Table 3. IC50 Values (μM) for Inhibition of Aggrecanases by Synthetic Peptidesa.
| peptide | parental sequence | ADAMTS4 | ADAMTS5 | ref |
|---|---|---|---|---|
| 521GGWGPWGPWGD531 | ADAMTS4 | 17b | ND | (140) |
| 521GGWGPWGPWGDCSRTCGGG539 | ADAMTS4 | 3b | ND | (140) |
| 533SRTCGGGVQFSSRDCTRPV551 | ADAMTS4 | 70b | ND | (140) |
| 555GGKYCEGRRTRFSCNTEDCP575 | ADAMTS4 | 38b | ND | (140) |
| Ac-NEFRQRETYMVF-NH2 | NA | 35c | ND | (141) |
| Ac-DVQEFRGVTAVIR-NH2 | NA | 35c | ND | (141) |
| Ac-DVQ(dE)FRGVTAVIR | NA | 10c | ND | (141) |
| KHN(dE)FRQRETYMVFKGK | NA | 8c | ND | (141) |
| CASESLC linear | TIMP3 | (74) | ND | (142) |
| CASESLC cyclic | TIMP3 | (25) | ND | (142) |
| CTEASESLAGC linear | TIMP3 | (120) | ND | (142) |
| CTEASESLAGC cyclic | TIMP3 | (18) | ND | (142) |
| CEASESLAGC linear | TIMP3 | (34) | ND | (142) |
| CEASESLAGC cyclic | TIMP3 | (3.7) | ND | (142) |
a
Note that different forms of enzymes were tested in the different studies. Kd values (in μM) are reported within parentheses and were measured by fluorescence polarization. Abbreviations: ND, not determined; NA, not applicable; Ac, acetyl. Unless indicated differently, all sequences are reported from the N- terminus to the C-terminus.
b
Values determined using bovine aggrecan (Glu392-Ala393 cleavage site).
c
Values determined using a QF-peptide.