Thiolactomycin-based β-Ketoacyl-AcpM Synthase A (KasA) Inhibitors: FRAGMENT-BASED INHIBITOR DISCOVERY USING TRANSIENT ONE-DIMENSIONAL NUCLEAR OVERHAUSER EFFECT NMR SPECTROSCOPY

Thiolactomycin (TLM) is a natural product inhibitor of KasA, the β-ketoacyl synthase A from Mycobacterium tuberculosis. To improve the affinity of TLM for KasA, a series of TLM analogs have been synthesized based on interligand NOEs between TLM and a pantetheine analog when both are bound simultaneo...

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Detalhes bibliográficos
Main Authors: Kapilashrami, Kanishk, Bommineni, Gopal R., Machutta, Carl A., Kim, Pilho, Lai, Cheng-Tsung, Simmerling, Carlos, Picart, Francis, Tonge, Peter J.
Formato: Artigo
Idioma:Inglês
Publicado em: American Society for Biochemistry and Molecular Biology 2013
Assuntos:
Enzymology
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC3585043/
https://ncbi.nlm.nih.gov/pubmed/23306195
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1074/jbc.M112.414516
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