
GLP-1 Treatment for Diabetes and Beyond
Tuesday, December 8, 2015
The launch of GLP-1 receptor agonists almost 10 years ago greatly improved the treatment options for type 2 diabetes. Currently, four GLP-1 receptor agonists are available as injectable treatments: Byetta (twice-daily), Bydureon (once-weekly), Victoza (once-daily) and Lyxumia (once-daily). This class of drug has received much attention based on its unique mechanism of action and pleiotropic effects. The GLP-1 receptor agonists potentiate insulin secretion, inhibit glucagon secretion, delay gastric emptying and reduce appetite thereby they not only improve glycemic control, but also induce weight loss. Despite the demonstrated efficacy of GLP-1 receptor agonists in lowering HbA1c, significant challenges remain as over one third of patients fail to reach target HbA1c goals. The promise of beneficial effects on pancreatic b-cell health and cardioprotection have proved challenging to show in the clinic and the translatability of these pleiotropic actions remains controversial. In addition, novel insights suggesting that GLP-1 receptor agonists are neuroprotective have spurred a number of clinical trials for the treatment of neurodegenerative disorders, including Alzheimer's disease. This symposium highlights emerging science for GLP-1 in the preclinical and clinical arena focusing on human genetics, novel cellular and molecular mechanisms for insulin secretion and weight loss, new indications and opportunities for drug development.
*Reception to follow.
Call for Poster Abstracts
Abstract submissions are invited for a poster session, and two abstracts will be selected for late breaking short talks. For complete submission instructions, please send an email to GLP-1@nyas.org with the words "Abstract Information" in the subject line. The deadline for abstract submission is November 20, 2015.
This event will also be broadcast as a webinar; registration is required.
Please note: Transmission of presentations via the webinar is subject to individual consent by the speakers. Therefore, we cannot guarantee that every speaker's presentation will be broadcast in full via the webinar. To access all speakers' presentations in full, we invite you to attend the live event in New York City when possible.
Registration Pricing
Member | $60 |
Student / Postdoc Member | $25 |
Nonmember (Academia) | $105 |
Nonmember (Corporate) | $160 |
Nonmember (Non-profit) | $105 |
Nonmember (Student / Postdoc / Resident / Fellow) | $70 |
Webinar Pricing
Member | $30 |
Student / Postdoc Member | $15 |
Nonmember (Academia) | $65 |
Nonmember (Corporate) | $85 |
Nonmember (Non-profit) | $65 |
Nonmember (Student / Postdoc / Resident / Fellow) | $45 |
The Biochemical Pharmacology Discussion Group is proudly supported by
American Chemical Society
Agenda
* Presentation times are subject to change.
Tuesday, December 8, 2015 | |
8:30 AM | Registration and Continental Breakfast |
9:00 AM | Opening Remarks |
Session 1: GLP-1 and the Treatment of Diabetes | |
9:15 AM | Novel Insights into GLP-1R Agonist Enhancement of Glucose-stimulated Insulin Secretion |
9:45 AM | Critical Appraisal of the Evidence for GLP-1 Analogues in Improving β-Cell Health |
10:15 AM | Next Generation GLP-1 Agonists - Examples of Dual Strategies |
10:45 AM | Networking Coffee Break |
11:15 AM | GLP-1R Mechanisms for the Treatment of Obesity |
Session 2: Late Breaking Data Presentations | |
11:45 AM | Pharmacological Analysis of Novel Biased Peptide Agonists of the Human Glucagon-like Peptide 1 Receptor |
12:00 PM | Sustained Release Formulation of Exenatide for the Treatment of Traumatic Brain Injury |
12:15 PM | Networking Lunch and Poster Session |
Session 3: Extrapancreatic Effects of GLP-1 and New Therapeutic Opportunities | |
1:30 PM | Neuroanatomical Mechanisms Mediating Central GLP-1 Effects on Energy Balance |
2:00 PM | Chemical Biotechnology Applied to Metabolic Diseases |
2:30 PM | GLP-1 and Dual GLP-1/GIP Receptor Agonists as Promising Therapeutics in Alzheimer's Disease |
3:00 PM | Coffee Break |
3:30 PM | Preclinical Evidence for Glucagon-Like Peptide-1 Receptor Agonist Induced Cardioprotection: Evidence for Improving Cardiac Metabolic Efficiency |
4:00 PM | Signal Bias and Allosterism at the GLP-1R: Implications for Small Molecule GLP-1R Agonists |
4:30 pm | Closing Remarks |
4:40 PM | Networking Reception |
5:40 PM | Adjourn |
Speakers
Organizers
Mercedes Beyna, MS
Biogen
Margaret Jackson, PhD
Pfizer
J. Brent Kuzmiski, PhD
Pfizer
Dr. Brent Kuzmiski is a Principal Scientist in Worldwide Research and Development at Pfizer located in Cambridge Massachusetts. Brent was trained as a neuroscientist and obtained his PhD from the University of Calgary, Canada. In 2011, Brent joined the Cardiovascular & Metabolic Disease Research Unit where his research focuses on the central nervous system regulation of metabolism and the development of drugs for the treatment of obesity and diabetes.
