In the news ! Pfizer's JAK-3 Inhibitor has the potential to be the next blockbuster for Autoimmune Disease.
Pfizer JAK-3 arthritis drug effective in studies
Drug CP-690,550
http://www.reuters.c...631123820091017
JAK3 Inhibitors in Organ Transplantation and Autoimmune Disease.
Xiong Z, Ma A, Chen H. Laboratory of Experimental Surgery, Department of Surgery, Research Centre, Centre hospitalier de l'Université de Montréal (CHUM), Hôpital Notre-Dame, and Université de Montréal, Montreal, Quebec, Canada. hui.fang.chen@umontreal.ca.
Janus kinase 3 (JAK3) is a cytoplasmic tyrosine kinase associated with the common gamma chain that is activated by multiple T-cell growth factors including IL-2, -4, -9, -15, and -21. From the recent reports, genetic absence or ablation of JAK3 is associated with defective T-cell immunity that results in severe combined immunodeficiency (SCID) and pharmacological inhibition has prolonged allograft survival in some models of organ transplantation. This review would provide an overview of some patents along with the role of JAK3 in the immune system and efficacy of JAK3 inhibitors in experimental allograft rejection and autoimmune disease.
Tyrosine kinases as new molecular targets in treatment of inflammatory disorders and leukemia.
Uckun FM, Mao C. Drug Discovery Program, Parker Hughes Institute, 2699 Patton Road, St. Paul, MN 55113, USA. fatih_uckun@ih.org
Many protein tyrosine kinases (PTK), including Janus kinase 3 (JAK3) and Bruton's tyrosine kinase (BTK), have been recently identified as potential drug targets to treat diverse diseases including inflammation and cancer. The wealth of structural information currently available for protein kinase-inhibitor complexes facilitates the structure-based design of novel kinase inhibitors. In this report, we discuss the structural basis of protein kinase inhibitor design and the common binding features of small molecule kinase inhibitors including pyridinyl imidazoles, purines, oxindoles, anilinoquinazolines and isoquinalines. The structural features of targeted kinase proteins and their inhibitor complexes are discussed with respect to their structure-and-activity relationships (SAR). We present a structural comparison of kinase inhibitors with a special emphasis on inhibitors of JAK3 and BTK.
Dieatary JAK3 Inhibitors ? ...
Flavones ?
