Featured Research

from universities, journals, and other organizations

Water-soluble 'gelatinase inhibitor' compounds show promise for treating neurological diseases

Date:
October 12, 2011
Source:
University of Notre Dame
Summary:
Scientists have taken a promising step on the road to developing new drugs for a variety of neurological diseases. The researchers focused on the design, synthesis and evaluation of water-soluble "gelatinase inhibitor" compounds.

Results of a study by a group of University of Notre Dame researchers represent a promising step on the road to developing new drugs for a variety of neurological diseases.

The group from the University's Departments of Chemistry and Biochemistry and Biological Sciences and the Friemann Life Sciences Center focused on the design, synthesis and evaluation of water-soluble "gelatinase inhibitor" compounds.

Gelatinases, a class of enzymes, have been implicated in a host of human diseases from cancer to cardiovascular conditions and in particular neurological conditions such as stroke, aneurysm and traumatic brain injury. Researchers have increasingly focused on developing potent gelatinase inhibitor drugs to treat acute gelatinase-dependent diseases.

The Notre Dame group has been investigating variants of a compound called "SB-3CT," which shows promise as a selective and potent gelatinase inhibitor. SB-3CT has exhibited potent efficacy in animal models for a variety of neurological and cancer diseases.

The preferred method of treatment for acute gelatinase-dependent diseases is intravenous infusion. Intravenous administration requires that the compound be water soluble. Unfortunately SB-3CT has poor water solubility and poor drug-like properties.

In a new approach, the Notre Dame researchers used a prodrug strategy to address this issue. A prodrug is an inactive precursor of a drug that is converted into its active form in the body by normal metabolic processes.

The prodrug strategy produced a greater than 5,000-fold increase in water solubility compared to SB-3CT. In addition to its high water solubility, the prodrug (referred to as ND-478) was chemically stable, non-toxic and was quickly converted to the active drug in the blood. These favorable properties of ND-478 make it suitable for intravenous administration in the treatment of acute gelatinase-dependent diseases. Such a compound offers the possibility of translation into the clinic for treatment of strokes, aneurysms and traumatic brain injury.

The Notre Dame research team included Mayland Chang, Shahriar Mobashery, Major Gooyit, Mijoon Lee, Valerie A. Schroeder, Masahiro Ikerjiri and Mark Suckow. Their paper appears in the Journal of Medicinal Chemistry.


Story Source:

The above story is based on materials provided by University of Notre Dame. Note: Materials may be edited for content and length.


Journal Reference:

  1. Major Gooyit, Mijoon Lee, Valerie A. Schroeder, Masahiro Ikejiri, Mark A. Suckow, Shahriar Mobashery, Mayland Chang. Selective Water-Soluble Gelatinase Inhibitor Prodrugs. Journal of Medicinal Chemistry, 2011; 54 (19): 6676 DOI: 10.1021/jm200566e

Cite This Page:

University of Notre Dame. "Water-soluble 'gelatinase inhibitor' compounds show promise for treating neurological diseases." ScienceDaily. ScienceDaily, 12 October 2011. <www.sciencedaily.com/releases/2011/10/111007161640.htm>.
University of Notre Dame. (2011, October 12). Water-soluble 'gelatinase inhibitor' compounds show promise for treating neurological diseases. ScienceDaily. Retrieved July 29, 2014 from www.sciencedaily.com/releases/2011/10/111007161640.htm
University of Notre Dame. "Water-soluble 'gelatinase inhibitor' compounds show promise for treating neurological diseases." ScienceDaily. www.sciencedaily.com/releases/2011/10/111007161640.htm (accessed July 29, 2014).

Share This




More Health & Medicine News

Tuesday, July 29, 2014

Featured Research

from universities, journals, and other organizations


Featured Videos

from AP, Reuters, AFP, and other news services

Deadly Ebola Virus Threatens West Africa

Deadly Ebola Virus Threatens West Africa

AP (July 28, 2014) West African nations and international health organizations are working to contain the largest Ebola outbreak in history. It's one of the deadliest diseases known to man, but the CDC says it's unlikely to spread in the U.S. (July 28) Video provided by AP
Powered by NewsLook.com
$15B Deal on Vets' Health Care Reached

$15B Deal on Vets' Health Care Reached

AP (July 28, 2014) A bipartisan deal to improve veterans health care would authorize at least $15 billion in emergency spending to fix a veterans program scandalized by long patient wait times and falsified records. (July 28) Video provided by AP
Powered by NewsLook.com
Two Americans Contract Ebola in Liberia

Two Americans Contract Ebola in Liberia

Reuters - US Online Video (July 28, 2014) Two American aid workers in Liberia test positive for Ebola while working to combat the deadliest outbreak of the virus ever. Linda So reports. Video provided by Reuters
Powered by NewsLook.com
Traditional African Dishes Teach Healthy Eating

Traditional African Dishes Teach Healthy Eating

AP (July 28, 2014) Classes are being offered nationwide to encourage African Americans to learn about cooking fresh foods based on traditional African cuisine. The program is trying to combat obesity, heart disease and other ailments often linked to diet. (July 28) Video provided by AP
Powered by NewsLook.com

Search ScienceDaily

Number of stories in archives: 140,361

Find with keyword(s):
Enter a keyword or phrase to search ScienceDaily for related topics and research stories.

Save/Print:
Share:

Breaking News:
from the past week

In Other News

... from NewsDaily.com

Science News

Health News

Environment News

Technology News



Save/Print:
Share:

Free Subscriptions


Get the latest science news with ScienceDaily's free email newsletters, updated daily and weekly. Or view hourly updated newsfeeds in your RSS reader:

Get Social & Mobile


Keep up to date with the latest news from ScienceDaily via social networks and mobile apps:

Have Feedback?


Tell us what you think of ScienceDaily -- we welcome both positive and negative comments. Have any problems using the site? Questions?
Mobile: iPhone Android Web
Follow: Facebook Twitter Google+
Subscribe: RSS Feeds Email Newsletters
Latest Headlines Health & Medicine Mind & Brain Space & Time Matter & Energy Computers & Math Plants & Animals Earth & Climate Fossils & Ruins