Sonya Dougal, PhD
The New York Academy of Sciences
Speakers
David D'Alessio, MD
Duke University
Dr. D’Alessio is Professor of Medicine at the Duke University School of Medicine and Director of the Division of Endocrinology. He is a staff physician at the Durham VA Medical Center where he has consultative practices in the lipid and the endocrinology clinics. Dr. D’Alessio has a primary research interest in the regulation of glucose tolerance and abnormalities that lead to type 2 diabetes. Work in his lab is directed at the interplay between circulating glucose, GI hormones and neural signals to control insulin secretion with a primary focus on the gut peptide GLP-1 and its role in normal physiology, type 2 diabetes and bariatric surgery.
Richard DiMarchi, PhD
Indiana University
Dr. DiMarchi contributions in peptide & protein sciences consists of three decades of work in academia, the pharmaceutical industry and biotechnology companies. He is the Cox Distinguished Professor of Biochemistry and Gill Chair in Biomolecular Sciences at Indiana University. He is a co-founder of Ambrx, Inc., Marcadia Biotech, Assembly, Calibrium and MB2 Biotech. He has served as a scientific advisor to multiple pharmaceutical companies and three venture funds; 5AM, TMP, and Twilight. He is Chairman of the Peptide Therapeutics Foundation and external board member at Assembly Biosciences and On-Target Therapeutics. Dr. DiMarchi is a retired Group Vice President at Eli Lilly & Company where for more than two decades he provided leadership in biotechnology, endocrine research and product development. He is readily recognized for discovery and development of rDNAderived Humalog® (LisPro-human insulin). As scientist and executive, Dr. DiMarchi also significantly contributed to the commercial development of Humulin®, Humatrope®, rGlucagon®, Evista®, and Forteo®. His current research is focused on developing macromolecules with enhanced therapeutic properties through biochemical and chemical optimization, an approach he has termed chemical-biotechnology. Dr. DiMarchi is the recipient of numerous awards including the 2005 AAPS Career Research Achievement Award in Biotechnology, the 2006 ACS Barnes Award for Leadership in Chemical Research Management, the 2006 ACS Esselen Award for Chemistry in the Service of Public Interest, the 2007 Carothers Award for Excellence in Polymer Sciences, the 2009 Watanabe Award for Life Sciences Research, the 2011 Merrifield Award for Career Contributions in Peptide Sciences, the 2012 Phillip Nelson Innovation Award, the 2014 Erwin Schrödinger-Preis, a 2014 inductee to the National Inventors Hall of Fame, the 2015 awardee of the Meienhofer Prize, the 2016 ACS Alfred Burger Award in Medicinal Chemistry and a 2016 inductee to the National Academy of Medicine.
Jean-Philippe Fortin, PhD
Pfizer Global
Dr. Jean-Philippe Fortin is a drug discovery biologist focused on the molecular and cellular pharmacology of G protein-coupled receptors (GPCRs). He received his PhD in Experimental Medicine in 2006 from Laval University, Canada, and completed his post-doctoral training at Tufts University in Boston. He is currently Principal Scientist and Lab Head within Pfizer’s Cardiovascular and Metabolic Disorders Research Unit located in Cambridge, Massachusetts. His research aims at building deep pharmacology knowledge around receptors involved in the control of metabolism, as well as designing innovative translational screening strategies to enable the discovery of safe and efficacious orthosteric and allosteric GPCR modulators.
