Towards selective mycobacterial ClpP1P2 inhibitors with reduced activity against the human proteasome

• Main Authors: Moreira, W, Santhanakrishnan, S, Ngan, G.J.Y, Low, C.B, Sangthongpitag, K, Poulsen, A, Dymock, B.W, Dick, T
• Other Authors: MICROBIOLOGY AND IMMUNOLOGY
• Format: Article
• Published: American Society for Microbiology 2020
• Subjects: 3 phenyl 1 [[2 (pyrazine 2 carboxamido) 3 (pyridin 2 yl)propanimido]propyl]boronic acid; boronic acid derivative; bortezomib; cytochrome P450; proteasome inhibitor; proteinase inhibitor; unclassified drug; antiinfective agent; bacterial protein; ClpP2 protein, bacteria; endopeptidase Clp; serine proteinase; animal experiment; animal model; antibacterial activity; Article; bacterial growth; bactericidal activity; controlled study; drug solubility; enzyme inhibition; growth inhibition; human; human cell; mouse; Mycobacterium tuberculosis; nonhuman; plasma protein binding; priority journal; animal; antagonists and inhibitors; drug design; drug effects; genetics; lung tuberculosis; microbial sensitivity test; microbiology; molecular model; Mycobacterium smegmatis; Animals; Anti-Bacterial Agents; Bacterial Proteins; Bortezomib; Drug Design; Endopeptidase Clp; Mice; Microbial Sensitivity Tests; Models, Molecular; Proteasome Inhibitors; Serine Endopeptidases; Tuberculosis, Pulmonary
• Online Access: https://scholarbank.nus.edu.sg/handle/10635/175227
• Institution: National University of Singapore

10.1128/AAC.02307-16