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A peptidomimetic is a small protein-like chain designed to mimic a peptide. [ 1 ] [ 2 ] They typically arise either from modification of an existing peptide, or by designing similar systems that mimic peptides, such as peptoids and β-peptides .
Peptidomimetic foldamers are synthetic molecules that mimic the structure of proteins, while nucleotidomimetic foldamers are based on the interactions in nucleic acids. Abiotic foldamers are stabilized by aromatic and charge-transfer interactions which are not generally found in nature. [ 2 ]
The first HIV protease inhibitor, saquinavir, is a peptidomimetic hydroxyethylamine [6] and was marketed in 1995. [18] It is a transition state analogue of a native substrate of the protease. [6] The observation that HIV-1 protease cleaves the sequences containing the dipeptides Tyr-Pro or Phe-Pro was the basic design criterion. [19]
Prohibitin-targeting peptide 1 (also known as prohibitin-TP01 and TP01; trade name Adipotide) is a peptidomimetic with sequence CKGGRAKDC-GG-D (KLAKLAK) 2.It is an experimental proapoptotic drug [1] that has been shown to cause rapid weight loss in mice [2] and rhesus monkeys. [3]
There are a number of different distinct classes of protein mimetics. Antibody mimetic - Molecules that mimic antigen binding activity of antibodies; Peptidomimetic - Small protein-like chains designed to mimic larger peptide.
A stapled peptide is a modified peptide (class A peptidomimetic), typically in an alpha-helical conformation, [2] that is constrained by a synthetic brace ("staple"). [3] The staple is formed by a covalent linkage between two amino acid side-chains, forming a peptide macrocycle. Staples, generally speaking, refer to a covalent linkage of two ...
Murepavadin also known as POL7080 is a Pseudomonas specific peptidomimetic antibiotic. [1] It is a synthetic cyclic beta hairpin peptidomimetic based on the cationic antimicrobial peptide protegrin I (PG-1) and the first example of an outer membrane protein-targeting antibiotic class with a novel, nonlytic mechanism of action, highly active and selective against the protein transporter LptD of ...
GGTI-297 is a potent, cell-permeable, and selective peptidomimetic inhibitor of GGTase I compared to farnesyltransferase (FTase). L-744,832 Dihydrochloride: sc-221800: L-744,832 Dihydrochloride is a Ras farnesyltransferase and p70 S6 kinase inhibitor. L-744,832 Dihydrochloride has been shown to induce tumor regression and apoptosis.