Diethyl-pythiDC (diethyl pythiDC) is a selective, small molecule inhibitor of P4HA1, inhibits collagen biosynthesis in breast cancer cells.
diethyl-pythiDC decreased levels of AGO2 in CRC cells, also reduced the malignant phenotypes of CRC cells, including cell proliferation, colony formation, invasion and spheroid-forming capacity.
diethyl-pythiDC (100 mg/kg) reduced growth in a CRC PDX model through the P4HA1 downstream targets, MMP1 and AGO2.
The prolyl-4-hydroxylase enzymes prolyl 4-hydroxylase, alpha polypeptide I (P4HA1), P4HA2, and P4HB are necessary for collagen synthesis and deposition; matrix metalloproteinases degrade collagen, P4HA1 catalyzes the formation of 4-hydroxyproline from proline residues, a process that is essential for the proper folding of collagen polypeptide chains into stable triple-helical molecules.
