Rafael M. Couñago

Rafael M. Couñago

SGC UNC

Couñago

Biography

Rafael M. Couñago, PhD, is a Principal Investigator at the Structural Genomics Consortium Chemical Biology Center at the University of North Carolina (SGC-UNC), Chapel Hill. Rafael´s research group at SGC-UNC uses protein biochemistry, structural biology and cell-based assays to illuminate protein function and explore new therapeutic strategies for human diseases. Current research at SGC-UNC is focused on enabling the discovery of new antiviral compounds and realizing SGC´s vision for Target 2035, an open science initiative that aims to create chemical and biological tools for every protein in the human genome with the goal of informing drug discovery (https://www.target2035.net/). Rafael joined SGC-UNC after working as a Principal Investigator at the Center of Medicinal Chemistry at the University of Campinas (UNICAMP), São Paulo, Brazil. Prior to that, Rafael served as Team Leader and CSO at SGC-UNICAMP, and was a post-doctoral researcher at the laboratories of Bostjan Kobe at the University of Queensland, Australia; Kurt Krause at Otago University, New Zealand, and Youssif Shamoo at Rice University, USA. Rafael has a strong track record in recombinant protein production, biochemical and cellular assay development, and structure determination, and has participated in a number of early-stage drug discovery projects in collaboration with both academic and industrial partners

2024

A Covalent Chemical Probe for Chikungunya nsP2 Cysteine Protease with Antialphaviral Activity and Proteome-wide Selectivity.

Ghoshal A, Tse EG, Hossain MA, Asressu KH, Merten EM, Sears JD, Howell S, Perveen S, Burdick J, Morales NL, Martinez SA, Law I, Davenport BJ, Morrison TE, Streblow ZJ, Streblow DN, Mordant AL, Webb TS, Cabrera A, Herring LE, Arrowsmith CH, Pearce KH, Moorman NJ, Heise MT, Couñago RM, Brown PJ, Willson TM

Res Sq. 2024-11-28 . .doi: 10.21203/rs.3.rs-5363451/v1

PMID: 39606462

Identification of a cell-active chikungunya virus nsP2 protease inhibitor using a covalent fragment-based screening approach.

Merten EM, Sears JD, Leisner TM, Hardy PB, Ghoshal A, Hossain MA, Asressu KH, Brown PJ, Tse EG, Stashko MA, Li K, Norris-Drouin JL, Herring LE, Mordant AL, Webb TS, Mills CA, Barker NK, Streblow ZJ, Perveen S, Arrowsmith CH, Couñago RM, Arnold JJ, Cameron CE, Streblow DN, Moorman NJ, Heise MT, Willson TM, Popov KI, Pearce KH

Proc Natl Acad Sci U S A. 2024-10-10 . 121(42):e2409166121 .doi: 10.1073/pnas.2409166121

PMID: 39388272

Strategic Fluorination to Achieve a Potent, Selective, Metabolically Stable, and Orally Bioavailable Inhibitor of CSNK2.

Ong HW, Yang X, Smith JL, Taft-Benz S, Howell S, Dickmander RJ, Havener TM, Sanders MK, Brown JW, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM

Molecules. 2024-9-14 . 29(17): .doi: 10.3390/molecules29174158

PMID: 39275006

More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication.

Ong HW, Yang X, Smith JL, Dickmander RJ, Brown JW, Havener TM, Taft-Benz S, Howell S, Sanders MK, Capener JL, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM

J Med Chem. 2024-7-3 . .doi: 10.1021/acs.jmedchem.4c00962

PMID: 38959455

Novel Dihydropteridinone Derivatives As Potent Inhibitors of the Understudied Human Kinases Vaccinia-Related Kinase 1 and Casein Kinase 1δ/ε.

de Souza Gama FH, Dutra LA, Hawgood M, Dos Reis CV, Serafim RAM, Ferreira MA, Teodoro BVM, Takarada JE, Santiago AS, Balourdas DI, Nilsson AS, Urien B, Almeida VM, Gileadi C, Ramos PZ, Salmazo A, Vasconcelos SNS, Cunha MR, Mueller S, Knapp S, Massirer KB, Elkins JM, Gileadi O, Mascarello A, Lemmens BBLG, Guimarães CRW, Azevedo H, Couñago RM

J Med Chem. 2024-5-23 . .doi: 10.1021/acs.jmedchem.3c02250

PMID: 38780468

2023

SGC-CAMKK2-1: A Chemical Probe for CAMKK2.

Wells C, Liang Y, Pulliam TL, Lin C, Awad D, Eduful B, O'Byrne S, Hossain MA, Catta-Preta CMC, Ramos PZ, Gileadi O, Gileadi C, Couñago RM, Stork B, Langendorf CG, Nay K, Oakhill JS, Mukherjee D, Racioppi L, Means AR, York B, McDonnell DP, Scott JW, Frigo DE, Drewry DH

Cells. 2023-1-11 . 12(2): .doi: 10.3390/cells12020287

PMID: 36672221

2022

An open source plant kinase chemogenomics set.

Ercoli MF, Ramos PZ, Jain R, Pilotte J, Dong OX, Thompson T, Wells CI, Elkins JM, Edwards AM, Couñago RM, Drewry DH, Ronald PC

Plant Direct. 2022-12-1 . 6(11):e460 .doi: 10.1002/pld3.460

PMID: 36447653

A Target Engagement Assay to Assess Uptake, Potency, and Retention of Antibiotics in Living Bacteria.

Fanti RC, Vasconcelos SNS, Catta-Preta CMC, Sullivan JR, Riboldi GP, Dos Reis CV, Ramos PZ, Edwards AM, Behr MA, Couñago RM

ACS Infect Dis. 2022-7-11 . .doi: 10.1021/acsinfecdis.2c00073

PMID: 35815896

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

J Med Chem. 2022-2-15 . .doi: 10.1021/acs.jmedchem.1c01165

PMID: 35167750

Development of dihydropyrrolopyridinone-based PKN2/PRK2 chemical tools to enable drug discovery.

Scott F, Fala AM, Takarada JE, Ficu MP, Pennicott LE, Reuillon TD, Couñago RM, Massirer KB, Elkins JM, Ward SE

Bioorg Med Chem Lett. 2022-1-29 . 60:128588 .doi: 10.1016/j.bmcl.2022.128588

PMID: 35104640