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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...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical Society
2022
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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 |
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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 |
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