NMT1 (N-myristoyltransferase 1)

Class

Small molecule myristoylation inhibitor (first-in-class)

Pathway

Blocks protein N-myristoylation, disrupting membrane association of proteins required for pro-survival signaling, proliferation, and angiogenesis

N-myristoyltransferase 1 (NMT1) is an enzyme that attaches a fatty acid called myristate onto the beginning of certain proteins, a modification known as N-myristoylation. This chemical tag anchors those proteins to cell membranes, which is often required for them to transmit signals properly. Many of the proteins that depend on this modification participate in pathways that drive cell survival, proliferation, and the formation of new blood vessels (angiogenesis) — processes that are frequently hijacked in cancer. By blocking NMT1, a small molecule can prevent these client proteins from reaching the membrane, dampening the signaling networks that support tumor growth and blood supply. Because myristoylation affects a broad set of proteins rather than a single pathway, inhibiting NMT1 represents a strategy aimed at disrupting multiple pro-tumorigenic processes simultaneously, rather than targeting one specific mutated driver. This mechanism is being explored primarily in oncology, where uncontrolled proliferation and angiogenesis are central features of disease progression. As a first-in-class approach, NMT1 inhibition is conceptually distinct from kinase or receptor-targeted therapies, since it acts further upstream on a shared protein-modification step rather than on a single receptor or enzyme active site.