The first targeted inhibitors of an essential M. tuberculosis cell wall lipase, Rv3802c, are described. Lead compounds exhibited nanomolar inhibition of the enzyme, and encouraging antibacterial activity against M. tuberculosis in vitro, supporting Rv3802c as a novel TB drug target.
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http://dx.doi.org/10.1039/c0cc05635a | DOI Listing |
Ecotoxicology
January 2025
Amity Institute of Environmental Sciences, Amity University, Sector-125, Noida, 201301, Uttar Pradesh, India.
As the global population continues to grow, the use of pesticides to increase food production is projected to escalate. Pesticides are critical in plant protection, offering a powerful defense against fungal diseases such as apple scab, leaf spot, sclerotinia rot, damping off, sheath blight, and root rot, which threaten crops like cereals, corn, cotton, soybean, sugarcane, tuberous vegetables, and ornamentals. Succinate Dehydrogenase Inhibitor (SDHI) fungicides represent a novel class essential for controlling fungal pathogens and bolstering food security.
View Article and Find Full Text PDFCell Biochem Biophys
January 2025
Division of Biomedical and Life Sciences, School of Science, Navrachana University, Vadodara, Gujarat, India.
Cancer Stem Cells (CSCs) play an important role in the development, resistance, and recurrence of many malignancies. These subpopulations of tumor cells have the potential to self-renew, differentiate, and resist conventional therapy, highlighting their importance in cancer etiology. This review explores the regulatory mechanisms of CSCs in breast, cervical, and lung cancers, highlighting their plasticity, self-renewal, and differentiation capabilities.
View Article and Find Full Text PDFSci Rep
January 2025
Department of Biophysics and Pharmacology, Bioscience Center, Federal University of Rio Grande do Norte, Natal, 59064-741, RN, Brazil.
The COVID-19 pandemic caused by SARS-CoV-2 continues to pose a major challenge to global health. Targeting the main protease of the virus (Mpro), which is essential for viral replication and transcription, offers a promising approach for therapeutic intervention. In this study, advanced computational techniques such as molecular docking and molecular dynamics simulations were used to screen a series of antiviral compounds for their potential inhibitory effect on the SARS-CoV-2 Mpro.
View Article and Find Full Text PDFNPJ Antimicrob Resist
March 2024
Sanford Burnham Prebys Medical Discovery Institute, La Jolla, CA, USA.
Comprehensive knowledge of mechanisms driving the acquisition of antimicrobial resistance is essential for the development of new drugs with minimized resistibility. To gain this knowledge, we combine experimental evolution in a continuous culturing device, the morbidostat, with whole genome sequencing of evolving cultures followed by characterization of drug-resistant isolates. Here, this approach was used to assess evolutionary dynamics of resistance acquisition against DNA gyrase/topoisomerase TriBE inhibitor GP6 in Escherichia coli and Acinetobacter baumannii.
View Article and Find Full Text PDFAdv Protein Chem Struct Biol
January 2025
Laboratory of Integrative Genomics, Department of Integrative Biology, School of BioSciences and Technology, Vellore Institute of Technology (VIT), Vellore, Tamil Nadu, India. Electronic address:
The prognosis for mixed-lineage leukemia (MLL), particularly in young children, remains a significant health concern due to the limited therapeutic options available. MLL refers to KMT2A chromosomal translocations that produce MLL fusion proteins. The protein menin, which is essential for the malignant potential of these MLL fusion proteins, offers novel targets for acute leukemia treatment.
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