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N-myristoyltransferase inhibitors are small molecules that target and inhibit N-myristoyltransferases, which block the addition of myristic acid to the penultimate glycine of proteins with myristoylation signal. The prototype is the DDD85646, [1] and the analogues IMP-1088 and zelenirstat (PCLX-001).
Myristic acid (IUPAC name: tetradecanoic acid) is a common saturated fatty acid with the molecular formula CH 3 (CH 2) 12 COOH. Its salts and esters are commonly referred to as myristates or tetradecanoates. The name of the acyl group derived from myristic acid is myristoyl or tetradecanoyl.
Zelenirstat is a strong pan-N myristoyl transferase inhibitor, which prevents addition of myristic acid into penultimate glycine of protein with myristoylation signal, and initially has been introduced as anti-tumor drug. [1] [2] [3] It has completed phase I clinical trial and is going through escalation phase. [4]
Nonanoic acid CH 3 (CH 2) 7 COOH C9:0 Capric acid: Decanoic acid CH 3 (CH 2) 8 COOH C10:0 Undecylic acid: Undecanoic acid CH 3 (CH 2) 9 COOH C11:0 Lauric acid: Dodecanoic acid CH 3 (CH 2) 10 COOH C12:0 Tridecylic acid: Tridecanoic acid CH 3 (CH 2) 11 COOH C13:0 Myristic acid: Tetradecanoic acid CH 3 (CH 2) 12 COOH C14:0 Pentadecylic acid ...
Myristoylation is a lipidation modification where a myristoyl group, derived from myristic acid, is covalently attached by an amide bond to the alpha-amino group of an N-terminal glycine residue. [1] Myristic acid is a 14-carbon saturated fatty acid (14:0) with the systematic name of n-tetradecanoic acid.
1-Tetradecanol may be prepared by the hydrogenation of myristic acid (or its esters); myristic acid itself can be found in nutmeg (from where it gains its name) but is also present in palm kernel oil and coconut oil and it is from these that the majority of 1-tetradecanol is produced. [3]
Lauric and myristic acids have melting points relatively close to human body temperature, so babassu oil can be applied to the skin as a solid that melts on contact. This heat transfer can produce a cooling sensation. It is an effective emollient.
Myristyl aldehyde, also known as tetradecanal, is a reduced form of myristic acid. It is naturally produced by bioluminescent bacteria of the Vibrio genus and is one of two substrates produced and consumed by the Vibrio fischeri luciferase light emission system.