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Structural characterization of human Vaccinia-Related Kinases (VRK) bound to small-molecule inhibitors identifies different P-loop conformations.
Couñago RM, Allerston CK, Savitsky P, Azevedo H, Godoi PH, Wells CI, Mascarello A, de Souza Gama FH, Massirer KB, Zuercher WJ, Guimarães CRW, Gileadi O. Couñago RM, et al. Among authors: massirer kb. Sci Rep. 2017 Aug 8;7(1):7501. doi: 10.1038/s41598-017-07755-y. Sci Rep. 2017. PMID: 28790404 Free PMC article.
Development of Pyridine-based Inhibitors for the Human Vaccinia-related Kinases 1 and 2.
Serafim RAM, de Souza Gama FH, Dutra LA, Dos Reis CV, Vasconcelos SNS, da Silva Santiago A, Takarada JE, Di Pillo F, Azevedo H, Mascarello A, Elkins JM, Massirer KB, Gileadi O, Guimarães CRW, Couñago RM. Serafim RAM, et al. Among authors: massirer kb. ACS Med Chem Lett. 2019 Aug 19;10(9):1266-1271. doi: 10.1021/acsmedchemlett.9b00082. eCollection 2019 Sep 12. ACS Med Chem Lett. 2019. PMID: 31531195 Free PMC article.
Binding and structural analyses of potent inhibitors of the human Ca2+/calmodulin dependent protein kinase kinase 2 (CAMKK2) identified from a collection of commercially-available kinase inhibitors.
Profeta GS, Dos Reis CV, Santiago ADS, Godoi PHC, Fala AM, Wells CI, Sartori R, Salmazo APT, Ramos PZ, Massirer KB, Elkins JM, Drewry DH, Gileadi O, Couñago RM. Profeta GS, et al. Among authors: massirer kb. Sci Rep. 2019 Nov 11;9(1):16452. doi: 10.1038/s41598-019-52795-1. Sci Rep. 2019. PMID: 31712618 Free PMC article.
Discovery of a Potent Dual SLK/STK10 Inhibitor Based on a Maleimide Scaffold.
Serafim RAM, Sorrell FJ, Berger BT, Collins RJ, Vasconcelos SNS, Massirer KB, Knapp S, Bennett J, Fedorov O, Patel H, Zuercher WJ, Elkins JM. Serafim RAM, et al. Among authors: massirer kb. J Med Chem. 2021 Sep 23;64(18):13259-13278. doi: 10.1021/acs.jmedchem.0c01579. Epub 2021 Aug 31. J Med Chem. 2021. PMID: 34463505
Development of the First Covalent Monopolar Spindle Kinase 1 (MPS1/TTK) Inhibitor.
M Serafim RA, da Silva Santiago A, Schwalm MP, Hu Z, Dos Reis CV, Takarada JE, Mezzomo P, Massirer KB, Kudolo M, Gerstenecker S, Chaikuad A, Zender L, Knapp S, Laufer S, Couñago RM, Gehringer M. M Serafim RA, et al. Among authors: massirer kb. J Med Chem. 2022 Feb 24;65(4):3173-3192. doi: 10.1021/acs.jmedchem.1c01165. Epub 2022 Feb 15. J Med Chem. 2022. PMID: 35167750
43 results