PRODUCTION OF A HORMONE RECEPTOR COMPETITIVE ANTAGONIST

Award Information
Agency: Department of Health and Human Services
Branch: N/A
Contract: N/A
Agency Tracking Number: 7939
Amount: $50,000.00
Phase: Phase I
Program: SBIR
Awards Year: 1988
Solicitation Year: N/A
Solicitation Topic Code: N/A
Solicitation Number: N/A
Small Business Information
Integrated Genetics Inc
1 Mountain Rd, Framingham, MA, 01701
DUNS: N/A
HUBZone Owned: N
Woman Owned: N
Socially and Economically Disadvantaged: N
Principal Investigator
 () -
Business Contact
Phone: () -
Research Institution
N/A
Abstract
RECENT RESEARCH IN REPRODUCTIVE ENDOCRINOLOGY HAS DEMONSTRATED THE IMPORTANCE OF FOLLICLE STIMULATING HORMONE (FSH) IN THE REGULATION OF GAMETOGENESIS AND GONADAL STEROIDPRODUCTION. IT HAS BEEN SHOWN THAT N-LINKED OLIGOSACCHARIDES, ATTACHED TO ASPARAGINE RESIDUES AT SPECIFIC SITES ALONG THE MOLECULE, ARE ESSENTIAL FOR POST-RECEPTOR TARGET CELL ACTIVATION BUT NOT RECEPTOR BINDING. THESE SUGARS ALSO PLAY A ROLE IN DETERMINING THE HALF-LIFE OF THE MOLECULE IN CIRCULATION. WE PLAN TO USE THE TECHNIQUE OF SITE-DIRECTED MUTAGENESIS TO PRODUCE A RECOMBINANT HUMAN FSH MOLECULE THAT WILL HAVE ONE OR MORE OFTHE ASPARAGINE RESIDUES REPLACED WITH A SIMILARLY CHARGED AMINO ACID TO "ERASE" THE SITE OF N-LINKED SUGAR ATTACHMENT.PRELIMINARY STUDIES HAVE SHOWN THAT REMOVAL OF SUGARS FROM THE ALPHA CHAIN SEVERELY DECREASE BIOLOGIC ACTIVITY. REMOVAL OF THESE SUGAR RESIDUES, BY MUTAGENESIS, WILL PRODUCE A LONG ACTING COMPETITIVE ANTAGONIST OF FSH, WHICH, WHEN ADMINISTERED TO HUMANS, WOULD BE EXPECTED TO RESULT IN AN ANOVULATORY STATE OR AZOSPERMIA. A MUTAGENIZED, RECOMBINANT HORMONE MAY BE PRODUCED IN LARGE AMOUNTS, WITH EACH BATCH EXHIBITING UNIFORM BIOCHEMICAL AND BIOLOGICAL PROPERTIES. THEREFORE, THIS PRODUCT WOULD BE AN EXCELLENT CHOICE AS A REVERSIBLE CONTRACEPTIVE IN MEN AND WOMEN.

* information listed above is at the time of submission.

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