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

Sheo B. Singh; Joshua Odingo; Mai A. Bailey; Bjorn Sunde; Aaron Korkegian; Theresa O'Malley; Yulia Ovechkina; Thomas R. Ioerger; James C. Sacchettini; Katherine Young; David B. Olsen; Tanya Parish

doi:10.1186/s13104-018-3526-z

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

Sheo B. Singh
, Joshua Odingo
, Mai A. Bailey
, Bjorn Sunde
, Aaron Korkegian
, Theresa O'Malley
, Yulia Ovechkina
, Thomas R. Ioerger
, James C. Sacchettini
, Katherine Young
, David B. Olsen
, Tanya Parish

Merck
SBS Pharma Consulting LLC
Infectious Disease Research Institute
Texas A&M University
TB Discovery Research

Research output: Contribution to journal › Article › peer-review

2 Citations (Scopus)

Abstract

Objective: Our aim was to identify natural products with anti-tubercular activity.

Results: 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.

Original language	English
Article number	416
Journal	BMC Research Notes
Volume	11
Issue number	1
DOIs	https://doi.org/10.1186/s13104-018-3526-z
Publication status	Published - 28 Jun 2018
Externally published	Yes

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

SDG 3 Good Health and Well-being

Keywords

Anti-tubercular
Antibacterial
Antibiotic resistance
Mycobacteria
Natural product

Access to Document

10.1186/s13104-018-3526-z

Cite this

Singh, S. B., Odingo, J., Bailey, M. A., Sunde, B., Korkegian, A., O'Malley, T., Ovechkina, Y., Ioerger, T. R., Sacchettini, J. C., Young, K., Olsen, D. B., & Parish, T. (2018). Identification of cyclic hexapeptides natural products with inhibitory potency against Mycobacterium tuberculosis. BMC Research Notes, 11(1), Article 416. https://doi.org/10.1186/s13104-018-3526-z

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abstract = "Objective: Our aim was to identify natural products with anti-tubercular activity. Results: A set of \textasciitilde{} 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.",

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doi = "10.1186/s13104-018-3526-z",

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AU - Singh, Sheo B.

AU - Odingo, Joshua

AU - Bailey, Mai A.

AU - Sunde, Bjorn

AU - Korkegian, Aaron

AU - O'Malley, Theresa

AU - Ovechkina, Yulia

AU - Ioerger, Thomas R.

AU - Sacchettini, James C.

AU - Young, Katherine

AU - Olsen, David B.

AU - Parish, Tanya

PY - 2018/6/28

Y1 - 2018/6/28

N2 - Objective: Our aim was to identify natural products with anti-tubercular activity. Results: 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.

AB - Objective: Our aim was to identify natural products with anti-tubercular activity. Results: 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.

KW - Anti-tubercular

KW - Antibacterial

KW - Antibiotic resistance

KW - Mycobacteria

KW - Natural product

U2 - 10.1186/s13104-018-3526-z

DO - 10.1186/s13104-018-3526-z

M3 - Article

C2 - 29954459

AN - SCOPUS:85049209216

SN - 1756-0500

VL - 11

JO - BMC Research Notes

JF - BMC Research Notes

IS - 1

M1 - 416

ER -

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

Abstract

UN SDGs

Keywords

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