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Insulin's structural behavior and its relation to activity
Author(s) -
Dodson E. J.,
Dodson G. G.,
Hubbard R. E.,
Reynolds C. D.
Publication year - 1983
Publication title -
biopolymers
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.556
H-Index - 125
eISSN - 1097-0282
pISSN - 0006-3525
DOI - 10.1002/bip.360220137
Subject(s) - chemistry , potency , insulin , biophysics , receptor , structure–activity relationship , stereochemistry , hormone , endocrinology , biochemistry , medicine , in vitro , biology
This paper discusses the hypothesis that insulin undergoes a conformational change either before or during its binding to the receptor. The evidence for this is not conclusive but allows us to reconcile the following observations: (1) no chemical modification or deletion of invariant surface residues has abolished the hormone's activity—only reduced its potency. (2) Reduction in potency follows many modifications to different side chains, both variant and invariant. (3) There are insulins with perfectly preserved structure (by the criteria of aggregation, spectroscopy, and x‐ray analysis) that have markedly reduced potency. (4) Insulins with disturbed structure still exhibit real, sometimes substantial activity.