ABSTRACT

Collagenases (especially MMP-1, MMP-8, and MMP-13) play crucial roles in several diseases, such as cancer, arthritis, periodontal disease, and cardiovascular disease.

Considering their implication in various disease conditions, collagenases can be regarded as promising biomolecular targets for designing effective collagenase inhibitors. Depending on different crystallographic data and existing collagenase inhibitors, ligand- and structure-based drug design (LBDD and SBDD) methodologies can be applied to designing and discovering new collagenase inhibitors. In this chapter, various drug-designing approaches conducted on existing collagenase inhibitors are discussed in detail. Applying these LBDD and SBDD methodologies to collagenase inhibitors may unveil novel collagenase inhibitors.