Category: Medicinal Chemistry

Treatment of Type 2 diabetes mellitus (T2DM): Can GLP-1 Receptor Agonists fill in the gaps?

Type 2 diabetes mellitus (T2DM) is a chronic metabolic syndrome, which occurs due to increased glucose levels in the human body. There has been lot of work in developing novel approaches to tackle this disease. GLP-1 receptor (GLP-1R), one of the class-B G-protein-coupled receptors (GPCR), is a budding molecular target to design drugs for treating type 2 diabetes. In this review, authors have summarized the physiological actions of Glucagon-like peptide-1 receptor (GLP-1R) and current available drugs based on GLP-1 RAs. Some of the exemplary studies in this area have been examined in detail. Authors conclude that development of degradation-resistant, long-acting GLP-1 receptor agonists is a promising area of research and lot of work needs to be done to understand its mechanism of action.

Published in: Chemical Biology Letters

Link: https://pubs.thesciencein.org/journal/index.php/cbl/article/view/132

Chemical libraries targeting Liver Stage Malarial infection

urn:nbn:sciencein.cbl.2019v6.96

Chemical Scaffolds Targeting liver-stage malaria parasite lifecycle

Published in: Chemical Biology Letters

  • Neha Sharma
  • Poonam FNU
  • Prakasha Kempaiah
  • Brijesh Rathi University of Delhi

Keywords: Malaria, Liver stage, Primaquine, Atovaquone, Clinical trials

Abstract

Despite the noteworthy advances in the use of chemotherapy for malaria, it continues to constantly affect large number of individuals. New molecules capable of blocking life-cycle of the parasite, preferably through targeting novel pathways and various modes of action, are increasingly becoming area of interest. Phenotypic screening of large chemical libraries is certainly one of the important criteria for the discovery of new and effective drugs. In recent years, diverse research groups including pharmaceutical industries have performed this large-scale phenotypic screening to identify the potential drug molecules. Most of the antimalarial drugs target blood-stage malarial infection and remain either less potent or ineffective against other life stages i.e. liver-stage, and the gametocyte stages of the parasite. Although, liver stage is considered as a crucial drug target, limited clinical options have significantly hampered the discovery of effective treatments. This short review presents the collection of selective molecules targeting specifically liver stage malaria parasites.

Cite as: Sharma, N., FNU, P., Kempaiah, P., & Rathi, B. (2019). Chemical libraries targeting Liver Stage Malarial infection. Chemical Biology Letters, 6(1), 14-22.

Retrieved full text from https://pubs.thesciencein.org/journal/index.php/cbl/article/view/41