| Literature DB >> 28056740 |
Lorelei Johnson1, Ing Swie Goping2, Aja Rieger2, Jonathan Y Mane1, Torin Huzil1, Asok Banerjee3, Richard Luduena3, Bashar Hassani1, Philip Winter1, Jack A Tuszynski1.
Abstract
In this paper we provide an overview of the status of various colchicine derivatives in preclinical development with special focus on their anti-cancer activity. We discuss several groups of compounds that have been designed to differentially bind with specific affinities for tubulin β isotypes, especially in regard to βIII, which is commonly over-expressed in cancer. Computational prediction, protein-based and cell-based assays are summarized as well as some animal tests conducted on these compounds. It is concluded that an untapped potential exists for exploiting the colchicine scaffold as a pharmacophore with the possibility of increasing its affinity for tubulin isotypes overexpressed in cancer and decreasing it for normal cells thereby widening the therapeutic window. Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.Entities:
Keywords: Animal tests; Anti-cancer; Colchicine Scaffold; Pharmacophore; Tubulin β isotypes
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Year: 2017 PMID: 28056740 DOI: 10.2174/1568026617666170104143618
Source DB: PubMed Journal: Curr Top Med Chem ISSN: 1568-0266 Impact factor: 3.295