FLUORESCENT AND PHOTO-AFFINITY ENKEPHALIN DERIVATIVES - PREPARATION AND INTERACTION WITH OPIATE RECEPTORS

被引：56

作者：

HAZUM, E ^{[1
]}

CHANG, KJ ^{[1
]}

SHECHTER, Y ^{[1
]}

WILKINSON, S ^{[1
]}

CUATRECASAS, P ^{[1
]}

机构：

[1] WELLCOME RES LABS,BECKENHAM BR3 3BS,KENT,ENGLAND

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 1979年 / 88卷 / 03期

关键词：

D O I：

10.1016/0006-291X(79)91485-2

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The fluorescent and photo-affinity derivatives of enkephalin, Tyr-D-Ala-Gly-Phe-Leu-Lys-Nε-Rhodamine (II) and Tyr-D-Ala-Gly-Phe-Leu-Lys-Nε-nitro-azidophenyl (III), were prepared by conventional methods followed by chemical modification. The two peptides inhibit the binding of 125I-labeled enkephalin to brain membrane preparations, with apparent IC50 values of 5.9 nM and 5.5 nM for peptides II and III, respectively. The iodinated derivative of peptide III binds specifically to brain membrane preparations with an apparent Kd of about 2.1 × 10-9M. © 1979.

引用

页码：841 / 846

页数：6

共 10 条

[1] CHANG KJ, 1978, MOL PHARMACOL, V14, P961
[2] CHANG KJ, J BIOL CHEM
[3] Goldman M., 1968, FLUORESCENT ANTIBODY
[4] HAZUM E, 1979, J BIOL CHEM, V254, P1765
[5] IDENTIFICATION OF 2 RELATED PENTAPEPTIDES FROM BRAIN WITH POTENT OPIATE AGONIST ACTIVITY
HUGHES, J
SMITH, TW
KOSTERLITZ, HW
FOTHERGILL, LA
MORGAN, BA
MORRIS, HR
[J]. NATURE, 1975, 258 (5536) : 577 - 579
[6] PREPARATION OF PHOTO-AFFINITY PROBES FOR INSULIN RECEPTOR SITE IN ADIPOSE AND LIVER-CELL MEMBRANES
LEVY, D
[J]. BIOCHIMICA ET BIOPHYSICA ACTA, 1973, 322 (02) : 329 - 336
[7] INTERACTION OF IODINATED ENKEPHALIN ANALOGS WITH OPIATE RECEPTORS
MILLER, RJ
CHANG, KJ
LEIGHTON, J
CUATRECASAS, P
[J]. LIFE SCIENCES, 1978, 22 (05) : 379 - 387
[8] D-ALA2-MET-ENKEPHALINAMIDE - POTENT, LONG-LASTING SYNTHETIC PENTAPEPTIDE ANALGESIC
PERT, CB
PERT, A
CHANG, JK
FONG, BTW
[J]. SCIENCE, 1976, 194 (4262) : 330 - 332
[9] MORPHINE-LIKE PEPTIDES IN MAMMALIAN BRAIN - ISOLATION, STRUCTURE ELUCIDATION, AND INTERACTIONS WITH OPIATE RECEPTOR
SIMANTOV, R
SNYDER, SH
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1976, 73 (07) : 2515 - 2519
[10] OPIATE RECEPTORS AND OPIOID PEPTIDES
SNYDER, SH
CHILDERS, SR
[J]. ANNUAL REVIEW OF NEUROSCIENCE, 1979, 2 : 35 - 64

← 1 →