Wiczk W, Lankiewicz L, Kasprzykowski F, Ołdziej S, Szmaciński H, Lakowicz J R, Grzonka Z
Faculty of Chemistry, University of Gdańsk, Poland.
Eur Biophys J. 1997;26(2):183-93. doi: 10.1007/s002490050070.
Analogues of arginine-vasopressin (AVP) in which substitution of the proline residue in position 7 (by either sarcosine or N-methylalanine) combined with replacement of the cysteine residue in position 1 were the subject of a fluorescence and molecular mechanics study. We obtained two groups of analogues: selective antidiuretic agonists (cysteine or beta-mercaptopropionic acid in position 1) and pressor and uterotonic antagonists (deaminopenicillamine or beta-mercapto-beta, beta-cyclopentamethylenepropionic acid in position 1). Using frequency-domain measurements of fluorescence resonance energy transfer (FRET) we estimated the distance distribution between the phenolic ring of Tyr2 and the disulphide bridge Cys1-Cys6. We also analyzed acrylamide quenching of tyrosyl fluorescence to determine the exposure of the tyrosyl ring to the solvent. Results from fluorescence experiments were compared with those from Monte Carlo simulation (ECEPP/3 force-field).
精氨酸加压素(AVP)的类似物,其中第7位脯氨酸残基被肌氨酸或N-甲基丙氨酸取代,并结合第1位半胱氨酸残基的替换,是荧光和分子力学研究的对象。我们获得了两组类似物:选择性抗利尿激动剂(第1位为半胱氨酸或β-巯基丙酸)和升压及子宫收缩拮抗剂(第1位为脱氨青霉胺或β-巯基-β,β-环戊亚甲基丙酸)。使用荧光共振能量转移(FRET)的频域测量,我们估计了Tyr2酚环与二硫键Cys1-Cys6之间的距离分布。我们还分析了丙烯酰胺对酪氨酸荧光的淬灭,以确定酪氨酸环对溶剂的暴露情况。荧光实验结果与蒙特卡罗模拟(ECEPP/3力场)结果进行了比较。