Dermorphin sequence with high δ-afinity by fixing the phe sidechain to trans at ξ1

D. Tourwé; K. Verschueren; G. Van Binst; P. Davis; F. Porreca; V. J. Hruby

doi:10.1016/S0960-894X(00)80235-8

Dermorphin sequence with high δ-afinity by fixing the phe sidechain to trans at ξ₁

D. Tourwé
, K. Verschueren
, G. Van Binst
, P. Davis
, F. Porreca
, V. J. Hruby

Research output: Contribution to journal › Article › peer-review

33 Scopus citations

Abstract

The Phe sidechain in dermorphin was fixed into the trans conformation by linking the aromatic ring to the Gly nitrogen through a methylene bridge. The compound has high μ- and δ-opioid activities.

Original language	English (US)
Pages (from-to)	1305-1308
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	2
Issue number	10
DOIs	https://doi.org/10.1016/S0960-894X(00)80235-8
State	Published - Oct 1992

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/S0960-894X(00)80235-8

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title = "Dermorphin sequence with high δ-afinity by fixing the phe sidechain to trans at ξ1",

abstract = "The Phe sidechain in dermorphin was fixed into the trans conformation by linking the aromatic ring to the Gly nitrogen through a methylene bridge. The compound has high μ- and δ-opioid activities.",

author = "D. Tourw{\'e} and K. Verschueren and \{Van Binst\}, G. and P. Davis and F. Porreca and Hruby, \{V. J.\}",

note = "Funding Information: Dr. J.E. Leysen (Janssen Research Foundation) is greatly acknowledged for the binding data; we thank S.E. de Laszlo (Merck Sharp \& Dohme) for communicating experimental details; and the National Institute of Drug Absense for partial support (U. of A.).",

year = "1992",

month = oct,

doi = "10.1016/S0960-894X(00)80235-8",

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T1 - Dermorphin sequence with high δ-afinity by fixing the phe sidechain to trans at ξ1

AU - Tourwé, D.

AU - Verschueren, K.

AU - Van Binst, G.

AU - Davis, P.

AU - Porreca, F.

AU - Hruby, V. J.

N1 - Funding Information: Dr. J.E. Leysen (Janssen Research Foundation) is greatly acknowledged for the binding data; we thank S.E. de Laszlo (Merck Sharp & Dohme) for communicating experimental details; and the National Institute of Drug Absense for partial support (U. of A.).

PY - 1992/10

Y1 - 1992/10

N2 - The Phe sidechain in dermorphin was fixed into the trans conformation by linking the aromatic ring to the Gly nitrogen through a methylene bridge. The compound has high μ- and δ-opioid activities.

AB - The Phe sidechain in dermorphin was fixed into the trans conformation by linking the aromatic ring to the Gly nitrogen through a methylene bridge. The compound has high μ- and δ-opioid activities.

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U2 - 10.1016/S0960-894X(00)80235-8

DO - 10.1016/S0960-894X(00)80235-8

M3 - Article

AN - SCOPUS:0026466124

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JO - Bioorganic and Medicinal Chemistry Letters

JF - Bioorganic and Medicinal Chemistry Letters

IS - 10

ER -

Dermorphin sequence with high δ-afinity by fixing the phe sidechain to trans at ξ₁

Abstract

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