Coming Down the Pike: Protein-Substrate Binding - Pharmaceutical Technology

Latest Issue
PharmTech

Latest Issue
PharmTech Europe

Coming Down the Pike: Protein-Substrate Binding
Drugmakers seeking to block the activity of a protein may have a new strategy at their disposal.


Pharmaceutical Technology

Drugmakers seeking to block the activity of a protein may have a new strategy at their disposal, according to a paper published in the June 11, 2008, issue of Nature. Traditionally, drugs that block protein activities do so by binding the protein's active site, which in turn prevents the natural substrate from binding at that site, which ultimately inhibits the protein's activity. But there may be another way to skin that particular cat. The new paradigm proposes to prevent substrate binding by attaching the drug directly to the substrate instead of to the protein. In theory, this also would prevent the substrate from binding the protein's active site with the same effect of inhibiting the protein's activity.

The notion of interfering with protein-substrate binding by tying up the substrate may have several advantages over the traditional approach. For one thing, many of the protein-blocking drugs are monoclonal antibodies, themselves large proteins that can be difficult to deliver. Substrate blocking, on the other hand, might be accomplished with smaller molecules. In addition, substrates are often found circulating in the bloodstream, which may facilitate drug delivery.

Source: T. Kodadek, "Biochemsitry: Molecular Cloaking Devices," Nature 453 (7197), 861–862 (2008).

ADVERTISEMENT

blog comments powered by Disqus
LCGC E-mail Newsletters

Subscribe: Click to learn more about the newsletter
| Weekly
| Monthly
|Monthly
| Weekly

Survey
FDASIA was signed into law two years ago. Where has the most progress been made in implementation?
Reducing drug shortages
Breakthrough designations
Protecting the supply chain
Expedited reviews of drug submissions
More stakeholder involvement
Reducing drug shortages
70%
Breakthrough designations
4%
Protecting the supply chain
17%
Expedited reviews of drug submissions
2%
More stakeholder involvement
7%
View Results
Eric Langerr Outsourcing Outlook Eric LangerTargeting Different Off-Shore Destinations
Cynthia Challener, PhD Ingredients Insider Cynthia ChallenerAsymmetric Synthesis Continues to Advance
Jill Wechsler Regulatory Watch Jill Wechsler Data Integrity Key to GMP Compliance
Sean Milmo European Regulatory WatchSean MilmoExtending the Scope of Pharmacovigilance Comes at a Price
From Generics to Supergenerics
CMOs and the Track-and-Trace Race: Are You Engaged Yet?
Ebola Outbreak Raises Ethical Issues
Better Comms Means a Fitter Future for Pharma, Part 2: Realizing the Benefits of Unified Communications
Better Comms Means a Fitter Future for Pharma, Part 1: Challenges and Changes
Source: Pharmaceutical Technology,
Click here