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News Article | April 17, 2017
Site: www.eurekalert.org

This article by Dr. Maria Digiacomo has been published in The Open Medicinal Chemistry Journal, Volume 11, 2017 Diabetes mellitus (DM) is probably one of the oldest known diseases and the incidence has been increasing steadily all over the world. This metabolic disease is characterized by chronic hyperglycemia due to defect in insulin secretion and/or insulin action. The etiopathology is very complex and is closely related with long-term damage, dysfunction, and failure of various organs, such as the eyes, kidneys, nerves, heart, and blood vessels. Strong epidemiological evidence suggest a relationship between blood sugar levels and the onset of diabetes complications, in fact, excess glucose in the body leads to conversion of sugar into its corresponding alcohol, namely sorbitol, via the polyol pathway. The activation of this pathway is dependent on the enzyme aldose reductase (ARL2) and thus its inhibition should be prevented or delay the onset of both micro- and macrovascular complications such as retinopathy, peripheral vascular disease and coronary artery disease. Currently, only the carboxylic acid epalrestat, an aldose reductase inhibitor (ARI), is available on the market and used for the treatment of diabetic neuropathy in Japan, India and China. Many ARIs have shown to be clinically unsuccessful because of adverse pharmacokinetics or toxic side-effects. In this study, we described the design, synthesis and biological evaluation of three small series of spirobenzopyran acetic acid derivatives, proposed as a scaffold for novel ALR2 inhibitors. Most of the new ARIs proved to inhibit the target enzyme, showing IC50 values in the micromolar/low micromolar range, without affecting the activity of another important enzyme, namely ARL1, which plays a detoxifying role in metabolic processes involved in the physiological homeostasis. These results suggested that the spirobenzopyran scaffold represents a new and promising tool that could pave the way to the discovery of novel and effective ARIs. For more information about the article, please visit https:/ Reference: Digiacomo, M.; (2017). Synthesis and Functional Evaluation of Novel Aldose Reductase Inhibitors Bearing a Spirobenzopyran Scaffold. The Open Medicinal Chemistry Journal., DOI: 10.2174/1874104501711010009


TORONTO, ON--(Marketwired - May 02, 2017) - In a live broadcast on Thursday, May 18, 2017, industry expert Dr. Sam Mann, Principal Scientist, Medicinal Chemistry from Charles River Laboratories will look at some of the complementary approaches to HTS from a chemist's perspective and how these strategies have been successfully applied to real drug discovery programs at Charles River for Charles River's partners. While high-throughput screening (HTS) remains a powerful weapon for hit identification, it is important to be aware of the many alternative tools available to the medicinal chemist for initiating a drug discovery program. No hit identification method is always fruitful; they all have their strengths and weaknesses, and only by judicious integration of hit identification approaches can the chances of success be maximized. For more information about this free webinar visit: Alternatives to HTS - Hit-finding Approaches in the Medicinal Chemist's Arsenal Xtalks, powered by Honeycomb Worldwide Inc., is a leading provider of educational webinars to the global Life Sciences community. Every year thousands of industry practitioners (from pharmaceutical & biotech companies, private & academic research institutions, healthcare centers, etc.) turn to Xtalks for access to quality content. Xtalks helps Life Science professionals stay current with industry developments, trends and regulations. Xtalks webinars also provide perspectives on key issues from top industry thought leaders and service providers. To learn more about Xtalks visit http://xtalks.com


