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

Vitamin D supplements, sleep could help manage pain

Bacopa: The Herb That May Increase Your Brain Power

Lilac Oil: More Than Just for Fragrance

Eat More Yogurt and Avoid Osteoporosis

Safflower: An Economically Important Herb That Can Benefit Humans and Animals Alike

What Is Bilberry Good For?

Coffee, herbal tea may help prevent liver fibrosis

Crafty Uses for Carrot Seed Oil

Higher omega 3 levels linked to improved brain blood flow

Curcumin, resveratrol, ursolic acid show promise against prostate cancer

 
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
Ultra EPA  - Fish Oil Mitochondria Ignite™ with NT Factor® FibroSleep™

Looking for Vitamins, Herbs and Supplements?
Search the ProHealth Store for Hundreds of Natural Health Products


Article Comments



Be the first to comment on this article!

Post a Comment


 
NAD+ Ignite with Niagen

Featured Products

Ultra ATP+, Double Strength Ultra ATP+, Double Strength
Get energized with malic acid & magnesium
Mitochondria Ignite™ with NT Factor® Mitochondria Ignite™ with NT Factor®
Reduce Fatigue up to 45%
FibroSleep™ FibroSleep™
The All-in-One Natural Sleep Aid
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

Natural Remedies

Prepare Yourself for Cold & Flu Season Prepare Yourself for Cold & Flu Season
Sleep Like a Baby in Nature's Cradle Sleep Like a Baby in Nature's Cradle
Live Without Anxiety or Stress Live Without Anxiety or Stress
Soothe, Heal and Regulate Your Digestive System with Nutrient-Rich Aloe Vera Soothe, Heal and Regulate Your Digestive System with Nutrient-Rich Aloe Vera
Bone Broth Benefits for Digestion, Arthritis and Cellulite Bone Broth Benefits for Digestion, Arthritis and Cellulite

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