NMT Inhibitors

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Overview Many proteins involved in a wide variety of signalling, including cellular transformation and oncogenesis, are myristoylated by N-Myristoyltransferase (NMT), ubiquitously distributed eukaryotic enzyme. NMT has been proposed as a therapeutic target in cancer among other indications. A team at Imperial College including ex-pharma medicinal chemist has built a industry-level drug discovery program and created a catalogue of subnanomolar novel small molecule inhibitors NMT.   Key Features Selective NMT inhibition leads to dose-responsive loss of Nmyristoylation on more than 100 protein targets in cells, and cytotoxicity in cancer cells. NMT inhibition leads to apoptosis following or concurrent with accumulation in the G1 phase. Well understood SAR + crystal structures with inhibitors bound. NMT inhibitors demonstrate synergistic anti-proliferative effects with existing oncology drugs in various cancer cell lines.   Development Stage This project  is currently focusing on mode of actions through which NMT inhibitors work to highlight specific types of cancer in which NMT inhibitors therapy might show the best efficacy. First indication includes blood cancers where monotherapy shows some promise. Team is also exploring combinational therapy where dual action of NMT inhibitors other oncology drugs synergise in pathways.   Intellectual Property IP package includes composition of matter and use in multiple indications protected by international patent application.