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 ?
JAK3 Inhibitors for Autoimmunity
Started by
youandme
, Oct 19 2009 09:30 AM
3 replies to this topic
#1
Posted 19 October 2009 - 09:30 AM
#2
Posted 05 February 2010 - 02:44 PM
Found Emodin is a potent JAK2 Inhibitor.
Emodin an extract from Rhubarb!
http://en.wikipedia.org/wiki/Emodin
Emodin has a cytotoxic activity against human multiple myeloma as a Janus-activated kinase 2 inhibitor
http://mct.aacrjourn.../3/987.abstract
Emodin found as an ingredient in Resveratrol supplements !
Can anyone point me to a Resveratrol Supply with high Emodin content !? Thanks
Also a study points to Resveratrol being a regulator of JAK
"resveratrol prevents phosphorylation of JAK, thereby inhibiting STAT1 phosphorylation"
Regulation of apoptosis by resveratrol through JAK/STAT and mitochondria mediated pathway in human epidermoid carcinoma A431 cells
One could hope the combo of Resveratrol and Emodin to be beneficial for Autoimmune Inflammation.
Lily has just bought Incytes lead compound INCB28050 JAK1/2 inhibitor that is in Phase 2 for RA
http://newsroom.lill...eleaseID=431576
Emodin an extract from Rhubarb!
http://en.wikipedia.org/wiki/Emodin
Emodin has a cytotoxic activity against human multiple myeloma as a Janus-activated kinase 2 inhibitor
http://mct.aacrjourn.../3/987.abstract
Emodin found as an ingredient in Resveratrol supplements !
Can anyone point me to a Resveratrol Supply with high Emodin content !? Thanks
Also a study points to Resveratrol being a regulator of JAK
"resveratrol prevents phosphorylation of JAK, thereby inhibiting STAT1 phosphorylation"
Regulation of apoptosis by resveratrol through JAK/STAT and mitochondria mediated pathway in human epidermoid carcinoma A431 cells
One could hope the combo of Resveratrol and Emodin to be beneficial for Autoimmune Inflammation.
Lily has just bought Incytes lead compound INCB28050 JAK1/2 inhibitor that is in Phase 2 for RA
http://newsroom.lill...eleaseID=431576
Edited by youandme, 05 February 2010 - 02:45 PM.
#3
Posted 06 February 2010 - 07:11 PM
You do know a high amount of Emodin will make you run to the bathroom... don't you?
So I suppose it's ok, if you didn't mind a runny stool, and have a bathroom next door.
A
So I suppose it's ok, if you didn't mind a runny stool, and have a bathroom next door.
A
#4
Posted 07 February 2010 - 10:55 AM
If it potentially stops cancer and fixes my autoimmunity....Id put a toilet in everyroom..more - perhaps just wear a nappy ..Id be so happy...im serious
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