《Stapled peptide targeting the CDK4/Cyclin D interface combined with Abemaciclib inhibits KRAS mutant lung cancer growth》 was written by Bouclier, Celine; Simon, Matthieu; Laconde, Guillaume; Pellerano, Morgan; Diot, Sebastien; Lantuejoul, Sylvie; Busser, Benoit; Vanwonterghem, Laetitia; Vollaire, Julien; Josserand, Veronique; Legrand, Baptiste; Coll, Jean-Luc; Amblard, Muriel; Hurbin, Amandine; Morris, May C.. Category: chlorides-buliding-blocks And the article was included in Theranostics in 2020. The article conveys some information:
CDK4/cyclin D kinase constitutes an attractive pharmacol. target for development of anticancer therapeutics, in particular in KRAS-mutant lung cancer patients, who have a poor prognosis and no targeted therapy available yet. Although several ATP-competitive inhibitors of CDK4 have been developed for anticancer therapeutics, they suffer from limited specificity and efficacy. As an alternative to ATP-competitive inhibitors we have designed a stapled peptide to target the main interface between CDK4 and cyclin D, and have characterized its physico-chem. properties and affinity to bind cyclin D1. We have validated a pos. correlation between CDK4/cyclin D level and KRAS mutation in lung cancer patients. The stapled peptide enters cells rapidly and efficiently, and inhibits CDK4 kinase activity and proliferation in lung cancer cells. Its intrapulmonary administration in mice enables its retention in orthotopic lung tumors and complete inhibition of their growth when co-administered with Abemaciclib. The stapled peptide targeting the main interface between CDK4 and cyclin D provides promising therapeutic perspectives for patients with lung cancer. The results came from multiple reactions, including the reaction of Benzylidenebis(tricyclohexylphosphine)dichlororuthenium(cas: 172222-30-9Category: chlorides-buliding-blocks)
Benzylidenebis(tricyclohexylphosphine)dichlororuthenium(cas: 172222-30-9) is the first metathesis catalyst to be widely used in organic synthesis. It is useful for acyclic diene metathesis polymerization (ADMET), Ring-Opening Metathesis Polymerization (ROMP) of strained cyclic olefins, ring opening metathesis (ROM), and so on.Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics