Wilding, Birgit published the artcileInvestigating the phosphinic acid tripeptide mimetic DG013A as a tool compound inhibitor of the M1-aminopeptidase ERAP1, Quality Control of 343338-28-3, the main research area is phosphinic acid tripeptide mimetic enantioselective synthesis inhibitor aminopeptidase ERAP1; peptidomimetic phosphinic acid library synthesis tool probe; chirality condensation protection phospha Michael addition epimerization resolution; enzyme inhibitor structure activity drug discovery target permeability; ERAP1 DG013A bound crystal structure mol docking antitumor agent; Chemical probe; DG013A; ERAP1; M1-aminopeptidase; Permeability.
ERAP1 is a zinc-dependent M1-aminopeptidase that trims lipophilic amino acids from the N-terminus of peptides. Owing to its importance in the processing of antigens and regulation of the adaptive immune response, dysregulation of the highly polymorphic ERAP1 has been implicated in autoimmune disease and cancer. To test this hypothesis and establish the role of ERAP1 in these disease areas, high affinity, cell permeable and selective chem. probes are essential. DG013A 1, is a phosphinic acid tripeptide mimetic inhibitor with reported low nanomolar affinity for ERAP1. However, this chemotype is a privileged structure for binding to various metal-dependent peptidases and contains a highly charged phosphinic acid moiety, so it was unclear whether it would display the high selectivity and passive permeability required for a chem. probe. Therefore, we designed a new stereoselective route to synthesize a library of DG013A 1 analogs to determine the suitability of this compound as a cellular chem. probe to validate ERAP1 as a drug discovery target.
Bioorganic & Medicinal Chemistry Letters published new progress about (Benzyloxy)carbonyl group. 343338-28-3 belongs to class amides-buliding-blocks, name is (S)-2-Methylpropane-2-sulfinamide, and the molecular formula is C4H11NOS, Quality Control of 343338-28-3.
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