Rob M Jones 
New Therapeutic Strategies for Type 2 Diabetes 
Small Molecule Approaches

The diabetes mellitus epidemic is unfolding across the globe with the World Health Organization (WHO) reporting a worldwide prevalence of 177 million patients with diabetes. Type 2 diabetes accounts for approximately ninety percent of all diabetes cases. Long-term complications of type 2 diabetes include atherosclerosis, heart disease, stroke, end-stage renal disease, retinopathy leading to blindness, nerve damage, sexual dysfunction, frequent infections, and difficult-to-treat foot ulcers, sometimes resulting in lower limb amputation. Diabetics are twice as likely to develop cardiovascular disease or have a stroke, two to six times more likely to have transient ischemic attacks, and fifteen to forty times more likely to require lower-limb amputation compared with the general population. In 2002, the total economic cost of diabetes was estimated to be $132 billion accounting for one in every ten health care dollars spent in the United States. As a direct consequence of this economic impact and in light of the fact that current approved therapies fail to provide adequate therapeutic advantage in preventing hyperglycemia, industry has been heavily focused on addressing new fundamental cellular mechanisms that will potentially address this unmet need. New Therapeutic Strategies for Type 2 Diabetes provides the reader with the most comprehensive survey to-date of the most innovative small molecule research strategies targeted at treating the burgeoning type 2 diabetes epidemic. Each chapter is written by a recognised thought-leader in this field. The book will be an invaluable reference for researchers and medicinal chemists that concisely explains the biological mechanisms underpinning each cutting-edge therapeutic strategy along with key medicinal chemistry rationales and up-to- date clinical findings.

Tabela de Conteúdo

Preface, Type 2 Diabetes – Disease Overview; Marketed Small Molecule Dipeptidyl Peptidase IV (DPP4) Inhibitors as a New Class of Oral Anti-diabetics; SGLT2 Inhibitors in Development; Glucokinase Activators in Development; 11 -Hydroxysteroid dehydrogenase type 1 (11 -HSD1) inhibitors in development; Recent Advances in PTP1B Inhibitor Development for the Treatment of Type-2 Diabetes and Obesity; Recent advances in the discovery of GPR119 agonists; Acyl-Co A:diacylglycerol acyltransferase-1 inhibition as an approach to the treatment of type 2 diabetes; Stearoyl-Co A Desaturase 1 (SCD1) Inhibitors: Bench to Bedside Must Only Go through Liver; TGR5 Agonists in Development; The discovery and development of MB07803, a second generation fructose-1, 6-bisphosphatase inhibitor with improved pharmacokinetic properties, as a potential treatment of type 2 diabetes; Inhibition of Glycogen Phosphorylase as a Strategy for the Treatment of Type 2 Diabetes; SIRT1 Activators in Development; Long-Chain Free Fatty Acid Receptor Agonists; Glucagon Receptor Antagonists in Development; ACC Inhibitors in Development; Index

Sobre o autor

Robert M. Jones is currently Senior Director of Medicinal Chemistry at Arena Pharmaceuticals and also serve as Adjunct Faculty to the University of Mississippi, Department of Medicinal Chemistry. He has been an active medicinal chemistry researcher for the past 16 years, 13 of which have been in industry. Over the past 8 years his research has focused on metabolic diseases in particular Type 2 Diabetes. His work has led to several compounds entering or being nominated for clinical development, including a first in class GPR119 agonist for T2D. He has also been cited as an inventor of ~ 63 patents / provisional filings; and has published ~ 60 manuscripts and abstracts in the field of medicinal chemistry.