Central Drug Research Institute

Silencing of E6/E7 proteins of HPV-16 in the CaCx cell line upregulate the expression of POTE-Paralogs

POTE proteins are known to be expressed in tissues such as normal prostate, placenta, ovary, testis, and embryo, and are collectively referred to as POTE-family proteins based on this organ-specific expression. The POTE gene spans 32 kb on chromosome 21q11.2, although its homolog...

Design, Synthesis and Dual-Stage Antimalarial Evaluation of β-Carboline−Metronidazole Hybrids: Structure−Activity Relationship and Molecular Docking Correlations

Abstract Malaria remains a major global health challenge, exacerbated by emerging drug-resistant Plasmodium strains. Herein, we report the design, synthesis, and dual-stage antimalarial evaluation of β-carboline−metronidazole hybrids. The synthesized hybrids, linked through ester...

β-Sheet Antimicrobial and Antimycobacterial Peptides with a High Therapeutic Index by Employing the Repeats of a 5-Mer Segment of α-Helical Cytolytic Melittin

Abstract Despite strong antimicrobial activity, high haemolytic/cytotoxic properties, associated with its non-cell-selective membrane-lytic property and its large size prohibits considering bee-venom, α-helical, 26-residue, melittin as a lead molecule for antimicrobial-drug devel...

Dopamine alters macrophage metabolism promoting intracellular Mycobacterium tuberculosis survival

Dopamine (DA) is thought to aggravate progress of bacterial infections and enhance risk of intracellular bacterial infection like tuberculosis (TB). Though TB patients are known to present with high dopamine levels the causal link between them has remained unexplored. Mycobacteri...

Uracil-Thianthrenium Salts (Uracil-TT+BF4–) as a Coupling Partner in Sonogashira Cross-Coupling Reactions: Access to 5-Alkynyl Uracils and Synthetic Applications

Abstract Cross-coupling reactions are powerful tools for forging two different organic fragments via formation of C–C or C–heteroatom bonds. Herein, we for the first time synthesize a bench-stable cross-coupling reagent, uracil-TT+BF4–, for Sonogashira-type reaction to install an...

TKL3 regulates blood-stage fitness, male gamete fertility, and transmission-stage development in Plasmodium berghei

Malaria parasites must undergo complex developmental transitions to complete their life cycle and transmit between vertebrate and mosquito hosts. These transitions are tightly regulated by protein phosphorylation events, yet the specific kinases involved remain poorly characteriz...

A Small Molecule Substrate Mimic to Inhibit Bacterial Hsp70 Chaperone Function

Given the rapid spread of antibiotic resistance worldwide, it is imperative to develop new strategies against pathogenic bacteria. Here, we report a small‐molecule inhibitor of bacterial heat shock protein 70 (Hsp70), called DnaK, a central component of the bacterial protein chap...

miR-451a is a differentially expressed blood-based microRNA in newly diagnosed CML identified by high-throughput profiling

Abstract Background microRNAs (miRNAs) are emerging as promising biomarkers in hematological malignancies due to their stability in blood. This study aimed to investigate the differential expression of miRNAs in chronic myeloid leukemia (CML) and evaluate the potential of miR-451...