G9a is a lysine methyltransferase (KMT) involved in epigenetic gene regulation by covalent modification of histones. It catalyses the transfer of methyl groups from S-adenosyl methionine (SAM) to lysine residues on histone proteins (Fig 1). Literature supports the role of G9a in mechanisms of carcinogenesis, making it an attractive oncology target.1-4 Domainex has solved the key technical drug discovery challenges associated with KMTs, including generating a number of proprietary crystal structures, assays and a novel screening library of small molecule inhibitors.
Drug Discovery Case Studies
Auspherix and Domainex worked together to develop a novel class of gold(I) antibiotics, with a broad spectrum antibacterial activity against the so-called ESKAPE pathogens.
Domainex has generated crystal structures, assays and a chemical library for lysine methyltransferases (KMTs), which are involved in epigenetic gene regulation
Domainex's lead programme targets key kinases (TBK1/IKKe) that have been validated as novel drug targets in inflammatory diseases such as psoriasis, rheumatoid arthritis, COPD
Using CDH technology, Domainex worked with UCB to develop the crystal structure of Mitogenactivated protein kinase kinase (MAPKK, MEK) for use in drug discovery.
Medicinal Chemists at Domainex collaborated with university researchers to develop novel inhibitors of a protease target, a potential treatment for asthma.
Using a peptidomimetic approach, Ark Therapeutics and Domainex have developed inhibitors of protein-protein interactions PPI targeting the NRP1 function.