SPECIAL NOTICE
A -- SH2 Domain-Binding Inhibitors Ready For Development
- Notice Date
- 12/30/2004
- Notice Type
- Special Notice
- NAICS
- 541710
— Research and Development in the Physical, Engineering, and Life Sciences
- Contracting Office
- Department of Health and Human Services, National Institutes of Health, National Cancer Institute, Bldg 427, Room 12, Frederick, MD, 21702
- ZIP Code
- 21702
- Solicitation Number
- Reference-Number-SF-SH2-01
- Description
- The National Cancer Institute (NCI) seeks a Cooperative Research and Development Agreement (CRADA) collaborator to develop a novel class of macrocyclic Grb2 SH2 domain-binding inhibitors that disrupt the interactions between Grb2 SH2 domains of proteins and proteins with phosphorylated moieties. As typified by Compound 1 (see http://ttb.nci.nih.gov for structure), these compounds display enhanced binding affinity and are very potent against proliferating cells in cell-based assays. Potential Commercial Applications: Oncogenic and hyper-proliferative disorders such as cancer, inflammation, autoimmune disease and allergies Main Advantages of the Technology: In extracellular assays these macrocyclic peptide mimetics display enhanced Grb2 SH2 domain-binding affinity over previously described SH2 domain-binding inhibitors. Addition to the extracellular media of cell cultures without the use of carrier peptides or membrane permeabalization techniques, results in cellular blockade cytoplasmic association of Grb2 with cognate activated tyrosine kinases. Administration to cultures of cancer cells driven by Grb2-dependent growth factor receptor pathways results in antimitogenic effects at non-cytotoxic concentrations. Current State of Development: Biological evaluation is limited to extracellular assays and cell culture systems. Animal studies require preparation of larger quantities of inhibitor than are currently available. Synthetic complexity currently limits scale up of compound needed for animal studies. Further R&D Required: Improving the synthesis of these compounds Preparing larger quantities of inhibitor than are currently available Conducting in vivo animal studies to aid in determining clinical efficacy and drug development Patent Status: International Patent Application filed on 6/26/2003 Pertinent References: Wei CQ, et al. J Med Chem. 2003 Jan 16;46(2):244-54. Shi ZD, et al. J Med Chem. 2004 Apr 8;47(8):2166-9. Contact Information: CRADA Contact: Steven C. Fausch, Ph.D., Technology Transfer Branch, NCI Phone: 301-846-6820; E-mail: fauschs@mail.nih.gov Licensing Contact: George G. Pipia, Ph.D., Office of Technology Transfer, NIH Phone: 301-435-5560; E-mail: pipiag@mail.nih.gov
- Record
- SN00728083-W 20050101/041230211644 (fbodaily.com)
- Source
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