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Page 1
Discovery of novel benzothiophene derivatives as potent and narrow spectrum inhibitors of DYRK1A and DYRK1B.
Segretti ND, Takarada JE, Ferreira MA Jr, da Silva Santiago A, Teodoro BVM, Damião MCFCB, Godoi PH, Cunha MR, Fala AM, Ramos PZ, Ishikawa EE, Mascarello A, Serafim RAM, Azevedo H, Guimarães CRW, Couñago RM. Segretti ND, et al. Among authors: guimaraes crw. Bioorg Med Chem Lett. 2022 Jul 15;68:128764. doi: 10.1016/j.bmcl.2022.128764. Epub 2022 May 2. Bioorg Med Chem Lett. 2022. PMID: 35504513
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: guimaraes crw. 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.
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: guimaraes crw. Sci Rep. 2017 Aug 8;7(1):7501. doi: 10.1038/s41598-017-07755-y. Sci Rep. 2017. PMID: 28790404 Free PMC article.
Identification of novel series of pyrazole and indole-urea based DFG-out PYK2 inhibitors.
Bhattacharya SK, Aspnes GE, Bagley SW, Boehm M, Brosius AD, Buckbinder L, Chang JS, Dibrino J, Eng H, Frederick KS, Griffith DA, Griffor MC, Guimarães CR, Guzman-Perez A, Han S, Kalgutkar AS, Klug-McLeod J, Garcia-Irizarry C, Li J, Lippa B, Price DA, Southers JA, Walker DP, Wei L, Xiao J, Zawistoski MP, Zhao X. Bhattacharya SK, et al. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7523-9. doi: 10.1016/j.bmcl.2012.10.039. Epub 2012 Oct 16. Bioorg Med Chem Lett. 2012. PMID: 23153798
2-Aminopyridine-Based Mitogen-Activated Protein Kinase Kinase Kinase Kinase 4 (MAP4K4) Inhibitors: Assessment of Mechanism-Based Safety.
Dow RL, Ammirati M, Bagley SW, Bhattacharya SK, Buckbinder L, Cortes C, El-Kattan AF, Ford K, Freeman GB, Guimarães CRW, Liu S, Niosi M, Skoura A, Tess D. Dow RL, et al. Among authors: guimaraes crw. J Med Chem. 2018 Apr 12;61(7):3114-3125. doi: 10.1021/acs.jmedchem.8b00152. Epub 2018 Apr 3. J Med Chem. 2018. PMID: 29570292
Activation of the G-protein-coupled receptor 119: a conformation-based hypothesis for understanding agonist response.
McClure KF, Darout E, Guimarães CR, DeNinno MP, Mascitti V, Munchhof MJ, Robinson RP, Kohrt J, Harris AR, Moore DE, Li B, Samp L, Lefker BA, Futatsugi K, Kung D, Bonin PD, Cornelius P, Wang R, Salter E, Hornby S, Kalgutkar AS, Chen Y. McClure KF, et al. J Med Chem. 2011 Mar 24;54(6):1948-52. doi: 10.1021/jm200003p. Epub 2011 Mar 1. J Med Chem. 2011. PMID: 21361292
From partial to full agonism: identification of a novel 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole as a full agonist of the human GPR119 receptor.
Futatsugi K, Mascitti V, Guimarães CR, Morishita N, Cai C, DeNinno MP, Gao H, Hamilton MD, Hank R, Harris AR, Kung DW, Lavergne SY, Lefker BA, Lopaze MG, McClure KF, Munchhof MJ, Preville C, Robinson RP, Wright SW, Bonin PD, Cornelius P, Chen Y, Kalgutkar AS. Futatsugi K, et al. Bioorg Med Chem Lett. 2013 Jan 1;23(1):194-7. doi: 10.1016/j.bmcl.2012.10.119. Epub 2012 Nov 5. Bioorg Med Chem Lett. 2013. PMID: 23177788
Design and evaluation of a 2-(2,3,6-trifluorophenyl)acetamide derivative as an agonist of the GPR119 receptor.
Mascitti V, Stevens BD, Choi C, McClure KF, Guimarães CR, Farley KA, Munchhof MJ, Robinson RP, Futatsugi K, Lavergne SY, Lefker BA, Cornelius P, Bonin PD, Kalgutkar AS, Sharma R, Chen Y. Mascitti V, et al. Bioorg Med Chem Lett. 2011 Mar 1;21(5):1306-9. doi: 10.1016/j.bmcl.2011.01.088. Epub 2011 Jan 25. Bioorg Med Chem Lett. 2011. PMID: 21310611
44 results