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

16 Tips from 16 Years Sick

Fibromyalgia Fare Fit for All Seasons

New Study Shows Artificial Sweeteners Lead to Diabetes

Essential Oils — An Effective and Healthy Option to Treat Headaches

Antioxidant treatment could halt neurodegeneration in early Parkinson's

Higher vitamin D levels associated with less severe disease in NAFLD patients

Krill Oil: Make This Omega-3 Supplement Part of Your Health Regimen

How zinc helps fight esophageal cancer

Everything You Need to Know About Black Cohosh

Low vitamin D levels predict ED in diabetics

 
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
Mitochondria Ignite™ with NT Factor® Optimized Curcumin Longvida® FibroSleep™


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

Natural Remedies

The Crucial Role CoQ10 Plays in Fibromyalgia and ME/CFS The Crucial Role CoQ10 Plays in Fibromyalgia and ME/CFS
"It's Not Easy Being Green" - But It Is Healthy
Carry a Massage Therapist in Your Pocket Carry a Massage Therapist in Your Pocket
Magnesium + Malic Acid: One-Two Punch for Pain & Fatigue Magnesium + Malic Acid: One-Two Punch for Pain & Fatigue
Herbal Inflammation Management for Whole Body Health Herbal Inflammation Management for Whole Body Health

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