Preferred Label : Lenumlostat;
NCIt synonyms : Lysyl Oxidase-like Protein 2 Inhibitor PAT-1251; LOXL2 Inhibitor GB2064;
NCIt definition : An orally available, small-molecule, irreversible inhibitor of lysyl oxidase homolog
2 (lysyl oxidase-like protein 2; LOXL2) with potential antifibrotic activity. Upon
oral administration, the aminomethyl pyridine moiety of lenumlostat interacts with
the active site of LOXL2 to form a pseudo-irreversible inhibitory complex, thereby
inhibiting the catalytic activity of LOXL2. LOXL2, a secreted glycoprotein, catalyzes
the post-translational oxidative deamination of lysine residues on target proteins,
including collagen and elastin, leading to the formation of deaminated lysine (allysine).
Condensation with other allysines or lysines drives the formation of inter- and intramolecular
cross-linkages that impact remodeling of the extracellular matrix (ECM), potentially
leading to fibrosis. Inhibition of LOXL2, which is often upregulated in fibrotic tissue,
may reduce fibrosis in certain chronic fibrotic diseases.;
UNII : Y3HMF6G24B;
CAS number : 2098884-52-5;
Molecule name : PAT-1251; PAT 1251; GB 2064; GB-2064;
NCI Metathesaurus CUI : CL969613;
Origin ID : C160691;
UMLS CUI : C5205467;
Semantic type(s)
- concept_is_in_subset
- has_target