TORONTO--(BUSINESS WIRE)--Cerveau Technologies, Inc. today announced finalization of a clinical supply agreement with Merck, known as MSD outside the US and Canada, providing access to an investigational imaging agent being evaluated in Positron Emission Tomography (PET) scans for assessing the status and progression of neurofibrillary tangles (NFTs) in the brain. NFTs made up of aggregated tau protein are believed to provide a hallmark of several neurodegenerative diseases, including Alzheimer’s disease. As part of the agreement Cerveau will be responsible for providing access to MK-6240 at multiple sites globally to be used in Merck-specific research initiatives. Cerveau will be accelerating technology transfer and site qualification in over fifteen sites to provide access to support broad availability. “At Cerveau, we are focused on providing information and technologies to researchers and clinicians in order to improve brain health,” said Rick Hiatt, President and Chief Executive Officer of Cerveau Technologies, Inc. “We are excited by the opportunity to work with Merck and the pharmaceutical industry in providing access to this investigational imaging agent to the broader scientific community. We are rapidly establishing collaborations and agreements to improve processes in order to support multiple initiatives around the world.” “There is a critical need for new imaging agents that provide sensitive biomarkers to enable early diagnosis of neurodegenerative diseases and allow for more appropriate staging of disease states, and measuring the effect of disease-modifying therapeutics,” said Cyrille Sur, Executive Director, Translational Imaging Biomarkers, Merck Research Laboratories. “Agreements such as this provide a platform to evaluate the potential of our novel Tau imaging agent.” In early studies published in the Journal of Medicinal Chemistry, Merck scientists reported that [18F]MK-6240 has a high specificity and selectivity for neurofibrillary tangles with favorable physicochemical properties and in vivo pharmacokinetics that warranted clinical investigation as a potential PET neuroimaging agent. Merck and Cerveau are currently conducting an open-label Phase 1 study to investigate the safety and efficacy of [18F]MK-6240 as a PET imaging agent for quantifying brain burden of neurofibrillary tangle pathology. For further information about the trial please go to clinical trials.gov (NCT02562989). Cerveau Technologies, Inc. is a partnership between Enigma Biomedical Group, Inc. and Sinotau Pharmaceutical Group. Cerveau's vision is to globally develop diagnostics and technology that will impact patients with neurodegenerative disorders including Alzheimer's disease.


News Article | February 15, 2017
Site: www.businesswire.com

CAMBRIDGE, Mass.--(BUSINESS WIRE)--Lando and Anastasi, LLP (L&A) today announced that Nathaniel Schafheimer, Ph.D., Wei Zhang, Ph.D., and Ioana Davies, Ph.D. have joined the firm. L&A continues to expand its Life Sciences practice, with the recent addition of three hires in the group. “Nathaniel, Wei, and Ioana have stellar backgrounds which dovetail well with our clients’ technologies,” commented Cathy McCarty, a Life Sciences partner and co-managing partner of the firm. “Adding new practitioners helps to maintain our technological currency, and these three bring a wonderful energy that complements our existing practice group,” added Diana Collazo, a Life Sciences partner. Ioana Davies is an organic chemist, whose practice focuses on patent prosecution, portfolio analysis and management, and diligence in all areas of the life sciences. Prior to joining L&A, she was a medicinal chemist at Vertex Pharmaceuticals for 13 years, the last 8 of which were as a senior research scientist. Ioana received a Ph.D. in Organic Chemistry from Yale University and she completed her postdoctoral fellowship in chemistry at California Institute of Technology. She earned an M.S. degree and a B.S., with honors, in chemistry from Babes-Bolyai University (Romania). Ioana is registered to practice before the U.S. Patent and Trademark Office, and is an inventor on 16 U.S. patents. She is the author of a number of scientific research articles published in well-known journals, including Bioorganic & Medicinal Chemistry Letters, Journal of Medicinal Chemistry, Organic Letters, and Journal of Organic Chemistry. Nathaniel Schafheimer works with L&A’s biotechnology clients in all aspects of patent prosecution, including portfolio and diligence analyses. Immediately prior to joining L&A, Nathaniel was a Technical Advisor at Ropes & Gray in Boston. Prior to joining Ropes, he was a post-doctoral associate at Massachusetts Institute of Technology, where he developed online biology courses on the edX learning platform covering a wide array of life science topics. Nathaniel received a Ph.D. in Biology from Massachusetts Institute of Technology. His doctoral research examined how ultraviolet light contributed to cataract development by monitoring the protein aggregation and structural conformation of human lens proteins. Nathaniel received both an M.S., summa cum laude, and a B.S., summa cum laude, from Brandeis University. Wei Zhang has extensive knowledge in the areas of immunology, antibody protein and polynucleotide therapies. She works with clients ranging from multinational pharmaceutical companies to biotechnology start-ups on the preparation and prosecution of patent applications, freedom to operate and patentability analyses, and due diligence reviews. Prior to joining L&A, Wei worked as an in-house patent agent at Agenus, a pioneer immune-oncology company prior to joining L&A. She also interned at Boehringer Ingelheim and at the Yale University Office of Cooperative Research. Wei received her Ph.D. in cell biology from Yale University. Her doctoral research was supervised by Dr. Peter Cresswell (member of the National Academy of Sciences), and focused on regulation of major histocompatability complex antigen presentation. She received her B.S. in biological science from Peking University, and is a J.D. Candidate (expected 2020) at Suffolk University Law School. Wei is registered to practice before the U.S. Patent and Trademark Office, and she is the lead author of scientific articles published in several journals, including Proceedings of the National Academy of Sciences of the United States of America and Journal of Biological Chemistry. Lando & Anastasi, LLP headquartered in Cambridge, Massachusetts, partners with clients to protect their innovations through effective intellectual property strategies, with an emphasis on creative solutions guided by a solid understanding of each client’s business imperatives. Well versed in a wide range of industries including life sciences, software, cleantech, medical devices, chemical and electrical, L&A attorneys counsel clients ranging from early-stage and venture-backed start-ups to national and global corporations.


