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Kinexus Launches DrugKiNET KnowledgeBase with 105,000 Experimentally Tested Protein Kinase Drug Interactions

Kinexus Bioinformatics Corporation, a world-leader in the study of molecular intelligence systems, announced the launch of its DrugKiNET KnowledgeBase (www.drugkinet.ca) for the identification and development of drug candidates that potently and selectively inhibit human protein kinases. This open-access website features quantitative data on the effects of over 800 chemical compounds on more than 400 protein kinases following careful annotation of hundreds of experiments documented in the scientific literature. This data was then used to train two different proprietary algorithms to predict the inhibitory effects of 550 of these compounds on 500 human protein kinases. This information can guide biomedical researchers in the discovery of new therapeutic targets for existing drugs, and aid in the design of promising new drugs.

At least 538 different protein kinases regulate each other and another approximately 21,500 diverse protein targets to coordinate all of the operations in living cells through complex molecular communications and control networks. Kinases are well recognized by the pharmaceutical and biotech industry as highly productive targets for drug development with applications for cancer, diabetes, Alzheimer’s disease and many other diseases. In fact, over 400 human disease have been linked to genetic mutations in the genes that encode protein kinases or the direct actions of environmental toxins that target protein kinases. Over the last decade, more than two dozen kinase inhibitors have already been approved for clinical use, primarily for cancer treatment. By targeting inappropriately active kinases, these small molecule drugs essentially re-program cancer cells for their demise.

Over the last year, Kinexus and their collaborators in the Mathematics of Information Technology and Complex Systems (MITACS) groups at the University of British Columbia and Simon Fraser University have worked to identify the specific parts of different protein kinases that are critical for recognition by each of 550 different compounds that have been experimentally shown to inhibit one or more kinases. These parts, termed Inhibitor Determining Residues (IDR’s), may be involved in recognizing and binding drugs, and their identification within DrugKiNET can facilitate further optimization of even more potent and specific protein kinase inhibitory drugs. Previously, Kinexus and its partners identified Substrate Determining Residues (SDR’s) in protein kinases that were important for recognition of their protein targets and deposited this information in their open-access PhosphoNET Knowledgebase (www.phosphonet.ca).

“We believe that DrugKiNET is an extremely unique and powerful resource for the biomedical research community,” commented Dr. Steven Pelech, President and Chief Scientific Officer of Kinexus and a professor in the Department of Medicine at the University of British Columbia. “Over a third of all pharmaceutical drug development is presently focused on protein kinase inhibitory drugs, but we expect this to increase even more, since the vast majority of protein kinases have yet to be pursued as drug targets, and definition of the precise roles of different kinases in non-cancer-related diseases is still in its infancy.”

Dr. Pelech added, “We are excited by the prospect that our algorithms can define new protein kinase targets for existing drugs, and that they can identify in the genes that encode protein kinases the specific mutations that may alter their sensitivities to these drugs. As Kinexus has the capability of testing the effects of drug candidates on over 350 different purified protein kinases in-house, we also have the ability to experimentally validate many of our drug predictions for our clients.”

Kinexus is a private, biotechnology company engaged in the research and development of innovative methods to map, track and manipulate cellular communication networks. The application of this knowledge positions Kinexus and its clients in drug development, rational drug design, disease diagnosis and personalized therapies to improve human health. Kinexus currently has agreements with over 1700 research laboratories in companies, universities, government institutions and hospitals in over 35 different countries. To learn more about the diverse proteomics and bioinformatics services offered by Kinexus, please visit www.kinexus.ca or call toll-free at 1-866-KINEXUS.

Source: Kinexus Bioinformatics Corporation

med fusion and Theranostics Health Release Novel Cancer Theranostic Test

med fusion and Theranostics Health will introduce the first of the TheraLink™Assays for use in patients with malignant diseases at the American Society of Clinical Oncology (ASCO) Annual ’13 Meeting, held in Chicago, IL from May 31, 2013 through June 4, 2013. The TheraLink™ HER Family Assay for primary, recurrent and metastatic breast cancers provides a molecular analysis of each patient’s unique cancer, based upon the functional activity of signal transduction pathways known to modulate cancerous growth. This ‘theranostic’ assay provides a comprehensive molecular profile of the HER family of cell surface receptors and three key signaling pathways modulated by the HER family which have important roles in the therapeutic approach to treating breast cancer. The TheraLink™ HER Family Assay is the first in a series of similar assays based upon measuring a panel of analytes, including a number of drug targets.

med fusion and Theranostics Health will also announce that they are entering into an exclusive distribution agreement for Theranostics Health’s TheraLink™ HER Family Assay. Under the terms of the agreement, med fusion and its affiliate, Pathologists Bio-Medical Laboratories (PBM), will provide a gateway for access to the theranostic test for the McKesson Network of oncologists, which includes US Oncology and Texas Oncology and to the oncologists of the Baylor Healthcare System. Oncologists will be able to order the assay through their pathology services directly from med fusion.

The TheraLink™ HER Family Assay measures the total amount and activation (phosphorylation) status of 14 critical proteins, receptors and signaling pathway members, providing actionable information for ten currently marketed therapeutics. Starting with a few histopathology sections taken from a core needle biopsy or open resection, the assay is a reverse-phase immunoassay that leverages the extreme sensitivity and precision of microarray technologies to measure these very low abundance proteins, with analyte-specific quantitation provided by on-array calibration samples along with positive and negative controls. The assay provides oncologists with actionable information on drug targets, directly linking active drug targets and the available therapies to identify the most effective personalized treatment options.