Keld Fosgerau, PhD
Zealand Pharma A/S
Keld Fosgerau (Danish, born 1969) joined Zealand in 2010 as Director of Pharmacology and became Vice President and Head of Research in 2013. Keld is temporarily acting as Senior Vice President for Research. For the last 18 Years, Keld Fosgerau has worked in the pharmaceutical industry including 10 years at Novo Nordisk in the search for novel drug targets and early lead development especially in the field of cardio-metabolism including obesity and diabetes, and has participated in several drug candidate projects entering the clinical stages. Moreover he has worked as research manager in biotech companies such as Rheoscience and Neurokey. Keld obtained his PhD in 2000 from University of Copenhagen, Denmark and University of Southern California, US in regulation of hepatic glycogen metabolism. Keld Fosgerau is a physiologist and pharmacologist by training with mathematical modelling of physiological systems as a major focus, and the author of more than 70 publications, published conference reports and patent applications.
Matthew R. Hayes, PhD
Perelman School of Medicine, University of Pennsylvania
Matt Hayes is an Assistant Professor of Nutritional Neuroscience, and Associate Director of the Translational Neuroscience Program in the Department of Psychiatry, Perelman School of Medicine at the University of Pennsylvania. Dr. Hayes earned his PhD in Nutritional Sciences from The Pennsylvania State University and conducted his postdoctoral fellowship in psychology and neuroscience at The University of Pennsylvania. His current NIH-funded research examines the neuroendocrinology of energy balance control using rodent models. In particular, the Hayes lab focusses their research efforts extensively on understanding the neural, behavioral, cellular, molecular, and physiological mechanisms by which hormones, such as glucagon-like peptide-1, amylin, and leptin regulate food intake and body weight through action in the mesolimbic reward system and caudal brainstem. In addition, the Hayes lab is also examining whether these energy balance-relevant neuroendocrine signaling pathways play a critical role in modulating drug taking and seeking using rodent models. These basic science research efforts are conducted with the intention that they will translate into improved pharmacological / behavioral treatments for obesity, diabetes, drug abuse and co-morbid diseases.
George G. Holz, PhD
State University of New York
Dr. Holz is a Molecular Pharmacologist and Cell Physiologist currently based at the State University of New York (SUNY) Upstate Medical University in Syracuse, NY where his faculty titles include those of New York State Empire Scholar and also Professor of Medicine and Pharmacology. Dr. Holz was a New York State Regent's Scholar at Cornell University (BS) and his PhD degree in Pharmacology was awarded by the University of Illinois College of Medicine in 1984. He has been actively engaged in studies of GLP-1 since 1990 at which time he served as an HHMI postdoc and a Harvard Medical School Assistant Professor working in the Laboratory of Molecular Endocrinology and Diabetes Unit at Massachusetts General Hospital. Prior to moving to SUNY in 2008, he spent ten years at New York University School of Medicine where as an Associate Professor of Physiology, Neuroscience, and Pharmacology he assembled an NIH and ADA funded team of scientists to investigate novel aspects of GLP-1 action in pancreatic beta cells. Presently, his laboratory's research interests revolve around drug development for the treatment of type 2 diabetes and obesity.
Beat Jucker, PhD
GlaxoSmithKline
Beat M. Jucker, PhD, is head of the US Preclinical & Translational Imaging (PCTI) group within the Platform Technology Sciences group at GlaxoSmithKline located in King of Prussia, PA. At GlaxoSmithKline, he initially supported preclinical imaging and metabolic phenotyping studies in the Cardiovascular and Urogenital Center of Excellence for Drug Discovery from 2001-2008 followed by leading a combined Imaging and Integrated Pharmacology group within the Heart Failure Discovery Performance Unit from 2008-2011. Currently as head of US PCTI (2011-present), his group supports the various preclinical, in vivo imaging needs of drug discovery, safety assessment, DMPK, etc. There is a strong emphasis within the group on developing PD readouts for clinical translation which has been applied to numerous therapeutic areas (i.e. Oncology, Cardiovascular, Respiratory, and Inflammation, musculoskeletal). His expertise includes using multi-modality imaging technologies to probe in vivo integrated physiology (i.e. hemodynamics, metabolism, anatomy) and drug biodistribution and pharmacodynamics in animals.
