Targeting a novel KRAS binding site: Application of one-component stapling of small (5-6-mer) peptides was written by Fumagalli, Gabriele;Carbajo, Rodrigo J.;Nissink, J. Willem M.;Tart, Jonathan;Dou, Rongxuan;Thomas, Andrew P.;Spring, David R.. And the article was included in Journal of Medicinal Chemistry in 2021.Electric Literature of C21H21NO4 The following contents are mentioned in the article:
RAS proteins are central in the proliferation of many types of cancer, but a general approach toward the identification of pan-mutant RAS inhibitors has remained unresolved. In this work, we describe the application of a binding pharmacophore identified from anal. of known RAS binding peptides to the design of novel peptides. Using a chem. divergent approach, we generated a library of small stapled peptides from which we identified compounds with weak binding activity. Exploration of structure-activity relationships (SARs) and optimization of these early compounds led to low-micromolar binders of KRAS that block nucleotide exchange. This study involved multiple reactions and reactants, such as (S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5Electric Literature of C21H21NO4).
(S)-1-(((9H-Fluoren-9-yl)methoxy)carbonyl)piperidine-2-carboxylic acid (cas: 86069-86-5) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Electric Literature of C21H21NO4
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem