Calcium pentosan polysulfate directly inhibits enzymatic activity of ADAMTS4 (aggrecanase-1) in osteoarthritic chondrocytes

Takizawa M, Yatabe T, Okada A, Chijiiwa M, Mochizuki S, Ghosh P, Okada Y · FEBS Letters

Calcium PPS blocked ADAMTS4's aggrecan-cutting activity in human OA chondrocytes without changing how much of the enzyme the cells made, and peptide-competition mapping placed the binding on the enzyme's C-terminal ancillary domain rather than its active site.

Population

Chondrocytes isolated from human osteoarthritic cartilage, stimulated with interleukin-1α

Intervention

Calcium PPS

Comparator

Untreated stimulated chondrocytes

Limitations

Isolated cells from surgical specimens; PPS's developer is a co-author; inhibition of one aggrecanase in culture does not establish that aggrecan is preserved in a living joint.