Matthew, Susan; Chen, Qi-Yin; Ratnayake, Ranjala; Fermaintt, Charles S.; Lucena-Agell, Daniel; Bonato, Francesca; Prota, Andrea E.; Lim, Seok Ting; Wang, Xiaomeng; Diaz, J. Fernando; Risinger, April L.; Paul, Valerie J.; Oliva, Maria Angela; Luesch, Hendrik published the artcile< Gatorbulin-1, a distinct cyclodepsipeptide chemotype, targets a seventh tubulin pharmacological site>, Product Details of C19H16O, the main research area is natural product marine cyanobacterium cyclodepsipeptide Gatorbulin1 total synthesis; antitumor agent tubulin targeted chemotherapy microtubule drug mechanism action; GB1 total synthesis esterification protection peptide coupling macrolactamization reduction; crystal structure tubulin CB1 complex NMR conformer chelation fluorescence; cyanobacteria; marine natural product; microtubules; total synthesis; tubulin.
Tubulin-targeted chemotherapy has proven to be a successful and wide spectrum strategy against solid and liquid malignancies. Therefore, new ways to modulate this essential protein could lead to new antitumoral pharmacol. approaches. Currently known tubulin agents bind to six distinct sites at α/β-tubulin either promoting microtubule stabilization or depolymerization We have discovered a seventh binding site at the tubulin intradimer interface where a novel microtubule-destabilizing cyclodepsipeptide, termed gatorbulin-1 (GB1), binds. GB1 has a unique chemotype produced by a marine cyanobacterium. We have elucidated this dual chem. and mechanistic novelty through multidimensional characterization, starting with bioactivity-guided natural product isolation and multinuclei NMR-based structure determination, revealing the modified pentapeptide with a functionally critical hydroxamate group. and validation by total synthesis. The modified pentapeptide was validated by total synthesis. We have investigated the pharmacol. using isogenic cancer cell screening, cellular profiling, and complementary phenotypic assays, and unveiled the underlying mol. mechanism by in vitro biochem. studies and high-resolution structural determination of the α/β-tubulin-GB1 complex.
Proceedings of the National Academy of Sciences of the United States of America published new progress about (Fluorenylmethoxy)carbonyl group. 76-84-6 belongs to class alcohols-buliding-blocks, and the molecular formula is C19H16O, Product Details of C19H16O.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts