(PRWEB) February 03, 2014
BPS Bioscience, Inc. (“BPS”) announces the availability of an assay kit specific for the C-terminal region of HSP90β and screening services for both inhibitors of HSP90α and domain-specific inhibitors of HSP90β. The two isoforms of the 90 kDa heat shock protein (HSP90α and β) are chaperones that direct proper protein folding, cellular transport, and degradation. These isoforms are integral to the folding and stabilization of over 50 proteins directly related to tumor growth, making HSP90 an exceptionally promising target for the development of anti-cancer drugs. HSP90 is also a key target for several neurodegenerative and inflammatory diseases, including Alzheimer’s and Parkinson’s.
HSP90 proteins are homodimers that contain N-terminal, middle, and C-terminal functional domains. ATP hydrolysis by the N-terminal domain is required for HSP90 function, and this activity is inhibited by the natural products geldanamycin and radicicol. The middle domain contains a high-affinity binding site for co-chaperones and client proteins. Finally, the C-terminal domain contains a secondary ATP binding site and a conserved binding site for co-chaperones. The HSP90 C-terminus does not exhibit ATPase activity. Instead, it contributes to a conformational change of the entire homodimer that is required for the binding and release of client proteins controlled by the ATPase cycle of the N-terminal domain.
Many oncogenes, including tyrosine kinases, transcription factors, and cell-cycle regulatory proteins, are client proteins of HSP90. HSP90 inhibitors binding to the ATP binding pocket at the N-terminal domain or preventing the conformational change of the C-terminal domain cause client protein degradation via the ubiquitin—proteasome pathway, thereby downregulating several redundant pathways crucial for cell viability and tumor development. A number of pharmaceutical companies have developed potent first- and second-generation anti-cancer drugs that inhibit HSP90 function. While the N-terminal domain of HSP90 has been widely exploited, recent evidence suggests that targeting the C-terminal domain will lead to the identification of new and innovative pharmacologic agents based on perturbation of the dimer interface or the alternate ATP binding site.
BPS is the first company to offer HSP90β assay kits that can differentiate binding to the C-terminus or N-terminus of the HSP90β protein. BPS is also the first company to offer services for screening inhibitors of the HSP90 pathway. BPS’s customizable services can determine IC50 values or screen multiple compounds against a single protein for the identification and evaluation of lead drug candidates.
In addition to the domain-specific HSP90β assay kits and HSP90α kit, BPS offers several high purity HSP enzymes for drug discovery research. BPS plans to continue assisting researchers identify and validate novel HSP therapeutics by offering additional HSP-related products and services in the coming months, including a C-terminal HSP90α assay.
To learn more about BPS Bioscience’s Heat Shock Protein products, please visit our website at http://bpsbioscience.com/product-search?search=hsp. For further information on BPS Bioscience’s screening services for HSP90, visit http://bpsbioscience.com/images/pdf/HSP_Screening.pdf
About BPS Bioscience
BPS Bioscience, Inc. is a leading manufacturer of recombinant proteins and assay kits for life science and drug discovery research. In addition to tools and services for HSP research, BPS offers Acetyltransferases, Bromodomains, HDACs, Histone Demethylases, Methyltransferases, Kinases, Phosphatases, Phosphodiesterases, Poly ADP Ribose Polymerases (PARPs), Proteases, and Ubiquitination Enzymes. BPS also provides custom protein expression, biochemical and cell-based assays, and compound screening and profiling services. Headquartered in San Diego, California, BPS has provided products and services to pharmaceutical companies and academic institutes in over 45 countries worldwide. By being at the forefront of technology development, BPS provides innovative, high quality life science products and services in a timely manner to help our customers accelerate drug discovery and development for the treatment of human diseases.
Visit BPS’s website for more information: http://www.bpsbioscience.com.