Related ArticlesPotent inhibitors of Mycobacterium tuberculosis growth identified by using in-cell NMR-based screening.
ACS Chem Biol. 2018 Jan 23;:
Authors: DeMott CM, Girardin R, Cobbert J, Reverdatto S, Burz DS, McDonough K, Shekhtman A
Abstract
In-cell NMR spectroscopy was used to screen for drugs that disrupt the interaction between prokaryotic ubiquitin like protein, Pup, and mycobacterial proteasome ATPase, Mpa. This interaction is critical for Mycobacterium tuberculosis resistance against nitric oxide (NO) stress; interruption of this process was proposed as a mechanism to control latent infection. Three compounds isolated from the NCI Diversity set III library rescued the physiological proteasome substrate from degradation suggesting that the proteasome degradation pathway was selectively targeted. Two of the compounds bind to Mpa with submicromolar to nanomolar affinity, and all three exhibit potency towards mycobacteria comparable to antibiotics currently available on the market, inhibiting growth in the low micromolar range.
PMID: 29359908 [PubMed - as supplied by publisher]
[NMR paper] Solution NMR Studies of Mycobacterium tuberculosis Proteins for Antibiotic Target Discovery.
Solution NMR Studies of Mycobacterium tuberculosis Proteins for Antibiotic Target Discovery.
Related Articles Solution NMR Studies of Mycobacterium tuberculosis Proteins for Antibiotic Target Discovery.
Molecules. 2017 Aug 31;22(9):
Authors: Kim DH, Kang SM, Lee BJ
Abstract
Tuberculosis is an infectious disease caused by Mycobacteriumtuberculosis, which triggers severe pulmonary diseases. Recently, multidrug/extensively drug-resistant tuberculosis strains have emerged and continue to threaten global health. Because of the...
[NMR paper] Automated NMR Fragment Based Screening Identified a Novel Interface Blocker to the LARG/RhoA Complex.
Automated NMR Fragment Based Screening Identified a Novel Interface Blocker to the LARG/RhoA Complex.
Related Articles Automated NMR Fragment Based Screening Identified a Novel Interface Blocker to the LARG/RhoA Complex.
PLoS One. 2014;9(2):e88098
Authors: Gao J, Ma R, Wang W, Wang N, Sasaki R, Snyderman D, Wu J, Ruan K
Abstract
The small GTPase cycles between the inactive GDP form and the activated GTP form, catalyzed by the upstream guanine exchange factors. The modulation of such process by small molecules has been proven to be a...
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[NMR paper] NMR assignment of protein Rv1980c from Mycobacterium tuberculosis.
NMR assignment of protein Rv1980c from Mycobacterium tuberculosis.
Related Articles NMR assignment of protein Rv1980c from Mycobacterium tuberculosis.
J Biomol NMR. 2005 Sep;33(1):73
Authors: Danahy JM, Potter BM, Geisbrecht BV, Laity JH
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[NMR paper] Privileged molecules for protein binding identified from NMR-based screening.
Privileged molecules for protein binding identified from NMR-based screening.
Related Articles Privileged molecules for protein binding identified from NMR-based screening.
J Med Chem. 2000 Sep 7;43(18):3443-7
Authors: Hajduk PJ, Bures M, Praestgaard J, Fesik SW
A statistical analysis of NMR-derived binding data on 11 protein targets was performed to identify molecular motifs that are preferred for protein binding. The analysis indicates that compounds which contain a biphenyl substructure preferentially bind to a wide range of proteins and...
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Novel Small Molecule Inhibitors of MDR Mycobacterium tuberculosis by NMR Fragment Scr
Novel Small Molecule Inhibitors of MDR Mycobacterium tuberculosis by NMR Fragment Screening of Antigen 85C.
Related Articles Novel Small Molecule Inhibitors of MDR Mycobacterium tuberculosis by NMR Fragment Screening of Antigen 85C.
J Med Chem. 2010 Nov 12;
Authors: Scheich C, Puetter V, Schade M
Protein target-based discovery of novel antibiotics has been largely unsuccessful despite rich genome information. Particularly in need are new antibiotics for tuberculosis, which kills 1.6 million people annually and shows a rapid increase in...
Potent inhibitors of Mycobacterium tuberculosis growth identified by using in-cell NMR-based screening.
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