期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 62, 期 21, 页码 9792-9805出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.9b01199
关键词
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资金
- Australian Research Council [DP180101804, DP140100174]
- University of Melbourne (Manchester-Melbourne Research Fund)
- UK Biotechnology and Biological Sciences Research Council (BBSRC) [BB/R009961/1]
- BBSRC [BB/M017702/1]
- BBSRC [BB/R009961/1, BB/M017702/1] Funding Source: UKRI
A series of analogues of cyclo(L-tyrosyl-L-tyrosine), the substrate of the Mycobacterium tuberculosis enzyme CYP121, have been synthesized and analyzed by UV-vis and electron paramagnetic resonance spectroscopy and by X-ray crystallography. The introduction of iodine substituents onto cyclo(L-tyrosyl-L-tyrosine) results in sub-mu M binding affinity for the CYP121 enzyme and a complete shift to the high-spin state of the heme Fe-III. The introduction of halogens that are able to interact with heme groups is thus a feasible approach to the development of next-generation, tight binding inhibitors of the CYP121 enzyme, in the search for novel antitubercular compounds.
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