Anaphylactoid Properties of LHRH Analogs (original) (raw)

1987

Abstract

The isolation and structural elucidation of LHRH by Schally [1] and Guillemin [2] in 1971 led to the synthesis of analogs which have been proposed for use in a variety of clinical disorders such as endometriosis, precocious puberty and prostatic carcinoma. These analogs have included both agonists, many of which are currently being studied clinically, and more recently, competitive antagonists. The first LHRH antagonists which were synthesized in 1972 [3] were not very potent, but did support the feasibility of synthesizing competitive antagonists. This led to research in many laboratories to improve the potency of antagonists. As reviewed by Karten [4], a large number of chemical modifications of LHRH have been attempted. Substitutions at positions 2, 3 and 6 have been among the most effective, although the structure activity relationships in this work appear to be very complex. One series of analogs with an arginine substituted at position 6 appears to be most potent [5,6]. One of these, [N-Ac-D-Nal(2)1, D-pF-Phe2, D-Trp3, D-Arg6] LHRH has been proposed for clinical studies.

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