Heat stress inducible cytoplasmic isoform of ClpB1 from Z. nummularia exhibits enhanced thermotolerance in transgenic tobacco

Molecular Biology Reports - Previously, we isolated CDS of Ziziphus nummularia isoform ZnJClpB1-C from heat stress-tolerant genotype Jaisalmer. To further functionally validate ZnJClpB1-C assumed...     

Discovery of thiazolyl-phthalazinone acetamides as potent glucose uptake activators via high-throughput screening

With the aim to discover orally active small molecules that stimulate glucose uptake, high throughput screening of a library of 5000 drug-like compounds was conducted in differentiated skeletal muscle cells in presence of insulin. N-Substituted phthalazinone acetamide was identified as a potential glucose uptake modulator. Several novel derivatives were synthesized to establish structure activity relationships. Identified lead thiazolyl-phthalazinone acetamide (7114863) increased glucose uptake (EC₅₀ of 0.07 ± 0.02 μM) in differentiated skeletal muscle cells in presence of insulin. Furthermore, 7114863 was superior to rosiglitazone under similar experimental conditions without inducing PPAR-γ agonist activity thus making it a very interesting scaffold.