硼代正亮氨酸作为P1残基用于设计选择性强效二肽基肽酶7抑制剂。
Boro-norleucine as a P1 residue for the design of selective and potent DPP7 inhibitors.
作者信息
Shreder Kevin R, Wong Melissa S, Corral Sergio, Yu Zhizhou, Winn David T, Wu Min, Hu Yi, Nomanbhoy Tyzoon, Alemayehu Senaiet, Fuller Stacy R, Rosenblum Jonathan S, Kozarich John W
机构信息
ActivX Biosciences, 11025 N. Torrey Pines Road, La Jolla, CA 92037, USA.
出版信息
Bioorg Med Chem Lett. 2005 Oct 1;15(19):4256-60. doi: 10.1016/j.bmcl.2005.06.076.
Dipeptide-based inhibitors with C-substituted (alkyl or aminoalkyl) alpha-amino acids in the P2 position and boro-norleucine (boro-Nle) in the P1 position were synthesized. Relative to boro-proline, boro-Nle as a P1 residue was shown able to significantly dial out DPP4, FAP, DPP8, and DPP9 activity. Dab-boro-Nle (4g) proved to be the most selective and potent DPP7 inhibitor with a DPP7 IC50 value of 480 pM.
合成了在P2位具有C-取代（烷基或氨基烷基）α-氨基酸且在P1位具有硼代正亮氨酸（boro-Nle）的基于二肽的抑制剂。相对于硼代脯氨酸，硼代正亮氨酸作为P1残基能够显著消除DPP4、FAP、DPP8和DPP9的活性。Dab-硼代正亮氨酸（4g）被证明是最具选择性和强效的DPP7抑制剂，其DPP7 IC50值为480 pM。
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