Document Detail


Contribution of residue B5 to the folding and function of insulin and IGF-I: constraints and fine-tuning in the evolution of a protein family.
MedLine Citation:
PMID:  19959476     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
Proinsulin exhibits a single structure, whereas insulin-like growth factors refold as two disulfide isomers in equilibrium. Native insulin-related growth factor (IGF)-I has canonical cystines (A6-A11, A7-B7, and A20-B19) maintained by IGF-binding proteins; IGF-swap has alternative pairing (A7-A11, A6-B7, and A20-B19) and impaired activity. Studies of mini-domain models suggest that residue B5 (His in insulin and Thr in IGFs) governs the ambiguity or uniqueness of disulfide pairing. Residue B5, a site of mutation in proinsulin causing neonatal diabetes, is thus of broad biophysical interest. Here, we characterize reciprocal B5 substitutions in the two proteins. In insulin, His(B5) --> Thr markedly destabilizes the hormone (DeltaDeltaG(u) 2.0 +/- 0.2 kcal/mol), impairs chain combination, and blocks cellular secretion of proinsulin. The reciprocal IGF-I substitution Thr(B5) --> His (residue 4) specifies a unique structure with native (1)H NMR signature. Chemical shifts and nuclear Overhauser effects are similar to those of native IGF-I. Whereas wild-type IGF-I undergoes thiol-catalyzed disulfide exchange to yield IGF-swap, His(B5)-IGF-I retains canonical pairing. Chemical denaturation studies indicate that His(B5) does not significantly enhance thermodynamic stability (DeltaDeltaG(u) 0.2 +/- 0.2 kcal/mol), implying that the substitution favors canonical pairing by destabilizing competing folds. Whereas the activity of Thr(B5)-insulin is decreased 5-fold, His(B5)-IGF-I exhibits 2-fold increased affinity for the IGF receptor and augmented post-receptor signaling. We propose that conservation of Thr(B5) in IGF-I, rescued from structural ambiguity by IGF-binding proteins, reflects fine-tuning of signal transduction. In contrast, the conservation of His(B5) in insulin highlights its critical role in insulin biosynthesis.
Authors:
Youhei Sohma; Qing-xin Hua; Ming Liu; Nelson B Phillips; Shi-Quan Hu; Jonathan Whittaker; Linda J Whittaker; Aubree Ng; Charles T Roberts; Peter Arvan; Stephen B H Kent; Michael A Weiss
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Publication Detail:
Type:  Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.     Date:  2009-12-03
Journal Detail:
Title:  The Journal of biological chemistry     Volume:  285     ISSN:  1083-351X     ISO Abbreviation:  J. Biol. Chem.     Publication Date:  2010 Feb 
Date Detail:
Created Date:  2010-02-08     Completed Date:  2010-05-11     Revised Date:  2012-04-05    
Medline Journal Info:
Nlm Unique ID:  2985121R     Medline TA:  J Biol Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  5040-55     Citation Subset:  IM    
Affiliation:
Department of Biochemistry and Molecular Biology, University of Chicago, Chicago, Illinois 60637, USA.
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MeSH Terms
Descriptor/Qualifier:
Animals
Cell Line
Circular Dichroism
Disulfides
Glycosylation
Humans
Insulin / chemical synthesis,  chemistry*,  pharmacology*
Insulin-Like Growth Factor I / chemical synthesis,  chemistry*,  pharmacology*
Magnetic Resonance Spectroscopy
Mice
Phosphorylation / drug effects
Proinsulin / biosynthesis,  genetics,  metabolism
Protein Folding
Protein Stability
Signal Transduction / drug effects
Structure-Activity Relationship
Grant Support
ID/Acronym/Agency:
DK48280/DK/NIDDK NIH HHS; R01 DK040949-11/DK/NIDDK NIH HHS; R01 DK069764/DK/NIDDK NIH HHS; R01 DK069764-01/DK/NIDDK NIH HHS; R01 DK40949/DK/NIDDK NIH HHS
Chemical
Reg. No./Substance:
0/Disulfides; 0/Insulin; 67763-96-6/Insulin-Like Growth Factor I; 9035-68-1/Proinsulin
Comments/Corrections

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