SOUTH SAN FRANCISCO, Calif., Feb. 14, 2017 (GLOBE NEWSWIRE) -- Global Blood Therapeutics, Inc. (GBT) (NASDAQ:GBT) today announced that a paper describing the discovery of GBT440 and its ability to bind to hemoglobin and prevent red blood cells from sickling was published online in ACS Medicinal Chemistry Letters, a peer-reviewed publication of the American Chemical Society. GBT440 is in Phase 3 development as a potentially disease-modifying therapy for sickle cell disease (SCD). The publication can be accessed at http://pubs.acs.org/doi/full/10.1021/acsmedchemlett.6b00491. "The underlying cause of SCD is the polymerization of sickle hemoglobin under low oxygen conditions, resulting in red blood cells taking on a sickle-like shape. These sickled cells are unable to pass through narrow blood vessels, resulting in severe painful crises for patients, anemia, multi-organ damage and premature death,” said Ted W. Love, M.D., president and chief executive officer of GBT. “This newly published paper further validates GBT440’s mechanism to increase the affinity of hemoglobin for oxygen and consequently inhibits the polymerization of sickle hemoglobin. As a result, GBT440 has the potential to fundamentally modify the course of SCD, which we are evaluating in our ongoing Phase 3 HOPE Study.” The published paper describes the process by which scientists discovered GBT440. The researchers first developed a series of compounds that increased the oxygen affinity of sickle hemoglobin (HbS) -- both on the isolated hemoglobin protein and in whole blood from sickle cell patients. They then selected compounds that demonstrated the best time to onset of polymerization of HbS. One compound in particular, now known as GBT440, demonstrated favorable pharmacokinetics in several animal species, showing that it could be given orally. Additionally, GBT440 was found to accumulate highly and favorably into red blood cells, suggesting that potentially therapeutic concentrations of GBT440 can be achieved in red blood cells at comparatively low plasma concentrations. About GBT440 in Sickle Cell Disease GBT440 is being developed as an oral, once-daily therapy for patients with SCD. GBT440 works by increasing hemoglobin's affinity for oxygen. Since oxygenated sickle hemoglobin does not polymerize, GBT believes GBT440 blocks polymerization and the resultant sickling of red blood cells. With the potential to restore normal hemoglobin function and improve oxygen delivery, GBT believes that GBT440 may potentially modify the course of SCD. In recognition of the critical need for new SCD treatments, the U.S. Food and Drug Administration (FDA) has granted GBT440 for the treatment of patients with SCD both fast track and orphan drug designations, and the European Commission (EC) has designated GBT440 for the treatment of patients with SCD as an orphan medicinal product. GBT is currently evaluating GBT440 in the HOPE (Hemoglobin Oxygen Affinity Modulation to Inhibit HbS PolymErization) Study, a Phase 3 clinical trial in patients age 12 and older with SCD. Additionally, GBT440 is being studied in the ongoing Phase 1/2 GBT440-001 trial and in an open-label, single and multiple dose study in adolescents (age 12 to 17) with SCD designed to assess the safety, tolerability, pharmacokinetics and exploratory treatment effect of GBT440. About Sickle Cell Disease (SCD) SCD is a lifelong inherited blood disorder caused by a genetic mutation in the beta-chain of hemoglobin, which leads to the formation of abnormal hemoglobin known as sickle hemoglobin (or HbS). In its deoxygenated state, HbS has a propensity to polymerize, or bind together, forming long, rigid rods