Structure-Activity Studies of Analogues of Blomhotin Mediating Contraction of Rat Fundus
スポンサーリンク
概要
- 論文の詳細を見る
Blomhotin is a novel peptide (pGlu^1-Gly^2-Arg^3-Pro^4-Pro^5-Gly^6-Pro^7-Pro^8-Ile^9-Pro^<10>-Arg^<11>) which has been isolated from the venom of Agkistrodon halys blomhoffii and exhibits contractile activity on rat stomach fundus. We carried out a structure-activity study of blomhotin and its related peptides, and the findings suggested that the N-terminal portion of blomhotin is mainly responsible for affinity for the blomhotin receptor, whereas the C-terminal portion of blomhotin, Pro-Ile-Pro-Arg, is responsible for complete activation of the blomhotin receptor in the rat stomach fundus. In particular, the amino acids at positions 9 and 11 of blomhotin appear to be essential for binding and intrinsic activity. Using knowledge gained from this structure-activity analysis, we have identified photoactive blomhotin analogues that have sufficient biological activity to probe the target molecule of blomhotin.
- 公益社団法人日本薬学会の論文
- 2000-11-01
著者
-
YANOSHITA Ryohei
Institute of Medicinal Chemistry, Hoshi University
-
Yanoshita Ryohei
Institute Of Medicinal Chemistry Hoshi University
-
SAMEJIMA Yuji
Institute of Medicinal Chemistry, Hoshi University
-
Samejima Yuji
Institute Of Medicinal Chemistry Hoshi University
-
IWASAKI Eyu
Institute of Medicinal Chemistry, Hoshi University
-
KAMBE Terumi
Institute of Medicinal Chemistry, Hoshi University
-
Iwasaki Eyu
Institute Of Medicinal Chemistry Hoshi University
-
Kambe Terumi
Institute Of Medicinal Chemistry Hoshi University
関連論文
- Exosome-Like Vesicles with Dipeptidyl Peptidase IV in Human Saliva(Biochemistry)
- Inhibition of LysoPAF Acetyltransferase by the Ingredients from Lithospermum Root
- Inhibition of LysoPAF Acetyltransferase Activity by Components of Licorice Root
- Structure-Activity Studies of Analogues of Blomhotin Mediating Contraction of Rat Fundus
- Inhibition of LysoPAF Acetyltransferase by the Ingredients from Lithospermum Root