Ebner8, Peter Ettmayer9, Christian Fischer10, Mathias Frederiksen11, Robert E Futrell1, Nathanael S Gray12,13, Stephanie B Hatch14, Stefan Knapp6,15,16, Ulrich Lücking17, Michael Michaelides18, Caitlin E Mills19, Susanne Müller6,15,16, Dafydd Owen20, Alfredo Picado1, Kumar S Saikatendu21, Martin Schröder6,15,16, Alexandra Stolz5,6,15, Mariana Tellechea5,6,15, Brandon J Turunen22, Santiago Vilar3, Jinhua Wang12,13, William J Zuercher1, Timothy M Willson1, David H Drewry1.   

Abstract

We describe the assembly and annotation of a chemogenomic set of protein kinase inhibitors as an open science resource for studying kinase biology. The set only includes inhibitors that show potent kinase inhibition and a narrow spectrum of activity when screened across a large panel of kinase biochemical assays. Currently, the set contains 187 inhibitors that cover 215 human kinases. The kinase chemogenomic set (KCGS), current Version 1.0, is the most highly annotated set of selective kinase inhibitors available to researchers for use in cell-based screens.

Entities:  

Keywords:  KCGS; chemogenomic set; drug discovery; druggable genome; kinase inhibitor; phenotypic screening; protein kinase; small molecules; understudied kinase

Year:  2021        PMID: 33429995     DOI: 10.3390/ijms22020566

Source DB:  PubMed          Journal:  Int J Mol Sci        ISSN: 1422-0067            Impact factor:   5.923


  10 in total

1.  Image-Based Annotation of Chemogenomic Libraries for Phenotypic Screening.

Authors:  Amelie Tjaden; Apirat Chaikuad; Eric Kowarz; Rolf Marschalek; Stefan Knapp; Martin Schröder; Susanne Müller
Journal:  Molecules       Date:  2022-02-21       Impact factor: 4.411

2.  Topographic mapping of the glioblastoma proteome reveals a triple-axis model of intra-tumoral heterogeneity.

Authors:  K H Brian Lam; Alberto J Leon; Weili Hui; Sandy Che-Eun Lee; Ihor Batruch; Kevin Faust; Almos Klekner; Gábor Hutóczki; Marianne Koritzinsky; Maxime Richer; Ugljesa Djuric; Phedias Diamandis
Journal:  Nat Commun       Date:  2022-01-10       Impact factor: 14.919

3.  Host kinase CSNK2 is a target for inhibition of pathogenic β-coronaviruses including SARS-CoV-2.

Authors:  Xuan Yang; Rebekah J Dickmander; Armin Bayati; Sharon A Taft-Benz; Jeffery L Smith; Carrow I Wells; Emily A Madden; Jason W Brown; Erik M Lenarcic; Boyd L Yount; Edcon Chang; Alison D Axtman; Ralph S Baric; Mark T Heise; Peter S McPherson; Nathaniel J Moorman; Timothy M Willson
Journal:  bioRxiv       Date:  2022-01-26

4.  Use of AD Informer Set compounds to explore validity of novel targets in Alzheimer's disease pathology.

Authors:  Frances M Potjewyd; Joel K Annor-Gyamfi; Jeffrey Aubé; Shaoyou Chu; Ivie L Conlon; Kevin J Frankowski; Shiva K R Guduru; Brian P Hardy; Megan D Hopkins; Chizuru Kinoshita; Dmitri B Kireev; Emily R Mason; Charles T Moerk; Felix Nwogbo; Kenneth H Pearce; Timothy I Richardson; David A Rogers; Disha M Soni; Michael Stashko; Xiaodong Wang; Carrow Wells; Timothy M Willson; Stephen V Frye; Jessica E Young; Alison D Axtman
Journal:  Alzheimers Dement (N Y)       Date:  2022-04-12

5.  AD Informer Set: Chemical tools to facilitate Alzheimer's disease drug discovery.

Authors:  Frances M Potjewyd; Joel K Annor-Gyamfi; Jeffrey Aubé; Shaoyou Chu; Ivie L Conlon; Kevin J Frankowski; Shiva K R Guduru; Brian P Hardy; Megan D Hopkins; Chizuru Kinoshita; Dmitri B Kireev; Emily R Mason; Charles T Moerk; Felix Nwogbo; Kenneth H Pearce; Timothy I Richardson; David A Rogers; Disha M Soni; Michael Stashko; Xiaodong Wang; Carrow Wells; Timothy M Willson; Stephen V Frye; Jessica E Young; Alison D Axtman
Journal:  Alzheimers Dement (N Y)       Date:  2022-04-20

6.  Temozolomide-induced guanine mutations create exploitable vulnerabilities of guanine-rich DNA and RNA regions in drug-resistant gliomas.

Authors:  Deanna M Tiek; Beril Erdogdu; Roham Razaghi; Lu Jin; Norah Sadowski; Carla Alamillo-Ferrer; J Robert Hogg; Bassem R Haddad; David H Drewry; Carrow I Wells; Julie E Pickett; Xiao Song; Anshika Goenka; Bo Hu; Samuel A Goldlust; William J Zuercher; Mihaela Pertea; Winston Timp; Shi-Yuan Cheng; Rebecca B Riggins
Journal:  Sci Adv       Date:  2022-06-22       Impact factor: 14.957

7.  Host Kinase CSNK2 is a Target for Inhibition of Pathogenic SARS-like β-Coronaviruses.

Authors:  Xuan Yang; Rebekah J Dickmander; Armin Bayati; Sharon A Taft-Benz; Jeffery L Smith; Carrow I Wells; Emily A Madden; Jason W Brown; Erik M Lenarcic; Boyd L Yount; Edcon Chang; Alison D Axtman; Ralph S Baric; Mark T Heise; Peter S McPherson; Nathaniel J Moorman; Timothy M Willson
Journal:  ACS Chem Biol       Date:  2022-06-19       Impact factor: 4.634

8.  Discovery of a Novel Template, 7-Substituted 7-Deaza-4'-Thioadenosine Derivatives as Multi-Kinase Inhibitors.

Authors:  Karishma K Mashelkar; Woong Sub Byun; Hyejin Ko; Kisu Sung; Sushil K Tripathi; Seungchan An; Yun A Yum; Jee Youn Kwon; Minjae Kim; Gibae Kim; Eun-Ji Kwon; Hyuk Woo Lee; Minsoo Noh; Sang Kook Lee; Lak Shin Jeong
Journal:  Pharmaceuticals (Basel)       Date:  2021-12-10

Review 9.  Targeting Protein Kinases and Epigenetic Control as Combinatorial Therapy Options for Advanced Prostate Cancer Treatment.

Authors:  Soghra Bagheri; Mahdie Rahban; Fatemeh Bostanian; Fatemeh Esmaeilzadeh; Arash Bagherabadi; Samaneh Zolghadri; Agata Stanek
Journal:  Pharmaceutics       Date:  2022-02-25       Impact factor: 6.321

10.  Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration.

Authors:  David H Drewry; Joel K Annor-Gyamfi; Carrow I Wells; Julie E Pickett; Verena Dederer; Franziska Preuss; Sebastian Mathea; Alison D Axtman
Journal:  J Med Chem       Date:  2021-08-01       Impact factor: 7.446

  10 in total

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