within a red blood cell (or RBC). The polymer rods deform RBCs to assume a sickled shape and to become inflexible, which can cause blockage in capillaries small blood vessels. Beginning in childhood, SCD patients suffer unpredictable and recurrent episodes or crises of severe pain due to blocked blood flow to organs, which often lead to psychosocial and physical disabilities. This blocked blood flow, combined with hemolytic anemia (the destruction of RBCs), can eventually lead to multi-organ damage and early death. Currently, the only FDA-approved therapy for SCD is hydroxyurea. About Global Blood Therapeutics Global Blood Therapeutics, Inc. is a clinical-stage biopharmaceutical company dedicated to discovering, developing and commercializing novel therapeutics to treat grievous blood-based disorders with significant unmet need. GBT is developing its lead product candidate, GBT440, as an oral, once-daily therapy for sickle cell disease. GBT is also investigating GBT440 for the treatment of hypoxemic pulmonary disorders in two ongoing Phase 2a studies in patients with idiopathic pulmonary fibrosis. To learn more, please visit: www.globalbloodtx.com. Forward-Looking Statements Statements we make in this press release may include statements that are not historical facts and are considered forward-looking within the meaning of Section 27A of the Securities Act of 1933, as amended and Section 21E of the Securities Exchange Act of 1934, as amended. We intend these forward-looking statements, including statements regarding the therapeutic potential and safety profile of GBT440, data and results pertaining to GBT440, our ability to implement our clinical development plans for GBT440, the timing of, and our ability to generate data from our ongoing clinical trials of GBT440 for sickle cell disease, including our ability to enroll patients in, conduct and complete our HOPE Study, to be covered by the safe harbor provisions for forward-looking statements contained in Section 27A of the Securities Act and Section 21E of the Securities Exchange Act and are making this statement for purposes of complying with those safe harbor provisions. These forward-looking statements reflect our current views about our plans, intentions, expectations, strategies and prospects, which are based on the information currently available to us and on assumptions we have made. We can give no assurance that the plans, intentions, expectations or strategies will be attained or achieved, and furthermore, actual results may differ materially from those described in the forward-looking statements and will be affected by a variety of risks and factors that are beyond our control including, without limitation, the risks that our clinical and preclinical development activities may be delayed or terminated for a variety of reasons, that regulatory authorities may disagree with our clinical development plans or require additional studies or data to support further clinical investigation of our product candidates, and that drug-related adverse events may be observed in later stages of clinical development, along with those risks set forth in our Annual Report on Form 10-K for the fiscal year ended December 31, 2015, and in our Quarterly Reports on Form 10-Q for the quarters ended March 31, 2016, June 30, 2016 and September 30, 2016, as well as discussions of potential risks, uncertainties and other important factors in our subsequent filings with the U.S. Securities and Exchange Commission. Except as required by law, we assume no obligation to update publicly any forward-looking statements, whether as a result of new information, future events or otherwise.


