TY - JOUR
T1 - Synthesis of leucine enkephalin derivatives
T2 - Structure-function studies
AU - Agarwal, Nirankar S.
AU - Hruby, Victor J.
AU - Katz, Robert
AU - Klee, Werner
AU - Nirenberg, Marshall
N1 - Funding Information:
*Department of Chemistry, University of Arizona, Tucson, Arizona; t Mid-Atlantic Research Institute, Bethesda, Maryland; #Laboratory of General and Comparative Biochemistry, National Institute of Mental Health, Bethesda, Maryland; flabor-atory of Biochemical Genetics, National Heart, Lung, and Blood Institute, National Institutes of Health, Bethesda, Maryland
PY - 1977/5/9
Y1 - 1977/5/9
N2 - The solid phase synthesis of highly purified [Leu5] enkephalin and of seven derivatives including [Ala2,Leu5]-, [Ser2,Leu5]-, [Ser3,Leu5]-, [Aba2,Leu5]-, and [des-Gly2(3),Leu5]enkephalins are reported, and their morphine-like activities in neuroblastoma x glioma cell homogenates were measured. Changes at the 2, 3, and 5 positions of the enkephalin provided analogues which were all less active than [Leu5] enkephalin. The results are discussed in terms of recently suggested conformational structures for the enkephalin peptides. No melanocyte stimulating activity was observed for [Leu5] enkephalin, [Ala2,Leu5]enkephalin, or [Ser2,Leu5] enkephalin.
AB - The solid phase synthesis of highly purified [Leu5] enkephalin and of seven derivatives including [Ala2,Leu5]-, [Ser2,Leu5]-, [Ser3,Leu5]-, [Aba2,Leu5]-, and [des-Gly2(3),Leu5]enkephalins are reported, and their morphine-like activities in neuroblastoma x glioma cell homogenates were measured. Changes at the 2, 3, and 5 positions of the enkephalin provided analogues which were all less active than [Leu5] enkephalin. The results are discussed in terms of recently suggested conformational structures for the enkephalin peptides. No melanocyte stimulating activity was observed for [Leu5] enkephalin, [Ala2,Leu5]enkephalin, or [Ser2,Leu5] enkephalin.
UR - http://www.scopus.com/inward/record.url?scp=0017682066&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0017682066&partnerID=8YFLogxK
U2 - 10.1016/0006-291X(77)91677-1
DO - 10.1016/0006-291X(77)91677-1
M3 - Article
C2 - 559493
AN - SCOPUS:0017682066
VL - 76
SP - 129
EP - 135
JO - Biochemical and Biophysical Research Communications
JF - Biochemical and Biophysical Research Communications
SN - 0006-291X
IS - 1
ER -