“We believe med fusion provides Theranostics Health with a unique opportunity to advance the use of the TheraLink™ Assays,” says Glenn Hoke , President and CEO of Theranostics Health. “Through relationships with their founders, including the McKesson family of health care companies and the Baylor Healthcare System, med fusion provides Theranostics Health with a strong marketing and distribution partner to ensure these assays find utility in the clinical setting.”

“Signal pathway analysis provides some of the most relevant information for targeting cancer therapies,” says Gary L. Smith , Ph.D., Interim CEO and Chief Operating Officer of med fusion. “Furthermore, our collaboration with Theranostics and PBM continues to support med fusion’s model of developing and creating strategic alliances that expand our offering of personalized diagnostic testing services within a patient-centric model of care delivery.”

Source: PR Newswire

H3 Biomedicine and BGI Announce Collaboration to Develop and Share Crucial Cancer Genomic Sequencing Data

H3 Biomedicine Inc., a biopharmaceutical company specializing in the discovery and development of oncology treatments, and BGI, the largest genomics organization in the world, jointly recently announced that they have entered into a partnership to sequence and publish genomic data from pre-clinical cancer models. This research, which aims to identify and validate recurrent gene mutations that are potential targets for drug therapies, is crucial for the entire oncology drug discovery industry. Consistent with their respective ongoing commitments to open-access research, as well as BGI’s distinguished history of published, collaborative research, H3 and BGI will release the cancer genomic data to the global research community upon completion of data analysis.

“We truly believe that genomic information generated from patient samples or material derived thereof should be shared with the scientific community. As a matter of fact, the community has benefited enormously from collaborative efforts like The Cancer Genome Atlas (TCGA) and International Cancer Genome Consortium (ICGC),” stated Markus Warmuth, M.D., president and chief executive officer, H3 Biomedicine. “Open access to this information has enabled countless scientific advances, and our intention is to further accelerate oncology drug discovery by releasing the data we generate with BGI. We see this as a significant step in building shared translational oncology platforms that will bring the research community together to deliver new personalized medicines, especially for those people living with cancers for which there are, today, limited treatment options.”

Recent advances in human cancer genomics have revealed novel cancer target opportunities that will enable personalized cancer medicine approaches. Many of the identified recurrent gene mutations exist at low frequencies and the information necessary to select relevant pre-clinical models to study these mutations does not exist. Under the partnership announced today, BGI will sequence 250 cancer cell lines via next-generation, whole exome sequencing in this first study. H3 Biomedicine and BGI will jointly analyze the data to deliver a highly curated set of genetically profiled, pre-clinical model information that will help to accelerate drug discovery and development efforts.

Yingrui Li, chief executive officer of BGI Americas, said, “We are pleased to collaborate with H3 Biomedicine, and to have this opportunity to apply our state-of-the-art, next-gen sequencing capabilities and bioinformatics expertise to help advance the discovery of novel cancer drug targets and full-scale pharmacogenomics findings. I believe this partnership will yield significant, valuable genomic information that will lay a solid foundation for developing pre-clinical cancer models and new anticancer drugs to benefit human health. BGI, in keeping with our global legacy of collaborative, published research, including our participation in ICGC, looks forward to partnering with H3 Biomedicine in developing and sharing this genomic data with the international research community.”

Source: H3 Biomedicine

Kinexus Identifies Over 966,000 Phosphorylation Sites in the Human Proteome

Kinexus Bioinformatics Corporation, a world-leader in molecular intelligence research, announced a major upgrade in its PhosphoNET KnowledgeBase (www.phosphonet.ca) for the study of cell communication systems. This open-access website now features data on over 177,000 experimentally-confirmed human phosphorylation sites (P-sites) and 789,000 additional P-sites predicted with a powerful algorithm trained with over 22,000 kinase-substrate pairs. PhosphoNET provides prediction of which kinases individually target each human P-site, and whether these P-sites are retained in proteins from over 20 other diverse organisms. Functionally critical P-sites that control proteins are more likely to also be found in other species. This information can guide biomedical researchers in the discovery of promising diagnostic biomarkers and therapeutic drug targets.

Advanced Cell Diagnostics Initiates Agreement to Study Biomarkers for Cancer Immunotherapy

Advanced Cell Diagnostics, Inc. (ACD) announced today that they have entered into an agreement with The Johns Hopkins University on behalf of its Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins to use ACD’s proprietary RNAscope® technology platform to validate novel biomarkers and drug targets for cancer immunotherapy.

Cancer immunotherapy, which aims to mobilize a patient’s immune system to fight cancer, has been gaining momentum recently with the FDA approval of anti-CTLA-4 therapy for melanoma and with the recent impressive and durable remissions produced by targeting PD1 in multiple solid tumors in early-phase clinical trials led by Johns Hopkins investigators. With many additional immune modulatory molecules identified for targeting that play major roles in specific subsets of cancer, it will be critical to develop standardized biomarkers to guide the application of the most effective immune therapies on a patient by patient basis.

Targeting the immune checkpoints that are often suppressed in many cancers has demonstrated tremendous potential. However, to identify biomarkers useful for guiding therapy, conventional approaches to biomarker analysis have proven inadequate, leading to conflicting results.

“The complex interplay between cancer cells and the immune system in the tumor microenvironment matches perfectly with RNAscope’s capability of single molecule sensitivity and single cell resolution, which can help pinpoint which cell is talking to which other cell,” said Dr. Yuling Luo, Founder, President and CEO of ACD. Dr. Luo added, “That knowledge will be essential for selecting optimal targets for drug development and predicting which patient will benefit from it. We feel extremely fortunate to be able to provide such a tool to the pioneers in this emerging and exciting field.”

Source: Advanced Cell Diagnostics