Publications by authors named "Karthik G Pujar"

Article Synopsis
  • - The study focuses on inhibiting DprE1, a crucial enzyme in the synthesis of cell wall components in mycobacteria, which include the bacteria causing tuberculosis.
  • - Researchers synthesized and tested 15 new compounds targeting DprE1, with two compounds (BOK-2 and BOK-3) showing promising inhibition at low concentrations (IC values of 2.2 and 3.0 μM, respectively).
  • - The research utilized molecular modeling to understand how these compounds interact with DprE1, paving the way for potential new treatments for tuberculosis through targeted drug design.
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HER2 receptors, overexpressed in certain human cancers, have drawn significant attention in cancer research due to their correlation with poor survival rates. Researchers have developed monoclonal antibodies like Trastuzumab and Pertuzumab against HER2 receptors, which have proven highly beneficial in cancer therapy. Bispecific antibodies like Zanidatamab and antibody-drug conjugates like T-DM1 have been developed to overcome the resistance associated with monotherapy.

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Breast cancer has been a leading cause of mortality among women worldwide in recent years. Targeting the lysophosphatidic acid (LPA)-LPA pathway using small molecules could improve breast cancer therapy. Thiazolidin-4-ones were developed and tested on MCF-7 cancer cells, and active compounds were analyzed for their effects on apoptosis, migration angiogenesis and LPA protein and gene expression.

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Mycobacterium tuberculosis (Mtb) has numerous cell wall and non-cell wall mediated receptors for drug action, of which cell wall mediated targets were found to be more promising because of their pivotal role in bacterial protection and survival. Herein, we reported the design and synthesis of a series of pyrazole-linked triazoles based on the reported structural features of promising drug candidates that target DprE1 receptors through a Structure-based drug design (SBDD) approach (6a-6j and 7a-7j). The synthesized compounds were evaluated for their in-vitro antitubercular activity against virulent strains of Mtb H37Rv.

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