Cargando…

Highly Efficient Real-Time TRPV1 Screening Methodology for Effective Drug Candidates

[Image: see text] 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 ti...

Descripción completa

Detalles Bibliográficos
Autores principales: Lim, Seong Gi, Seo, Sung Eun, Jo, Seongjae, Kim, Kyung Ho, Kim, Lina, Kwon, Oh Seok
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2022
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9583638/
https://www.ncbi.nlm.nih.gov/pubmed/36278091
http://dx.doi.org/10.1021/acsomega.2c04202
_version_ 1784813115876048896
author Lim, Seong Gi
Seo, Sung Eun
Jo, Seongjae
Kim, Kyung Ho
Kim, Lina
Kwon, Oh Seok
author_facet Lim, Seong Gi
Seo, Sung Eun
Jo, Seongjae
Kim, Kyung Ho
Kim, Lina
Kwon, Oh Seok
author_sort Lim, Seong Gi
collection PubMed
description [Image: see text] 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.
format Online
Article
Text
id pubmed-9583638
institution National Center for Biotechnology Information
language English
publishDate 2022
publisher American Chemical Society
record_format MEDLINE/PubMed
spelling pubmed-95836382022-10-21 Highly Efficient Real-Time TRPV1 Screening Methodology for Effective Drug Candidates Lim, Seong Gi Seo, Sung Eun Jo, Seongjae Kim, Kyung Ho Kim, Lina Kwon, Oh Seok ACS Omega [Image: see text] 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. American Chemical Society 2022-10-04 /pmc/articles/PMC9583638/ /pubmed/36278091 http://dx.doi.org/10.1021/acsomega.2c04202 Text en © 2022 The Authors. Published by American Chemical Society https://creativecommons.org/licenses/by-nc-nd/4.0/Permits non-commercial access and re-use, provided that author attribution and integrity are maintained; but does not permit creation of adaptations or other derivative works (https://creativecommons.org/licenses/by-nc-nd/4.0/).
spellingShingle Lim, Seong Gi
Seo, Sung Eun
Jo, Seongjae
Kim, Kyung Ho
Kim, Lina
Kwon, Oh Seok
Highly Efficient Real-Time TRPV1 Screening Methodology for Effective Drug Candidates
title Highly Efficient Real-Time TRPV1 Screening Methodology for Effective Drug Candidates
title_full Highly Efficient Real-Time TRPV1 Screening Methodology for Effective Drug Candidates
title_fullStr Highly Efficient Real-Time TRPV1 Screening Methodology for Effective Drug Candidates
title_full_unstemmed Highly Efficient Real-Time TRPV1 Screening Methodology for Effective Drug Candidates
title_short Highly Efficient Real-Time TRPV1 Screening Methodology for Effective Drug Candidates
title_sort highly efficient real-time trpv1 screening methodology for effective drug candidates
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9583638/
https://www.ncbi.nlm.nih.gov/pubmed/36278091
http://dx.doi.org/10.1021/acsomega.2c04202
work_keys_str_mv AT limseonggi highlyefficientrealtimetrpv1screeningmethodologyforeffectivedrugcandidates
AT seosungeun highlyefficientrealtimetrpv1screeningmethodologyforeffectivedrugcandidates
AT joseongjae highlyefficientrealtimetrpv1screeningmethodologyforeffectivedrugcandidates
AT kimkyungho highlyefficientrealtimetrpv1screeningmethodologyforeffectivedrugcandidates
AT kimlina highlyefficientrealtimetrpv1screeningmethodologyforeffectivedrugcandidates
AT kwonohseok highlyefficientrealtimetrpv1screeningmethodologyforeffectivedrugcandidates