Overman RC - Search Results

1

A-loop interactions in Mer tyrosine kinase give rise to inhibitors with two-step mechanism and long residence time of binding.

Pflug A, Schimpl M, Nissink JWM, Overman RC, Rawlins PB, Truman C, Underwood E, Warwicker J, Winter-Holt J, McCoull W. Pflug A, et al. Among authors: overman rc. Biochem J. 2020 Nov 27;477(22):4443-4452. doi: 10.1042/BCJ20200735. Biochem J. 2020. PMID: 33119085 Free PMC article.

2

Generating Selective Leads for Mer Kinase Inhibitors-Example of a Comprehensive Lead-Generation Strategy.

Nissink JWM, Bazzaz S, Blackett C, Clark MA, Collingwood O, Disch JS, Gikunju D, Goldberg K, Guilinger JP, Hardaker E, Hennessy EJ, Jetson R, Keefe AD, McCoull W, McMurray L, Olszewski A, Overman R, Pflug A, Preston M, Rawlins PB, Rivers E, Schimpl M, Smith P, Truman C, Underwood E, Warwicker J, Winter-Holt J, Woodcock S, Zhang Y. Nissink JWM, et al. J Med Chem. 2021 Mar 25;64(6):3165-3184. doi: 10.1021/acs.jmedchem.0c01904. Epub 2021 Mar 8. J Med Chem. 2021. PMID: 33683117

3

The structure of human GCN2 reveals a parallel, back-to-back kinase dimer with a plastic DFG activation loop motif.

Maia de Oliveira T, Korboukh V, Caswell S, Winter Holt JJ, Lamb M, Hird AW, Overman R. Maia de Oliveira T, et al. Biochem J. 2020 Jan 17;477(1):275-284. doi: 10.1042/BCJ20190196. Biochem J. 2020. PMID: 31868900

4

Development of Specific, Irreversible Inhibitors for a Receptor Tyrosine Kinase EphB3.

Kung A, Chen YC, Schimpl M, Ni F, Zhu J, Turner M, Molina H, Overman R, Zhang C. Kung A, et al. J Am Chem Soc. 2016 Aug 24;138(33):10554-60. doi: 10.1021/jacs.6b05483. Epub 2016 Aug 11. J Am Chem Soc. 2016. PMID: 27478969 Free PMC article.

5

A Chemical-Genetic Approach to Generate Selective Covalent Inhibitors of Protein Kinases.

Kung A, Schimpl M, Ekanayake A, Chen YC, Overman R, Zhang C. Kung A, et al. ACS Chem Biol. 2017 Jun 16;12(6):1499-1503. doi: 10.1021/acschembio.6b01083. Epub 2017 May 8. ACS Chem Biol. 2017. PMID: 28459525 Free PMC article.

6

Biochemical and biophysical characterization of four EphB kinase domains reveals contrasting thermodynamic, kinetic and inhibition profiles.

Overman RC, Debreczeni JE, Truman CM, McAlister MS, Attwood TK. Overman RC, et al. Biosci Rep. 2013 Jun 5;33(3):e00040. doi: 10.1042/BSR20130028. Biosci Rep. 2013. PMID: 23627399 Free PMC article.

7

Completing the structural family portrait of the human EphB tyrosine kinase domains.

Overman RC, Debreczeni JE, Truman CM, McAlister MS, Attwood TK. Overman RC, et al. Protein Sci. 2014 May;23(5):627-38. doi: 10.1002/pro.2445. Epub 2014 Mar 11. Protein Sci. 2014. PMID: 24677421 Free PMC article.

8

Stability and solubility engineering of the EphB4 tyrosine kinase catalytic domain using a rationally designed synthetic library.

Overman RC, Green I, Truman CM, Read JA, Embrey KJ, McAlister MS, Attwood TK. Overman RC, et al. Protein Eng Des Sel. 2013 Oct;26(10):695-704. doi: 10.1093/protein/gzt032. Epub 2013 Jul 8. Protein Eng Des Sel. 2013. PMID: 23840071

9

Structural and binding characterization of the LacdiNAc-specific adhesin (LabA; HopD) exodomain from Helicobacter pylori.

Paraskevopoulou V, Schimpl M, Overman RC, Stolnik S, Chen Y, Nguyen L, Winkler GS, Gellert P, Klassen JS, Falcone FH. Paraskevopoulou V, et al. Among authors: overman rc. Curr Res Struct Biol. 2020 Dec 15;3:19-29. doi: 10.1016/j.crstbi.2020.12.004. eCollection 2021. Curr Res Struct Biol. 2020. PMID: 34235483 Free PMC article.

10

Discovery of N-(4-{[5-Fluoro-7-(2-methoxyethoxy)quinazolin-4-yl]amino}phenyl)-2-[4-(propan-2-yl)-1 H-1,2,3-triazol-1-yl]acetamide (AZD3229), a Potent Pan-KIT Mutant Inhibitor for the Treatment of Gastrointestinal Stromal Tumors.

Kettle JG, Anjum R, Barry E, Bhavsar D, Brown C, Boyd S, Campbell A, Goldberg K, Grondine M, Guichard S, Hardy CJ, Hunt T, Jones RDO, Li X, Moleva O, Ogg D, Overman RC, Packer MJ, Pearson S, Schimpl M, Shao W, Smith A, Smith JM, Stead D, Stokes S, Tucker M, Ye Y. Kettle JG, et al. Among authors: overman rc. J Med Chem. 2018 Oct 11;61(19):8797-8810. doi: 10.1021/acs.jmedchem.8b00938. Epub 2018 Sep 24. J Med Chem. 2018. PMID: 30204441

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