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

15 Health Benefits of Chia Seeds, According to Science

Tangerine Oil: A Citrusy Essential Oil With Well-Rounded Uses

Natural Remedies for the Prevention of Dry Eyes

Magnesium Deficiency Raises Your Risk of Many Chronic Ailments

Resveratrol supplementation improves arterial stiffness in type 2 diabetics

CoQ10's Potential Capabilities for Your Health

How Can Melatonin Benefit You?

Cloves: Boost Your Immune System the Sweet and Spicy Way

Testosterone replacement therapy associated with improved urinary, sexual function

8 Chia Seed Recipes

 
Print Page
Email Article

Abstract: Probing the activation site of ribonuclease L with new N(6)-substituted 2',5'-adenylate trimers

  [ 7 votes ]   [ Discuss This Article ]
www.ProHealth.com • April 9, 2003


Bioorg Med Chem 2003 May;11(9):2041-9

Munch U, Chen L, Bayly SF, Torrence PF.

Section on Biomedical Chemistry, Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, MD 20892-0805, Bethesda, USA

2-5A trimer [5'-monophosphoryladenylyl(2'-5')adenylyl(2'-5')adenosine] activates RNase L. While the 5'-terminal and 2'-terminal adenosine N(6)-amino groups play a key role in binding to and activation of RNase L, the exocyclic amino function of the second adenylate (from the 5'-terminus) plays a relatively minor role in 2-5A's biological activity.

To probe the available space proximal to the amino function of the central adenylate of 2-5A trimer during binding to RNase L, a variety of substituents were placed at that position. To accomplish this, the convertible building block 5'-O-dimethoxytrityl-3'-O-(tert-butyldimethylsilyl)-6-(2,4-dinitrophenyl)thioinosine 2'-(2-cyanoethylN,N-diisopropylphosphoramidite) was prepared as a synthon to introduce 6-(2,4-dinitrophenyl)thioinosine into the middle position of the 2-5A trimer during automated synthesis. Post-synthetic treatment with aqueous amines transformed the (2,4-dinitrophenyl)thioinosine into N(6)-substituted adenosines.

Assays of these modified trimers for their ability to bind and activate RNase L showed that activation activity could be retained, albeit with some sacrifice compared to unmodified p5'A2'p5'A2'p5'A.

Thus, the spatial domain about thisN(6)-amino function could be available for modifications to enhance the biological potency of 2-5A analogues and to ligate 2-5A to targeting vehicles such as antisense molecules.

PMID: 12670655 [PubMed - in process]




Post a Comment

Featured Products From the ProHealth Store
Optimized Curcumin Longvida® Vitamin D3 Extreme™ 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

Energy NADH™ 12.5mg Energy NADH™ 12.5mg
Improve Energy & Cognitive Function
Vitamin D3 Extreme™ Vitamin D3 Extreme™
50,000 IU Vitamin D3 - Prescription Strength
Ultra ATP+, Double Strength Ultra ATP+, Double Strength
Get energized with malic acid & magnesium
FibroSleep™ FibroSleep™
The All-in-One Natural Sleep Aid
Ultra EPA  - Fish Oil Ultra EPA - Fish Oil
Ultra concentrated source of essential fish oils

Natural Remedies

Aches and Pains? A Simple Solution You'll Love Aches and Pains? A Simple Solution You'll Love
"It's Not Easy Being Green" - But It Is Healthy
Coenzyme Q10 - The Energy Maker Coenzyme Q10 - The Energy Maker
Sleep Like a Baby in Nature's Cradle Sleep Like a Baby in Nature's Cradle
Aching Muscles? Top 10 Nutrients to Take Back Your Life Aching Muscles? Top 10 Nutrients to Take Back Your Life

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