News Article | December 27, 2016
Site: www.eurekalert.org

Vanderbilt University scientists have received notification from the U.S. Food and Drug Administration (FDA) that testing in humans may proceed for an investigational new drug for Alzheimer's disease after more than 10 years of research by scientists at Vanderbilt University and Vanderbilt University Medical Center. It is relatively uncharted territory for an academic drug discovery group to take a molecule from the laboratory setting to the clinical trials stage. "The movement to the clinical phase of the research is the result of tireless colleagues reaching across disciplines in pursuit of the shared goal of hoping to someday improve the lives of individuals with Alzheimer's disease and possibly other brain disorders, such as schizophrenia," said Provost and Vice Chancellor for Academic Affairs Susan R. Wente, Ph.D. "This work exactly illustrates the critical role that basic science conducted in partnership with a world-class medical center can play in advancing knowledge in an attempt to fight a devastating disease." For Alzheimer's disease, the aim is for the investigational drug to target major pathologies of the disease and selectively activate a key receptor in the brain. The Vanderbilt researchers believe that the current standard of care for Alzheimer's disease, cholinesterase inhibitors, has a different mechanism of action. They are hoping to establish through future clinical testing that the molecule is broadly effective across a number of cognitive and neuropsychiatric disorders, including schizophrenia. "This is the first instance I am aware of where an academic drug discovery group moved a molecule designed to hopefully treat a chronic brain disorder all the way from early discovery to human trials without there being, at some point along the way, a pharmaceutical partner," said P. Jeffrey Conn, Ph.D., Lee E. Limbird Professor of Pharmacology in the Vanderbilt University School of Medicine and director of the Vanderbilt Center for Neuroscience Drug Discovery (VCNDD). "And that really is crossing what people refer to all of the time as the 'Valley of Death,' where good research discoveries have a hard time moving into the clinical testing phase due to lack of funding," he said. "Importantly, at this early stage, the FDA has only granted permission to assess potential safety of this investigational new drug in healthy volunteers" said Conn. "We cannot predict the outcome, but if these studies are successful in demonstrating that the investigational drug can be safely administered to humans, this would pave the way to allow filing of additional applications with the FDA to seek permission to advance to testing for efficacy in improving cognitive function in patients suffering from Alzheimer's disease, and possibly schizophrenia or other brain disorders. While we cannot predict the outcome of any future safety or efficacy studies, this decision by FDA allowing clinical research to begin represents a major milestone in allowing us to hopefully provide answers to those critical questions in the future." VCNDD Co-Director Craig W. Lindsley, Ph.D., director of Medicinal Chemistry and William K. Warren, Jr. Professor of Medicine, said Phase I testing will assess drug safety and tolerability in healthy volunteer participants, a process that could take a year. If successful, the Phase II and III studies would include efficacy assessments in patients with Alzheimer's disease and could take three to five years to complete. "We are hoping to address what we see as an unmet medical need," Lindsley said. "For Alzheimer's patients, the standard of care for symptomatic treatment remains cholinesterase inhibitors, which are 25 years old at this point. There hasn't been any real scientific advancement in this field in a long time." Lindsley and Conn credit The William K. Warren Foundation for its philanthropic investments along the way to make clinical trials for this investigational drug a reality. "One of the most challenging things about doing this in an academic environment is funding," Lindsley said. "Every step requires funding and if there is a delay or break in funding, then everything sits idle and potentially innovative approaches for patient care do not advance." "Being matched with the Warrens happened serendipitously. They have invested so much in our programs, and it is wonderful to show them progress on their investments," he said. "Without the financial support from the Warrens, this investigational drug would not be poised to enter human clinical trials." The William K. Warren Foundation Chief Executive Officer John-Kelly Warren said he is gratified that FDA has allowed for the investigational drug to proceed to testing in human beings. "Although this is an important sequential milestone, the only milestone that matters to us is the hope that one day we will learn that this investigational new drug has positively and safely changed the life of a patient suffering from a brain disorder such as schizophrenia or Alzheimer's disease," Warren said. "That day will warrant a celebration felt in the heavens. Until then, we are prepared to support the VCNDD research team until they can deliver the necessary results," he said. A NIH National Cooperative Drug Discovery/Development grant funded the early basic science and discovery of this investigational drug and the Alzheimer's Drug Discovery Foundation and Harrington Discovery Institute helped support some of the key toxicity studies that FDA required, Conn said. "The investigational new drug has the potential to improve cognitive functions with fewer unwanted side effects. This could someday be an important advance for the treatment of cognitive deficits in psychiatric disorders and Alzheimer's disease," said Joshua Gordon, M.D., Ph.D., director of the National Institute of Mental Health, which co-funded the research. Conn and Lindsley said Vanderbilt's "team science" approach included contributions from the director of Translational Pharmacology and Development for the VCNDD and Assistant Professor Carrie K. Jones, Ph.D., who coordinated the IND drafting, submission, and subsequent development into Phase I, director of Molecular Pharmacology for the VCNDD and Research Associate Professor of Pharmacology Colleen Niswender, Ph.D., for the molecular pharmacology; Research Assistant Professor of Pharmacology Jerri Rook, Ph.D., for the behavioral studies; and Research Assistant Professor of Pharmacology Thomas Bridges, Ph.D., and Research Assistant Professor of Pharmacology Anna Blobaum, Ph.D., for drug metabolism and pharmacokinetic profiling. Paul Newhouse, M.D., director of the Center for Cognitive Medicine at VUMC and Jim Turner Professor in Cognitive Disorders, is expected to lead the upcoming clinical study funded in part by the Alzheimer's Association and Alzheimer's Drug Discovery Foundation.


