細菌ヒスチジンキナーゼに対する共有結合性阻害剤の開発
Patricia D Rodriguez1, Conrad A Fihn2, Manibarsha Goswami1
1Department of Chemistry, University of Minnesota, 207 Pleasant Street SE, Minneapolis, Minnesota, 55455, USA. carlsone@umn.edu.
Abstract:
Antivirulence therapies offer an alternative strategy against antimicrobial resistance. We synthesized 2-aminobenzothiazole sulfonyl fluoride analogs for covalent histidine kinase inhibition. In vitro and in cellulo assays also identified lead inhibitors for affinity-based probe development. However, alkyne incorporation reduced bioactivity, emphasizing the challenges of designing functional probes while preserving inhibitor potency.
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関連する概念動画
Enzyme Inhibition
Covalently Linked Protein Regulators
These groups modify specific amino acids in a protein....