Dong Seok Kim, PhD
National Institute on Aging / Peptron Inc
Dong Seok Kim is a biochemist with special interest in Immunology and Neuroscience. He holds PhD degree in Biochemistry, specializing in integrin signaling in the tumor environment from Yonsei University, Seoul, Korea. His research focused on the ubiquitin-mediated regulation of protein expression during T cell activation in National Cancer Institute, Bethesda MD. He joined Peptron in 2012 to lead a research team for the peptide-based new drug development. He is currently working on the development of GLP-1 agonists, especially sustained release formulation of exenatide, for the treatment of neurodegenerative diseases as a guest scientist in National Institute on Aging in Blatimore MD.
Lotte Bjerre Knudsen, DMSc
Novo Nordisk
Lotte Bjerre Knudsen is a Scientific Vice President in Global Research at Novo Nordisk in Denmark. Lotte Bjerre Knudsen is a chemist by training, has a doctoral degree in scientific medicine and has worked for Novo Nordisk for 25 years. Lotte Bjerre Knudsen is a recognised expert of GLP-1 based drug discovery and mechanism of action studies in diabetes, obesity and toxicology. Her research focuses on drug discovery, receptor expression, molecular pharmacology, In vivo pharmacology, mechanistic toxicology and mechanism of action of drugs in obesity and diabetes, and has resulted in 60 peer-reviewed original papers.
Patrick M. Sexton, PhD
Monash University
Patrick Sexton is a leading international researcher in the field of G protein-coupled receptors (GPCRs), and in particular with respect to allosteric modulation of receptors, ligand-directed signal bias and in the structure/function of Class B GPCRs and accessory proteins. His research crosses industry and academic boundaries through elucidation of fundamental biology and the intersection of this with drug-receptor interactions. He has authored over 200 publications, with major contributions to understanding of the distribution of receptors, the structural interface between peptide ligands and receptors, modulation of receptors by accessory proteins, detection and quantification of small molecule allosteric drug effects and ligand-biased signalling. He is a 2014 Thomson Reuters highly cited researcher in Pharmacology and Toxicology.
Konrad Talbot, PhD
Cedars-Sinai Medical Center
Dr. Konrad Talbot is a neurobiologist who has been studying the molecular basis of Alzheimer’s disease (AD) and schizophrenia for nearly twenty years. He received his PhD in behavioral neuroscience from UCLA in 1989. After serving as an Assistant Professor at Mount St. Mary’s College and later St. Olaf College, he began postdoctoral training in neurodegenerative disease research in the Department of Pathology and Laboratory Medicine at the University of Pennsylvania (1997-2001). Dr. Talbot later served there as a senior research investigator (2001-2007) and faculty member (2008-2012) in the Department of Psychiatry. Between 2006 and 2012, he and his coworkers established the existence, cause, and cognitive correlates of brain insulin resistance in AD. In 2013, Dr. Talbot joined the AD research faculty at Cedars-Sinai Medical Center in Los Angeles, where he was appointed Associate Professor in 2014. His work is now focused on developing treatments of AD using agonists of receptors for the incretins GLP-1 and GIP, which can markedly reduce brain insulin resistance. Dr. Talbot’s work has been supported by the Alzheimer’s Association and NIH and has been published in such leading journals as Nature Medicine, the Proceedings of the National Academy, and the Journal of Clinical Investigation.
Sponsors
Promotional Partners
Nutrition Obesity Research Center
The Biochemical Pharmacology Discussion Group is proudly supported by
American Chemical Society
Abstracts
Novel Insights into GLP-1R Agonist Enhancement of Glucose-Stimulated Insulin Secretion
George G. Holz, PhD, State University of New York
Is GLP-1 a Hormone: Whether and when?