News Article | March 2, 2017
Site: www.eurekalert.org

This research article by Dr. Rita Mahanta et al has been published in Cardiovascular & Hematological Agents in Medicinal Chemistry Investigations by researchers of Zoology Department of Cotton College, Guwahati, and Gauhati University, Guwahati, Assam, India, have revealed that long term exposure to elevated doses of Anabolic Androgenic Steroids (AAS) can significantly affect aldosterone concentration and serum sodium/ potassium levels in albino mice. The research led by Dr. Rita Mahanta, Associate Professor (Retd.) in the Department of Zoology, Cotton College, Guwahati and Ph.D. student, Parmita Chowdhury from Gauhati University, Zoology Department, have discovered that prolonged administration of Nandrolone Decanoate, an AAS, upon a group of male albino mice significantly increased serum aldosterone and sodium ion levels when compared with a group of albino mice that did not receive such treatment. Post treatment alterations were also revealed through measuring the level of potassium ion but this change was reported to be insignificant. This study, published in the journal Cardiovascular and Hematological Agents in Medicinal Chemistry (Bentham Science), volume 14, issue 3, further emphasizes that a change of this kind where a marked increase in aldosterone levels occurred upon chronic exposure to Nandrolone Decanoate could be a possible indication of steroid related cardiovascular disorders as a number of literatures are available that support the correlation between aldosterone concentration and cardiovascular diseases. For more information about this article, please visit http://benthamscience.


