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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 .
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.
[7] [8] The largest groups of peptidomimetic consist of β-peptides, γ-peptides and δ-peptides, and the possible monomeric combinations. [8] The amino acids of these peptides only differ by one (β), two (γ), or three (δ) methylene carbons, yet the structural changes were profound. These peptide sequences are highly studied as sequence ...
Peptoids (root from the Greek πεπτός, peptós "digested"; derived from πέσσειν, péssein "to digest" and the Greek-derived suffix -oid meaning "like, like that of, thing like a _____," ), or poly-N-substituted glycines, are a class of biochemicals known as biomimetics that replicate the behavior of biological molecules. [1]
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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 ...
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]