Highly efficient real-time TRPV1 screening methodology for effective drug candidates

Cited 3 time in scopus
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Title
Highly efficient real-time TRPV1 screening methodology for effective drug candidates
Author(s)
Seong Gi Lim; Sung Eun Seo; Seongjae Jo; Kyung Ho Kim; Lina Kim; Oh Seok Kwon
Bibliographic Citation
ACS Omega, vol. 7, no. 41, pp. 36441-36447
Publication Year
2022
Abstract
Transient receptor potential vanilloid 1 (TRPV1) agonists that bind to the vanilloid pocket are being actively studied in the pharmaceutical industry to develop novel treatments for chronic pain and cancer. To discover synthetic vanilloids without the side effect of capsaicin, a time-consuming process of drug candidate selection is essential to a myriad of chemical compounds. Herein, we propose a novel approach to field-effect transistors for the fast and facile screening of lead vanilloid compounds for the development of TRPV1-targeting medications. The graphene field-effect transistor was fabricated with human TRPV1 receptor protein as the bioprobe, and various analyses (SEM, Raman, and FT-IR) were utilized to verify successful manufacture. Simulations of TRPV1 with capsaicin, olvanil, and arvanil were conducted using AutoDock Vina/PyMOL to confirm the binding affinity. The interaction of the ligands with TRPV1 was detected via the fabricated platform, and the collected responses corresponded to the simulation analysis.
ISSN
2470-1343
Publisher
Amer Chem Soc
DOI
http://dx.doi.org/10.1021/acsomega.2c04202
Type
Article
Appears in Collections:
Division of Research on National Challenges > Infectious Disease Research Center > 1. Journal Articles
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