News Article | November 17, 2016
Site: www.nanotech-now.com

Abstract: Three-dimensionally Functionalized Reverse Phase Glycoprotein Array for Cancer Biomarker Discovery and Validation Li Pan1, Hillary Andaluz Aguilar2, Linna Wang3, Anton Iliuk3,4, and W. Andy Tao1,2,3,4,5 1 Department of Medicinal Chemistry & Molecular Pharmacology 2 Department of Chemistry 3 Department of Biochemistry, Purdue University, West Lafayette, IN 4 Tymora Analytical Operations, West Lafayette, IN 5 Center for Cancer Research, Purdue University, West Lafayette, IN Glycoproteins have vast structural diversity which plays an important role in many biological processes and have great potential as disease biomarkers. Here we report a novel functionalized reverse phase protein array (RPPA), termed polymer-based reverse phase GlycoProtein Array (polyGPA), to specifically capture and profile glycoproteomes, and validate glycoproteins. Nitrocellulose membrane functionalized with globular hydroxyaminodendrimers was used to covalently capture pre-oxidized glycans on glycoproteins from complex protein samples such as biofluids. The captured glycoproteins were subsequently detected using the same validated antibodies as in RPPA. We demonstrated the outstanding specificity, sensitivity, and quantitative capabilities of polyGPA by capturing and detecting purified as well as endogenous alpha-1-acid glycoprotein (AGP) in human plasma. We further applied quantitative N-glycoproteomics and the strategy to validate a panel of glycoproteins identified as potential biomarkers for bladder cancer by analyzing urine glycoproteins from bladder cancer patients or matched healthy individuals. A Purdue University biochemist has developed a novel method for detecting certain types of proteins that serve as indicators for cancer and other diseases. Glycoproteins are formed when sugars attach to and modify a protein. In some cases, a combination of glycoproteins present in a sample of blood or urine could be an indicator of disease or cancer. But those glycoproteins can be elusive. There has been no antibody to differentiate between them and regular proteins. And the complex and bulky sugar groups can make it difficult for even standard protein-detection antibodies to find their targets. W. Andy Tao, a Purdue professor of biochemistry, has developed a novel protein array, a high throughput platform to analyze multiple proteins in parallel, for separating glycoproteins from unmodified proteins. Tao also demonstrated its effectiveness for identifying glycoproteins associated with bladder cancer. The findings were published Monday (Nov. 14) in the Journal of the American Chemical Society. Tao developed a nano-sized polymer, called polyGPA, that attaches to the sugar groups of glycoproteins and brings them to the surface of the protein array. The nanopolymer also repositions the glycoprotein so that the antibodies used to detect unmodified proteins can better reach their targets. "There are many sugar types and combinations. Sugar modification can be a very important indication of disease state," Tao said. "A panel of proteins modified by sugars may be an indication of a particular disease." Tao said tests showed his method is 17 times to 25 times more likely to identify proteins that might have otherwise been missed in regular testing procedures. He was also able to identify glycoproteins associated with bladder cancer in a urine sample. "It is possible to use our platform to identify these sugar-modified proteins as a biomarker for bladder cancer," Tao said. Tao will work to commercialize his nanopolymer-modified protein array through his company, Tymora Analytical Operations, which operates in the Purdue University Research Park. The company makes the pIMAGO nanopolymer, which can be used to determine whether cancer drugs have been effective against biochemical processes that can lead to cancer cell formation, and polyMAC, a nanopolymer that helps scientists retrieve and study proteins that are undergoing processes related to cancer cell formation. For more information, please click If you have a comment, please us. Issuers of news releases, not 7th Wave, Inc. or Nanotechnology Now, are solely responsible for the accuracy of the content.


News Article | February 28, 2017
Site: www.eurekalert.org

The aim of the present article is to compare the structural features of a particular group of pyridoxal 5'-phosphate-dependent decarboxylases, namely the group II ?-decarboxylases. These enzymes are: aromatic amino acid, cysteine sulfinic acid, glutamate and histidine decarboxylases. They are involved in the synthesis of dopamine/serotonin, hypotaurine, ?-aminobutyric acid and histamine, respectively, molecules known to play essential biological roles. Dopamine and serotonin as well as ?-aminobutyric are essential neurotransmitters, histamine and hypotaurine play several roles in many physiological and pathological processes. Despite a common fold-type, these decarboxylases have evolved specific structural elements responsible for their unique substrate preference. The effort of this review is to combine a literature update with bioinformatic analyses in order to point out the determinants of the structural basis for substrate specificity as well as the importance of some residues/regions for the catalytic competence. We find that all of them share a mobile catalytic loop, and that two of them (aromatic amino acid and glutamate decarboxylases) undergo an open-to-close conformational change when the coenzyme binds to the protein moiety in the so-called apo-to-holo transition. Drawing attention on these elements is crucial in correlating subtle structural modifications to functional properties for the understanding, at a molecular level, of a pathological condition. For example, residues of the mobile loop as well as those involved in the apo-to-holo transition could be considered preferential targets for planning aimed drug-design or for developing a pharmacological chaperone approach. This represents an urgent task given the increasingly important role played by these decarboxylases in several different pathological states: autoimmune diseases, type I diabetes, Parkinson's disease, aromatic amino acid decarboxylase deficiency, Tourette's syndrome and cholangiocarcinoma. Thus, this research approach is of topical interest in the purpose of fine tuning the therapy for different diseases. For more information about the article, please visit: http://www. Reference: Paiardini, A.; (2017). New Insights Emerging from Recent Investigations on Human Group II Pyridoxal 5'-Phosphate Decarboxylases. Current Medicinal Chemistry., DOI: 10.2174/0929867324666161123093339


