Literature DB >> 30616053

Structure-activity relationship (SAR) studies of synthetic glycogen synthase kinase-3β inhibitors: A critical review.

M Xu1, S L Wang1, L Zhu1, P Y Wu1, W B Dai1, K P Rakesh2.   

Abstract

Glycogen Synthase Kinase-3 (GSK-3) is a constitutively dynamic, omnipresent serine/threonine protein kinase regularly called as a "multitasking kinase" due to its pliable function in diverse signaling pathways. It exists in two isoforms i.e., GSK-3α and GSK-3β. Inhibition of GSK-3 may be useful in curing various diseases such as Alzheimer's disease, type II diabetes, mood disorders, cancers, chronic inflammatory agents, stroke, bipolar disorders and so on, but the approach poses significant challenges. Lithium was the first GSK-3β inhibitor to be used for therapeutic outcome and has been effectively used for many years. In recent years, a large number of structurally diverse potent GSK-3β inhibitors are reported. The present review focuses on the recent developments in the area of medicinal chemistry to explore the diverse chemical structures of potent GSK-3β inhibitors and also describes its structure-activity relationships (SAR) and molecular binding interactions of favorable applicability in various diseases.
Copyright © 2018 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  GSK-3β; Molecular docking; SAR; Synthetic analogs

Mesh:

Substances:

Year:  2018        PMID: 30616053     DOI: 10.1016/j.ejmech.2018.12.073

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  6 in total

1.  The crystal structure of the protein kinase HIPK2 reveals a unique architecture of its CMGC-insert region.

Authors:  Christopher Agnew; Lijun Liu; Shu Liu; Wei Xu; Liang You; Wayland Yeung; Natarajan Kannan; David Jablons; Natalia Jura
Journal:  J Biol Chem       Date:  2019-07-24       Impact factor: 5.157

2.  Optimization of Indazole-Based GSK-3 Inhibitors with Mitigated hERG Issue and In Vivo Activity in a Mood Disorder Model.

Authors:  Federica Prati; Rosa Buonfiglio; Guido Furlotti; Claudia Cavarischia; Giorgina Mangano; Rossella Picollo; Laura Oggianu; Anna di Matteo; Silvana Olivieri; Graziella Bovi; Pier Francesca Porceddu; Angelo Reggiani; Beatrice Garrone; Francesco Paolo Di Giorgio; Rosella Ombrato
Journal:  ACS Med Chem Lett       Date:  2020-03-24       Impact factor: 4.345

3.  Lithium Chloride Protects against Sepsis-Induced Skeletal Muscle Atrophy and Cancer Cachexia.

Authors:  Ji-Hyung Lee; Seon-Wook Kim; Jun-Hyeong Kim; Hyun-Jun Kim; JungIn Um; Da-Woon Jung; Darren R Williams
Journal:  Cells       Date:  2021-04-26       Impact factor: 6.600

4.  Novel oxindole/benzofuran hybrids as potential dual CDK2/GSK-3β inhibitors targeting breast cancer: design, synthesis, biological evaluation, and in silico studies.

Authors:  Wagdy M Eldehna; Sara T Al-Rashood; Tarfah Al-Warhi; Razan O Eskandrani; Amal Alharbi; Ahmed M El Kerdawy
Journal:  J Enzyme Inhib Med Chem       Date:  2021-12       Impact factor: 5.051

5.  Glycogen Synthase Kinase 3β: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery?

Authors:  Angela De Simone; Vincenzo Tumiatti; Vincenza Andrisano; Andrea Milelli
Journal:  J Med Chem       Date:  2020-12-21       Impact factor: 7.446

6.  Sulfur-containing therapeutics in the treatment of Alzheimer's disease.

Authors:  Haizhou Zhu; Venkateshwara Dronamraju; Wei Xie; Swati S More
Journal:  Med Chem Res       Date:  2021-01-15       Impact factor: 1.965

  6 in total

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