Celogentin mimetics as inhibitors of tubulin polymerization

Varsha J Thombare; James A Holden; Eric C Reynolds; Neil M O'Brien-Simpson; Craig A Hutton

doi:10.1002/psc.3239

Celogentin mimetics as inhibitors of tubulin polymerization

J Pept Sci. 2020 Mar;26(3):e3239. doi: 10.1002/psc.3239. Epub 2019 Dec 17.

Authors

Varsha J Thombare^{1

2}, James A Holden^{2

3}, Eric C Reynolds^{2

3}, Neil M O'Brien-Simpson^{2

3}, Craig A Hutton^{1

2}

Affiliations

¹ School of Chemistry, The University of Melbourne, Victoria, 3010, Australia.
² Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Victoria, 3010, Australia.
³ Melbourne Dental School and Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Victoria, 3010, Australia.

PMID: 31847053
DOI: 10.1002/psc.3239

Abstract

Bicyclic analogues of celogentin C have been synthesized in which the side chain-side chain cross-links are replaced by thioether bonds. Several of the simplified bicyclic peptides displayed potent inhibition of tubulin polymerization.

MeSH terms

Chromatography, High Pressure Liquid
Molecular Structure
Peptides, Cyclic / chemistry
Peptides, Cyclic / pharmacology*
Polymerization / drug effects
Structure-Activity Relationship
Tubulin / chemistry*

Substances

Peptides, Cyclic
Tubulin
celogentin C

Abstract

MeSH terms

Substances

Grants and funding