- Incoming Industry Veteran to Lead Clinical Supply Chain Operations and Architect the Build Out of the Anticipated Commercial Supply Chain NEW YORK, Oct. 31, 2016 (GLOBE NEWSWIRE) -- Actinium Pharmaceuticals, Inc. (NYSE MKT:ATNM) ("Actinium" or "the Company"), a biopharmaceutical Company developing innovative targeted payload immunotherapeutics for the treatment of advanced cancers, announced today the appointment of Bernie Cunningham, Ph.D, to the position of Executive Director of Clinical Supply Chain and Logistics, and CMC Project Management. This new hire will report to Kaushik J. Dave, Ph.D, Actinium’s Chief Executive Officer, as a keystone hire in the Company’s growing Supply Chain Team. “We are enormously gratified to welcome Dr. Cunningham to the Actinium Pharmaceuticals team,” said Kaushik J. Dave, Ph.D, Actinium’s Chief Executive Officer. “The hiring of such a skilled and experienced executive shortly after onboarding Dr. Maria Nunes and Ms. Laura Chen reinforces my confidence in our ability to attract requisite talent as we continue to perfect pre-commercialization capabilities for our phase 2 and phase 3 programs, increase readiness for commercialization and also prepare for pipeline expansion.” Dr. Cunningham will have a leadership role, responsible for further establishment of the Company’s supply chain infrastructure and related distribution strategies, all of which will provide critical support to clinical operations both in the United States and outside the United States. She will also oversee Actinium’s relationships with external contract manufacturing organizations and contract testing labs for all clinical trial material supplies. Dr. Cunningham has approximately thirty years of experience in the pharmaceutical and biotechnology industries, with a dedication to supply chain and project management within the last fifteen years. As a Certified Project Management Professional she brings extensive experience in development of investigational medical products in various physical forms. She led teams and directed multiple projects in manufacturing, supply chain and QA/QC at companies including Mesoblast and OSI Pharmaceuticals. She began her professional career as a Research Scientist and Principal Investigator at OSI Pharmaceuticals, and most recently had the title of Director, Project Management – Manufacturing and QA at Mesoblast. Dr. Cunningham holds a Ph.D. in Medicinal Chemistry from University of Aston in Birmingham, U.K., as well as a BSc (Hons) from University of Aston, and has written a number of papers published in peer-reviewed pharmacology journals. Actinium Pharmaceuticals, Inc. (www.actiniumpharma.com) is a New York-based biopharmaceutical company developing innovative targeted payload immunotherapeutics for the treatment of advanced cancers. Actinium's targeted radioimmunotherapy products are based on its proprietary delivery platform for the therapeutic utilization of alpha-emitting Actinium-225 and Bismuth-213 and certain beta emitting radiopharmaceuticals in conjunction with monoclonal antibodies. The Company's lead radiopharmaceutical product candidate Iomab-B is designed to be used, upon approval, in preparing patients for hematopoietic stem cell transplant, commonly referred to as bone marrow transplant. The Company is conducting a single, pivotal, multicenter Phase 3 clinical study of Iomab-B in refractory or relapsed AML patients over the age of 55 with a primary endpoint of durable complete remission. The Company's second product candidate, Actimab-A, is continuing its clinical development in a Phase 1/2 trial for patients newly diagnosed with AML over the age of 60 in a single-arm multicenter trial. This news release contains "forward-looking statements" as defined in the Private Securities Litigation Reform Act of 1995. These statements are based on management's current expectations and involve risks and uncertainties, which may cause actual results to differ materially from those set forth in the statements. The forward-looking statements may include statements regarding product development, product potential, or financial performance. No forward-looking statement can be guaranteed and actual results may differ materially from those projected. Actinium Pharmaceuticals undertakes no obligation to publicly update any forward-looking statement, whether as a result of new information, future events, or otherwise.

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