In Silico Analysis of Triamterene as a Potential Dual Inhibitor of VEGFR-2 and c-Met Receptors

Stuart Lutimba, Baraya Saleem, Eiman Aleem, Mohammed A. Mansour · 2024

Read In Silico Analysis of Triamterene as a Potential Dual Inhibitor of VEGFR-2 and c-Met Receptors by Stuart Lutimba, Baraya Saleem, Eiman Aleem, Mohammed A. Mansour (2024) in the Tower of Babel, a free online library of public-domain works preserved in clean, searchable text. No sign-up. The full text is served as a plain-text file at a predictable URL, where text is present: https://antarctic-labs.com/tower-of-babel/pmc-11676455.txt.

Description

Stuart Lutimba and co-authors screen approved drugs in silico for a double hit on two cancer receptors in a 2024 study. The receptors VEGFR-2 and c-Met each drive tumor growth and blood vessel supply, and blocking one alone invites resistance. A single drug blocking both could outflank that escape.

Computer docking and molecular dynamics simulations tested 2,016 approved drugs against both targets. Two drugs proved strong but single-minded, one for each receptor. A third, the diuretic triamterene, bound both receptors specifically and strongly. Simulations mapped the exact residues it grips in each active site. The authors present triamterene as a repurposing candidate and the screen as a template for dual-inhibitor hunts, pending lab validation.

Catalog record

CREATORStuart Lutimba, Baraya Saleem, Eiman Aleem, Mohammed A. Mansour
YEAR2024
COLLECTIONPAPERS
FORMATTXT
FILE SIZE54 KB
VERSION1.0
LICENSECC BY 4.0
RIGHTSCC BY
SOURCEEurope PMC

Source: https://europepmc.org/articles/PMC11676455

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