ProHealth health Vitamin and Natural Supplement Store and Health
Home  |  Log In  |  My Account  |  View Cart  View Your ProHealth Vitamin and Supplement Shopping Cart
800-366-6056  |  Contact Us  |  Help
Facebook Google Plus
Fibromyalgia  Chronic Fatigue Syndrome & M.E.  Lyme Disease  Natural Wellness  Supplement News  Forums  Our Story
Store     Brands   |   A-Z Index   |   Best Sellers   |   New Products   |   Deals & Specials   |   Under $10   |   SmartSavings Club

Trending News

Is a Good Night's Sleep at the Top of Your Wishlist?

Ashwagandha Helps Hormones - Aids Arthritis

A Breathalyzer for Disease?

Why You Should Be Eating More Porcini Mushrooms

Tryptophan's Possible Effects for Your Health

How Bacopa Can Help Improve Your Cognitive Function

Black Tea Is Great for Your Gut

Magnesium Reduces Diabetes and Helps Keep You Young

Lavender Aromatherapy Can Ease Pre-Op Anxiety

Mint: Learn More About This Refreshing and Invigorating Herb

 
Print Page
Email Article

Abstract: Structural insights and biological effects of glycogen synthase kinase 3 specific inhibitor AR-A014418

  [ 46 votes ]   [ Discuss This Article ]
www.ProHealth.com • September 17, 2003


J Biol Chem. 2003 Aug 19 [Epub ahead of print].

Bhat RV, Xue Y, Berg S, Hellberg (1) S, Ormo M, Nilsson Y, Radesater AC, Jerning E, Markgren PO, Borgegard T, Nylof M, Gimenez-Cassina A, Hernandez F, Lucas JJ, Diaz-Nido J, Avila J.

Research DMPK, AstraZeneca RD Sdertlje, Sdertlje 15185.

Glycogen synthase kinase 3 (GSK3) is a serine/threonine kinase that has been implicated in pathological conditions such as diabetes and Alzheimer's disease. We report the characterization of a GSK3 inhibitor, AR-A014418, which inhibits GSK3 (IC50 104+27 nM), in an ATP competitive manner (Ki, 38 nM). AR-A014418 does not significantly inhibit cdk2 or cdk5 (IC50 > 100 mM) or 26 other kinases demonstrating high specificity for GSK3.

We report the co-crystallisation of AR-A014418 with the GSK3beta protein and provide a description of the interactions within the ATP pocket as well as an understanding of the structural basis for the selectivity of AR-A014418. AR-A014418 inhibits tau phosphorylation at a GSK3 specific site (Ser-396) in cells stably expressing human 4-repeat tau protein.

AR-A014418 protects N2A neuroblastoma cells against cell death mediated by inhibition of the PI3K/PKB survival pathway. Furthermore, AR-A014418 inhibits neurodegeneration mediated by beta-amyloid peptide in hippocampal slices. AR-A014418 may thus have important applications as a tool to elucidate the role of GSK3 in cellular signaling and possibly in Alzheimers disease. AR-A014418 is the first compound of a family of specific inhibitors of GSK3 that does not significantly inhibit closely related kinases such as cdk2 or cdk5.

PMID: 12928438 [PubMed - as supplied by publisher]




Post a Comment

Featured Products From the ProHealth Store
Ultra ATP+, Double Strength Ultra EPA  - Fish Oil Mitochondria Ignite™ with NT Factor®


Article Comments



Be the first to comment on this article!

Post a Comment


 
Optimized Curcumin Longvida with Omega-3

Featured Products

Optimized Curcumin Longvida® Optimized Curcumin Longvida®
Supports Cognition, Memory & Overall Health
Ultra EPA  - Fish Oil Ultra EPA - Fish Oil
Ultra concentrated source of essential fish oils
Mitochondria Ignite™ with NT Factor® Mitochondria Ignite™ with NT Factor®
Reduce Fatigue up to 45%
Energy NADH™ 12.5mg Energy NADH™ 12.5mg
Improve Energy & Cognitive Function
Ultra ATP+, Double Strength Ultra ATP+, Double Strength
Get energized with malic acid & magnesium

Natural Remedies

D-ficient? Health Risks You Need to Know About D-ficient? Health Risks You Need to Know About
Can Pomegranates Slow Aging? Can Pomegranates Slow Aging?
Optimize Your Immune System Naturally: Thymic Protein A Optimize Your Immune System Naturally: Thymic Protein A
Break Free From Fibromyalgia Break Free From Fibromyalgia
Live Without Anxiety or Stress Live Without Anxiety or Stress

CONTACT US
ProHealth, Inc.
555 Maple Ave
Carpinteria, CA 93013
(800) 366-6056  |  Email

· Become a Wholesaler
· Vendor Inquiries
· Affiliate Program
SHOP WITH CONFIDENCE
Credit Card Processing
SUBSCRIBE TO OUR NEWSLETTERS
Get the latest news about Fibromyalgia, M.E/Chronic Fatigue Syndrome, Lyme Disease and Natural Wellness

CONNECT WITH US ProHealth on Facebook  ProHealth on Twitter  ProHealth on Pinterest  ProHealth on Google Plus

© 2017 ProHealth, Inc. All rights reserved. Pain Tracker App  |  Store  |  Customer Service  |  Guarantee  |  Privacy  |  Contact Us  |  Library  |  RSS  |  Site Map