PF00349412 is a selective inhibitor of protozoan protein N-myristoyltransferases. Inhibition of N-myristoyltransferase has been validated pre-clin. as a target for the treatment of fungal and trypanosome infections, using species-specific inhibitors.
Myristoyl coenzyme A (myristoyl-CoA) is a derivative of CoA that contains the long-chain fatty acid myristic acid . It is a substrate for N-myristoyltransferase during myristoylation, a process that adds a myristoyl group to proteins either during translation to modify protein activity or post-translationally in apoptotic cells. It is also a substrate in the de novo synthesis of phosphatidylinositol .
FTR1335 is a CaNMT inhibitor (IC50 = 0.49 nM) with good fungal selectivity. CaNMT inhibitors are fungicidal and show antifungal activity against Candida (especially fluconazole-resistant strains). They function by inhibiting N-myristoyltransferase (NMT), which catalyzes the transfer of a C14 fatty acif from myristoyl-CoA to the N-terminal of glycine in many fungal proteins. Without this process, fungi can die. This process also occurs in humans, and as such selectivity is an important characteristic of these drugs.
Myristoyl coenzyme A lithium 为含锂标记的 Myristoyl coenzyme A (CoA),关键参与病毒生物学中N-肉豆蔻酰转移酶 (NMT) 控制的肉豆蔻酰化过程。NMT 在结肠上皮肿瘤细胞中相较正常细胞展现出更高的活性。已知,还原形态的 CoA 是调控 NMT 活性的主要因素,反之氧化态的 CoA 则抑制 NMT 促进的肉豆蔻酰化。因此,Myristoyl coenzyme A 表现出通过阻断肉豆蔻酰化过程的潜在抗癌和抗病毒作用。