LOX Inhibitor CCT365623 Small Molecule (Tool Compound)
Invented by Leo Leung , Caroline Springer
Invented at Cancer Research UK Manchester Institute
- References (1)
- Inventor Info
|Antigen/Gene or Protein Targets
|LOX, protein-6-lysine oxidase
Lysyl oxidase (LOX) and its family members LOX-like (LOXL) are copper-dependent amine oxidases that covalently cross-link collagens and elastin in the tumor extracellular matrix. LOX is secreted as a catalytically inactive 50 kDa pro-protein, which is cleaved to an active 32 kDa enzyme by proteases such as procollagen C-proteinase. LOX and LOXL have variable N-termini, and share a highly conserved C-terminus, where the catalytic domain is located. The catalytic site comprises a copper binding motif and a covalently bound lysine tyrosylquinone (LTQ) cofactor, where peptidyl lysine residues (H2NCH2R) are converted to the corresponding α-aminoadipic-δ-semialdehyde (O=CHR) in an oxidative deamination reaction. The newly formed aldehyde residues undergo spontaneous cross-linking with adjacent nucleophilic functionalities, leading to the insoluble extracellular protein matrices.
LOX and LOXL2 have important roles in promoting tumor growth in many types of cancer. In particular, LOX has been demonstrated to be a critical mediator of cancer metastasis. Therapeutic agents targeting the activity of LOX are thus proposed as cancer treatments, especially against metastasis where no effective therapeutic methods are currently available.
|On Target IC50
|Patent Application Number WO 2017/141049 A1
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