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Identification of cyclic hexapeptides natural products with inhibitory potency against Mycobacterium tuberculosis.

Sheo B SinghJoshua OdingoMai A BaileyBjorn SundeAaron KorkegianTheresa O'MalleyYulia OvechkinaThomas R IoergerJames C SacchettiniKatherine YoungDavid B OlsenTanya Parish
Published in: BMC research notes (2018)
A set of ~ 500 purified natural product compounds was screened for inhibition against the human pathogen Mycobacterium tuberculosis. A series of cyclic hexapeptides with anti-tubercular activity was identified. Five analogs from a set of sixteen closely related compounds were active, with minimum inhibitory concentrations ranging from 2.3 to 8.9 μM. Eleven structural analogs had no significant activity (MIC > 20 μM) demonstrating structure activity relationship. Sequencing of resistant mutant isolates failed to identify changes accounting for the resistance phenotype.
Keyphrases
  • mycobacterium tuberculosis
  • structure activity relationship
  • endothelial cells
  • pulmonary tuberculosis
  • molecular docking
  • single cell
  • induced pluripotent stem cells
  • candida albicans
  • pluripotent stem cells