https://pubmed.ncbi.nlm.nih.gov/38116436
This study describes the development of HDAC degraders using hydrophobic tagging technology, resulting in a compound that significantly decreases HDAC1 levels in multiple myeloma cells.
https://pubmed.ncbi.nlm.nih.gov/38116436
This study describes the development of HDAC degraders using hydrophobic tagging technology, resulting in a compound that significantly decreases HDAC1 levels in multiple myeloma cells.
https://pubmed.ncbi.nlm.nih.gov/38116435
The abstract reports the repurposing of the azole antifungal Clotrimazole as a potential treatment for drug-resistant tuberculosis, showing equipotent activity against the Mtb H37Rv strain compared to Linezolid, but with significantly less inhibition of monoamine oxidase (MAO) enzymes, suggesting a reduced serotonergic toxicity burden.
https://pubmed.ncbi.nlm.nih.gov/38116434
Researchers have identified inhibitory peptides that suppress the formation of toxic fibrils in mutant Huntingtin proteins associated with Huntington’s disease, providing a potential therapeutic lead for further optimization and development.
https://pubmed.ncbi.nlm.nih.gov/38116433
A 6-methyl modification on certain antifolate drugs, like pemetrexed, abolishes transport by the ubiquitous RFC while preserving antitumor efficacy and selectivity for tumor-selective transporters, suggesting a promising approach for tumor-targeted therapeutics.
https://pubmed.ncbi.nlm.nih.gov/38116432
The MAIP antimalarial prediction platform, when combined with a robust compound selection workflow and high-throughput screening cascade, identified eight novel, druglike molecules with good potency and ADME profiles from a public library.
https://pubmed.ncbi.nlm.nih.gov/38116430
The abstract reports the discovery and characterization of a kinase inhibitor, CZC-54252, and its 39 analogues that show nanomolar inhibition against five Plasmodium falciparum kinases, with eight submicromolar inhibitors demonstrating potent antiplasmodial activity.
https://pubmed.ncbi.nlm.nih.gov/38116429
Scientists have created and tested bioconjugates of melanostatin and amantadine that positively allosterically modulate human dopamine D2 receptors, with some showing mild toxicity at high concentrations.
https://pubmed.ncbi.nlm.nih.gov/38116428
Synthetic silicon-incorporated cannabinoids show promising inhibition of heme-induced NLRP3 inflammasome, offering potential for treatment of inflammatory diseases like sickle cell anemia and thalassemia.
https://pubmed.ncbi.nlm.nih.gov/38116427
Scientists have developed conformationally restricted negamycin derivatives, TCP-304 and TCP-306, that show potent readthrough activity for TGA and TAG mutations in Duchenne muscular dystrophy.