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Alkyloxy carbonyl modified hexapeptides as a high affinity compounds for Wnt5A protein in the treatment of psoriasis

Psoriasis is one of the most prevalent chronic inflammatory diseases of the skin. The Wnt pathways have been documented to play essential role in stem cell self-renewal and keratinocyte differentiation in the skin. Antagonizing the Wnt5a protein would emerge as a novel therapeutics in psoriasis trea...

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Autores principales: Kelotra, Ankit, Gokhale, Sadashiv M, Kelotra, Seema, Mukadam, Vaidehi, Nagwanshi, Komal, Bandaru, Srinivas, Nayarisseri, Anuraj, Bidwai, Anil
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Biomedical Informatics 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4312367/
https://www.ncbi.nlm.nih.gov/pubmed/25670877
http://dx.doi.org/10.6026/97320630010743
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author Kelotra, Ankit
Gokhale, Sadashiv M
Kelotra, Seema
Mukadam, Vaidehi
Nagwanshi, Komal
Bandaru, Srinivas
Nayarisseri, Anuraj
Bidwai, Anil
author_facet Kelotra, Ankit
Gokhale, Sadashiv M
Kelotra, Seema
Mukadam, Vaidehi
Nagwanshi, Komal
Bandaru, Srinivas
Nayarisseri, Anuraj
Bidwai, Anil
author_sort Kelotra, Ankit
collection PubMed
description Psoriasis is one of the most prevalent chronic inflammatory diseases of the skin. The Wnt pathways have been documented to play essential role in stem cell self-renewal and keratinocyte differentiation in the skin. Antagonizing the Wnt5a protein would emerge as a novel therapeutics in psoriasis treatment. In this view, we have developed and characterized series of compounds by attaching varied tertiary alkyloxy carbonyl groups at the N-terminal end of the hexapeptide (Met-Asp-Gly-Cys-Glu-Leu) bestowed to inhibit Wnt/Ca2+ signaling in psoriasis. Hexapeptide compound with 1,1-diphenylethoxy carbonyl group attached to N-terminal end of hexapeptide demonstrated highest binding affinity amongst all the evaluated compounds. The compound identified in the study can be subjected further for in vitro and in vivo studies for ADMET properties.
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spelling pubmed-43123672015-02-10 Alkyloxy carbonyl modified hexapeptides as a high affinity compounds for Wnt5A protein in the treatment of psoriasis Kelotra, Ankit Gokhale, Sadashiv M Kelotra, Seema Mukadam, Vaidehi Nagwanshi, Komal Bandaru, Srinivas Nayarisseri, Anuraj Bidwai, Anil Bioinformation Hypothesis Psoriasis is one of the most prevalent chronic inflammatory diseases of the skin. The Wnt pathways have been documented to play essential role in stem cell self-renewal and keratinocyte differentiation in the skin. Antagonizing the Wnt5a protein would emerge as a novel therapeutics in psoriasis treatment. In this view, we have developed and characterized series of compounds by attaching varied tertiary alkyloxy carbonyl groups at the N-terminal end of the hexapeptide (Met-Asp-Gly-Cys-Glu-Leu) bestowed to inhibit Wnt/Ca2+ signaling in psoriasis. Hexapeptide compound with 1,1-diphenylethoxy carbonyl group attached to N-terminal end of hexapeptide demonstrated highest binding affinity amongst all the evaluated compounds. The compound identified in the study can be subjected further for in vitro and in vivo studies for ADMET properties. Biomedical Informatics 2014-12-31 /pmc/articles/PMC4312367/ /pubmed/25670877 http://dx.doi.org/10.6026/97320630010743 Text en © 2014 Biomedical Informatics This is an open-access article, which permits unrestricted use, distribution, and reproduction in any medium, for non-commercial purposes, provided the original author and source are credited.
spellingShingle Hypothesis
Kelotra, Ankit
Gokhale, Sadashiv M
Kelotra, Seema
Mukadam, Vaidehi
Nagwanshi, Komal
Bandaru, Srinivas
Nayarisseri, Anuraj
Bidwai, Anil
Alkyloxy carbonyl modified hexapeptides as a high affinity compounds for Wnt5A protein in the treatment of psoriasis
title Alkyloxy carbonyl modified hexapeptides as a high affinity compounds for Wnt5A protein in the treatment of psoriasis
title_full Alkyloxy carbonyl modified hexapeptides as a high affinity compounds for Wnt5A protein in the treatment of psoriasis
title_fullStr Alkyloxy carbonyl modified hexapeptides as a high affinity compounds for Wnt5A protein in the treatment of psoriasis
title_full_unstemmed Alkyloxy carbonyl modified hexapeptides as a high affinity compounds for Wnt5A protein in the treatment of psoriasis
title_short Alkyloxy carbonyl modified hexapeptides as a high affinity compounds for Wnt5A protein in the treatment of psoriasis
title_sort alkyloxy carbonyl modified hexapeptides as a high affinity compounds for wnt5a protein in the treatment of psoriasis
topic Hypothesis
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4312367/
https://www.ncbi.nlm.nih.gov/pubmed/25670877
http://dx.doi.org/10.6026/97320630010743
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