Literature DB >> 20227879

Endoxifen is a new potent inhibitor of PKC: a potential therapeutic agent for bipolar disorder.

Shoukath M Ali1, Ateeq Ahmad, Syed Shahabuddin, Moghis U Ahmad, Saifuddin Sheikh, Imran Ahmad.   

Abstract

Protein kinase C (PKC) plays a major role in regulation of both pre and postsynaptic neurotransmission. Excessive activation of PKC results in symptoms related to bipolar disorder. Tamoxifen, a widely used breast cancer drug is known to inhibit PKC and demonstrate antimanic properties in human. We describe herein the synthesis of endoxifen, a tamoxifen active metabolite and compared its PKC inhibitory activity with that of tamoxifen. Endoxifen exhibited fourfold higher potency compared to tamoxifen. Copyright 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID： 20227879     DOI： 10.1016/j.bmcl.2010.02.024

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

Review 1.  Tamoxifen and amphetamine abuse: Are there therapeutic possibilities?

Authors:  Sarah Mikelman; Natalie Mardirossian; Margaret E Gnegy
Journal:  J Chem Neuroanat       Date:  2016-08-30       Impact factor: 3.052

2.  Design and synthesis of norendoxifen analogues with dual aromatase inhibitory and estrogen receptor modulatory activities.

Authors:  Wei Lv; Jinzhong Liu; Todd C Skaar; David A Flockhart; Mark Cushman
Journal:  J Med Chem       Date:  2015-03-09       Impact factor: 7.446

3.  Characterization of the isomeric configuration and impurities of (Z)-endoxifen by 2D NMR, high resolution LC⬜MS, and quantitative HPLC analysis.

Authors:  Phyllis Elkins; Donna Coleman; Jason Burgess; Michael Gardner; John Hines; Brendan Scott; Michelle Kroenke; Jami Larson; Melissa Lightner; Gregory Turner; Jonathan White; Paul Liu
Journal:  J Pharm Biomed Anal       Date:  2013-07-24       Impact factor: 3.935

Review 4.  Role of Protein Kinase C in Bipolar Disorder: A Review of the Current Literature.

Authors:  Ashwini Saxena; Giselli Scaini; Daniela V Bavaresco; Camila Leite; Samira S Valvassori; André F Carvalho; João Quevedo
Journal:  Mol Neuropsychiatry       Date:  2017-10-07

Review 5.  Proof of concept trials in bipolar disorder and major depressive disorder: a translational perspective in the search for improved treatments.

Authors:  Rodrigo Machado-Vieira; Carlos A Zarate
Journal:  Depress Anxiety       Date:  2011-02-24       Impact factor: 6.505

Review 6.  Endoxifen, an Estrogen Receptor Targeted Therapy: From Bench to Bedside.

Authors:  Swaathi Jayaraman; Joel M Reid; John R Hawse; Matthew P Goetz
Journal:  Endocrinology       Date:  2021-12-01       Impact factor: 5.051

7.  Calcium-dependent intracellular signal pathways in primary cultured adipocytes and ANK3 gene variation in patients with bipolar disorder and healthy controls.

Authors:  A Hayashi; K Le Gal; K Södersten; D Vizlin-Hodzic; H Ågren; K Funa
Journal:  Mol Psychiatry       Date:  2014-10-14       Impact factor: 15.992

8.  New model of action for mood stabilizers: phosphoproteome from rat pre-frontal cortex synaptoneurosomal preparations.

Authors:  Maria Corena-McLeod; Consuelo Walss-Bass; Alfredo Oliveros; Andres Gordillo Villegas; Carolina Ceballos; Cristine M Charlesworth; Benjamin Madden; Paul J Linser; Leslie Van Ekeris; Kristin Smith; Elliott Richelson
Journal:  PLoS One       Date:  2013-05-14       Impact factor: 3.240

9.  Endoxifen, a New Treatment Option for Mania: A Double-Blind, Active-Controlled Trial Demonstrates the Antimanic Efficacy of Endoxifen.

Authors:  A Ahmad; S Sheikh; T Shah; M S Reddy; Bsv Prasad; K K Verma; B B Chandrakant; M Paithankar; P Kale; R V Solanki; R Patel; H Barkate; I Ahmad
Journal:  Clin Transl Sci       Date:  2016-06-27       Impact factor: 4.689
  9 in total

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