David D'Alessio, MD, Duke University
Next Generation GLP-1 Agonists – Examples of Dual Strategies
Keld Fosgerau, PhD, Zealand Pharma A/S
GLP-1R Mechanisms for the Treatment of Obesity
Lotte Bjerre Knudsen, DMSc, Novo Nordisk
Pharmacological Analysis of Novel Biased Peptide Agonists of the Human Glucagon-like Peptide 1 Receptor
Jean-Philippe Fortin1
Coauthors: Joseph-Brent Kuzmiski, Barbara Bernardo, Richard Derksen, Jocelyn E. Manning Fox, Patrick MacDonald, David Edmonds, David Tess, Cindy Li, Paula Loria, Amit Kalgutkar, Meg Landis, Lucy Rogers, Chris Limberakis, Alan Mathiowetz, Dan Lettiere, Heather Eng, David Price, Margaret Jackson and David Griffit
1 Pfizer Worldwide Research and Development, Cardiovascular and Metabolic Diseases Research Unit, Pfizer Inc. Cambridge, MA, USA
Sustained Release Formulation of Exenatide for the Treatment of Traumatic Brain Injury
Dong Seok Kim, PhD1,2
Coauthors: Yazhou Li PhD1, Ian Tamargo1, Hee Kyoung Kim2, David Tweedie PhD1, Chaim G. Pick PhD3, Lital Rachmany3, Heeyong Lee PhD2 , Barry Hoffer MD/PhD4 and Nigel H Greig PhD1
1 National Institute on Aging, Baltimore, MD
2 Peptron Inc., Daejeon, Korea
3 Tel Aviv university, Israel
4 Case Western Reserve University, Cleveland, OH
Neuroanatomical Mechanisms Mediating Central GLP-1 Effects on Energy Balance
Matthew R. Hayes, PhD, Perelman School of Medicine, University of Pennsylvania
Chemical Biotechnology Applied to Metabolic Diseases
Richard DiMarchi, PhD, Indiana University
References
- “A Rationally Designed Peptide of Triple Gut Hormone Action Cures Obesity and Diabetes” Nature Medicine (2015), 21:27-36
- “Chemical Synthesis of Insulin Analogs Through a Novel Precursor” ACS Chem. Biol., (2014), 9:683
- “Break on Through to the Other 1” Cell Metabolism (2014), 20:554
- “Unimolecular Dual Incretins Maximize Metabolic Benefits in Rodents, Monkeys, and Humans” Sci. Trans. Med. (2013), 5:209
- “Targeted Estrogen Delivery Reverses The Metabolic Syndrome” Nature Medicine Nature Medicine (2012), Volume:18:1847
- FGF21 Analogs of Sustained Action Enabled by Orthogonal Biosynthesis Demonstrate Enhanced Antidiabetic Pharmacology in Rodents, Diabetes (2012), 61(2), 505-12.
GLP-1 and Dual GLP-1/GIP Receptor Agonists as Promising Therapeutics in Alzheimer’s Disease
Konrad Talbot, PhD, Cedars-Sinai Medical Center
Preclinical Evidence for Glucagon-Like Peptide-1 Receptor Agonist Induced Cardioprotection: Evidence for Improving Cardiac Metabolic Efficiency
Beat M. Jucker, PhD1,2
Coauthors: Weike Bao, MD, PhD1, Karpagam Aravindhan, PhD1, Hasan Alsaid, PhD2, Thimmaiah Chendrimada, PhD1, Lucy J. Holt, PhD3, Elena DeAngelis, PhD3, Mathew Szapacs, PhD4, Mark R. Harpel, PhD1, Larry Jolivette, PhD1, Robert N. Willette, PhD1, John J. Lepore, MD1
1 Heart Failure Discovery Performance Unit, Metabolic Pathways and Cardiovascular Therapy Area Unit
2 Preclinical and Translational Imaging, Platform Technology
3 Innovation BDU, Biopharm Research
4 DMPK, Platform Technology and Science, GlaxoSmithKline, King of Prussia, Pennsylvania, United States
Signal Bias and Allosterism at the GLP-1R: Implications for Small Molecule GLP-1R Agonists
Patrick Sexton, PhD, Monash University
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