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      Biomedical Importance of Indoles

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          Abstract

          The indole nucleus is an important element of many natural and synthetic molecules with significant biological activity. This review covers some of the relevant and recent achievements in the biological, chemical and pharmacological activity of important indole derivatives in the areas of drug discovery and analysis.

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          Overexpression of alpha2A-adrenergic receptors contributes to type 2 diabetes.

          Vini Nagaraj, Albert Salehi, Leif Groop … (2010)
          Several common genetic variations have been associated with type 2 diabetes, but the exact disease mechanisms are still poorly elucidated. Using congenic strains from the diabetic Goto-Kakizaki rat, we identified a 1.4-megabase genomic locus that was linked to impaired insulin granule docking at the plasma membrane and reduced beta cell exocytosis. In this locus, Adra2a, encoding the alpha2A-adrenergic receptor [alpha(2A)AR], was significantly overexpressed. Alpha(2A)AR mediates adrenergic suppression of insulin secretion. Pharmacological receptor antagonism, silencing of receptor expression, or blockade of downstream effectors rescued insulin secretion in congenic islets. Furthermore, we identified a single-nucleotide polymorphism in the human ADRA2A gene for which risk allele carriers exhibited overexpression of alpha(2A)AR, reduced insulin secretion, and increased type 2 diabetes risk. Human pancreatic islets from risk allele carriers exhibited reduced granule docking and secreted less insulin in response to glucose; both effects were counteracted by pharmacological alpha(2A)AR antagonists.
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            Structure, bioactivity and synthesis of natural products with hexahydropyrrolo[2,3-b]indole.

            Pau Ruiz-Sanchis, Svetlana Savina, Fernando Albericio … (2011)
            Research on natural products containing hexahydropyrrolo[2,3-b]indole (HPI) has dramatically increased during the past few years. Newly discovered natural products with complex structures and important biological activities have recently been isolated and synthesized. This review summarizes the structures, biological activities, and synthetic routes for natural compounds containing HPI, emphasizing the different strategies for assembling this motif. It covers a broad range of molecules, from small alkaloids to complex peptides.
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              Tryptophan biosynthesis and metabolism: biochemical and molecular genetics.

              Peter R Last, E Radwanski (1995)
              Article 0 comments Cited 76 times – based on 0 reviews     Review now
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                Author and article information

                Journal
                Journal ID (nlm-ta): Molecules
                Journal ID (iso-abbrev): Molecules
                Journal ID (publisher-id): molecules
                Title: Molecules
                Publisher: MDPI
                ISSN (Electronic): 1420-3049
                Publication date (Electronic): 06 June 2013
                Publication date Collection: June 2013
                Volume: 18
                Issue: 6
                Pages: 6620-6662
                Affiliations
                [1 ]Plasma Bioscience Research Center, Kwangwoon University, Seoul 139701, Korea; E-Mails: attri.pankaj@ 123456gmail.com (P.A.); nash_bms@ 123456yahoo.co.in (N.K.); hyeokkim@ 123456kw.ac.kr (C.H.K.)
                [2 ]Department of Chemistry, University of Delhi, Delhi 110007, India
                Author notes
                [* ] Authors to whom correspondence should be addressed; E-Mails: kaushik.nagendra@ 123456gmail.com (N.K.K); neha.bioplasma@ 123456gmail.com (N.K.); averma@ 123456acbr.du.ac.in (A.K.V.); ehchoi@ 123456kw.ac.kr (E.H.C.); Tel.: +82-10-4187-8618 (N.K.K.) Fax: +82-940-5664 (N.K.K).
                Article
                Publisher ID: molecules-18-06620
                DOI: 10.3390/molecules18066620
                PMC ID: 6270133
                PubMed ID: 23743888
                SO-VID: f295016b-4974-4fcd-995c-57a328deca26
                Copyright © © 2013 by the authors; licensee MDPI, Basel, Switzerland.
                License:

                This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/3.0/).

                History
                Date received : 17 April 2013
                Date revision received : 27 May 2013
                Date accepted : 28 May 2013
                Categories
                Subject: Review

                Keywords: indole,biomedical application,bioactivity,pharmacological activity
                Data availability:
                Keywords: indole, biomedical application, bioactivity, pharmacological activity

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