Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity

Amit A Joharapurkar, Nirav A Dhanesha, Mukul R Jain Department of Pharmacology and Toxicology, Zydus Research Centre, Cadila Healthcare Limited, Ahmedabad, India Abstract: Worldwide prevalence of obesity has nearly doubled since 1980. Obesity is the result of interactions among the environmental f...

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Autores principales: Joharapurkar AA, Dhanesha NA, Jain MR
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Publicado: Dove Medical Press 2014
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spelling oai:doaj.org-article:1cfb07d69eeb45deaa87a8b0f73ea83c2021-12-02T08:05:04ZInhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity1178-7007https://doaj.org/article/1cfb07d69eeb45deaa87a8b0f73ea83c2014-02-01T00:00:00Zhttp://www.dovepress.com/inhibition-of-the-methionine-aminopeptidase-2-enzyme-for-the-treatment-a15982https://doaj.org/toc/1178-7007 Amit A Joharapurkar, Nirav A Dhanesha, Mukul R Jain Department of Pharmacology and Toxicology, Zydus Research Centre, Cadila Healthcare Limited, Ahmedabad, India Abstract: Worldwide prevalence of obesity has nearly doubled since 1980. Obesity is the result of interactions among the environmental factors, genetic predisposition, and human behavior. Even modest weight reduction in obese patients provides beneficial health outcomes. For effective weight reduction, a drug should either increase energy expenditure or decrease energy intake without causing serious adverse effects. To overcome lack of efficacy and central nervous system related side effects, exploitation of the peripheral mechanism of anti-obesity action is needed. Inhibition of pathological angiogenesis in adipose tissue is one such peripheral mechanism that has attracted the attention of researchers in this area. Although originally developed as anti-cancer agents, methionine aminopeptidase (MetAP2) inhibitors induce significant and sustained weight reduction. Here, we review preclinical and clinical pharmacology of MetAP2 inhibitors. Beloranib is a prototype MetAP2 inhibitor, and currently in advanced clinical trials for the treatment of obesity. Clinical data of beloranib indicate that MetAP2 inhibitors could be a future treatment option for weight reduction without serious adverse effects. Further clinical data from Phase III trials will add to our growing knowledge of MetAP2 inhibitor potential for anti-obesity therapy. Keywords: angiogenesis, beloranib, body weight, MetAP2, anti-obesityJoharapurkar AADhanesha NAJain MRDove Medical PressarticleSpecialties of internal medicineRC581-951ENDiabetes, Metabolic Syndrome and Obesity: Targets and Therapy, Vol 2014, Iss default, Pp 73-84 (2014)
institution DOAJ
collection DOAJ
language EN
topic Specialties of internal medicine
RC581-951
spellingShingle Specialties of internal medicine
RC581-951
Joharapurkar AA
Dhanesha NA
Jain MR
Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity
description Amit A Joharapurkar, Nirav A Dhanesha, Mukul R Jain Department of Pharmacology and Toxicology, Zydus Research Centre, Cadila Healthcare Limited, Ahmedabad, India Abstract: Worldwide prevalence of obesity has nearly doubled since 1980. Obesity is the result of interactions among the environmental factors, genetic predisposition, and human behavior. Even modest weight reduction in obese patients provides beneficial health outcomes. For effective weight reduction, a drug should either increase energy expenditure or decrease energy intake without causing serious adverse effects. To overcome lack of efficacy and central nervous system related side effects, exploitation of the peripheral mechanism of anti-obesity action is needed. Inhibition of pathological angiogenesis in adipose tissue is one such peripheral mechanism that has attracted the attention of researchers in this area. Although originally developed as anti-cancer agents, methionine aminopeptidase (MetAP2) inhibitors induce significant and sustained weight reduction. Here, we review preclinical and clinical pharmacology of MetAP2 inhibitors. Beloranib is a prototype MetAP2 inhibitor, and currently in advanced clinical trials for the treatment of obesity. Clinical data of beloranib indicate that MetAP2 inhibitors could be a future treatment option for weight reduction without serious adverse effects. Further clinical data from Phase III trials will add to our growing knowledge of MetAP2 inhibitor potential for anti-obesity therapy. Keywords: angiogenesis, beloranib, body weight, MetAP2, anti-obesity
format article
author Joharapurkar AA
Dhanesha NA
Jain MR
author_facet Joharapurkar AA
Dhanesha NA
Jain MR
author_sort Joharapurkar AA
title Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity
title_short Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity
title_full Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity
title_fullStr Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity
title_full_unstemmed Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity
title_sort inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity
publisher Dove Medical Press
publishDate 2014
url https://doaj.org/article/1cfb07d69eeb45deaa87a8b0f73ea83c
work_keys_str_mv AT joharapurkaraa inhibitionofthemethionineaminopeptidase2enzymeforthetreatmentofobesity
AT dhaneshana inhibitionofthemethionineaminopeptidase2enzymeforthetreatmentofobesity
AT jainmr inhibitionofthemethionineaminopeptidase2enzymeforthetreatmentofobesity
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