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Structure-Activity Relationship Study on Col-003, a Protein-Protein Interaction Inhibitor Between Collagen and Hsp47

Structure-Activity Relationship Study on Col-003, a Protein-Protein Interaction Inhibitor Between Collagen and Hsp47

Masahito Yoshida, Masazumi Saito, Shinya Ito, Koji Ogawa, Naoki Goshima, Kazuhiro Nagata, Takayuki Doi

Chem Pharm Bull (Tokyo). 2020 Mar 1;68(3):220-226.

PMID: 31582590

Abstract:

This study demonstrates the structure-activity relationship of Col-003, a potent collagen-heat-shock protein 47 (Hsp47) interaction inhibitor. Col-003 analogues were successfully synthesized by Pd(0)-catalyzed cross-coupling reactions of 5-bromosalicylaldehyde derivatives with alkyl-metal species, and the inhibitory activities of the synthetic analogues were evaluated using surface plasmon resonance analysis (BIAcore). We succeeded in discovering two potent inhibitors that showed 85 and 81% inhibition at a concentration of 1.9 µM against the collagen-Hsp47 interaction. This indicates that elongation of an alkyl linker between two aromatic rings could considerably improve inhibitory activity due to the adjustment of a pendant phenyl moiety to an appropriate position, in addition to the hydrophobic interaction with an alkyl linker moiety.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP328565168	Col003		328565-16-8	Price

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