Identification of a new p53/MDM2 inhibitor motif inspired by studies of chlorofusin was written by Cominetti, Marco M. D.;Goffin, Sarah A.;Raffel, Ewan;Turner, Kerrie D.;Ramoutar, Jordann C.;O’Connell, Maria A.;Howell, Lesley A.;Searcey, Mark. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2015.Related Products of 313648-56-5 This article mentions the following:
Previous studies on the natural product chlorofusin have shown that the full peptide and azaphilone structure are required for inhibition of the interaction between MDM2 and p53. In the current work, the authors utilized the cyclic peptide as a template and introduced an azidonorvaline amino acid in place of the ornithine/azaphilone of the natural product and carried out click chem. with the resulting peptide. From this small library the first ever non-azaphilone containing chlorofusin analog with MDM2/p53 activity was identified. Further studies then suggested that the simple structure of the Fmoc-norvaline amino acid that had undergone a click reaction was also able to inhibit MDM2/p53 interaction. This is an example where studies of a natural product have led to the serendipitous identification of a new small mol. inhibitor of a protein-protein interaction. In the experiment, the researchers used many compounds, for example, Dimethyl 5-ethynylisophthalate (cas: 313648-56-5Related Products of 313648-56-5).
Dimethyl 5-ethynylisophthalate (cas: 313648-56-5) belongs to esters. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Polyesters are important plastics, with monomers linked by ester moieties. Many esters have the potential for conformational isomerism, but they tend to adopt an s-cis (or Z) conformation rather than the s-trans (or E) alternative, due to a combination of hyperconjugation and dipole minimization effects. The preference for the Z conformation is influenced by the nature of the substituents and solvent, if present. Lactones with small rings are restricted to the s-trans (i.e. E) conformation due to their cyclic structure.Related Products of 313648-56-5
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics