| Name | prolyl dipeptidase DPP8 |
|---|---|
| Synonyms | DP8; DPP 8; DPP8; DPRP 1; DPRP1; Dipeptidyl peptidase 8; Dipeptidyl peptidase IV related protein 1; Dipeptidyl peptidase VIII… |
| Name | piperazine |
|---|---|
| CAS | piperazine |
| PubMed | Abstract | RScore(About this table) | |
|---|---|---|---|
| 15664838 | Jiaang WT, Chen YS, Hsu T, Wu SH, Chien CH, Chang CN, Chang SP, Lee SJ, Chen X: Novel isoindoline compounds for potent and selective inhibition of prolyl dipeptidase DPP8. Bioorg Med Chem Lett. 2005 Feb 1;15(3):687-91. Isoindoline with a 1-(4,4'-difluor-benzhydryl)-piperazine group at the P2 site was observed to be a very potent DPP8 inhibitor, having an IC (50) value of 14nM with at least a 2500-fold selectivity over either DPP-IV or DPP-II. |
36(0,1,1,6) | Details |
| 17352677 | Thornberry NA, Weber AE: Discovery of JANUVIA (Sitagliptin), a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Curr Top Med Chem. 2007;7(6):557-68. The observation that both compounds inhibit the related peptidases DPP8 and DPP9 led to the hypothesis that inhibition of DPP8 and/or DPP9 could evoke severe toxicities in preclinical species. Initial work in an alpha-amino acid series related to isoleucyl thiazolidide was discontinued due to lack of selectivity; however, SAR studies on two screening leads led to the identification of a highly selective beta-amino acid piperazine series. |
1(0,0,0,1) | Details |