Method for determining inhibitors of neurotrypsin

Details Method for determining inhibitors of neurotrypsin Method for determining inhibitors of neurotrypsin

2011-03-01

2011-03-01

Weber, Jon P (Department: 1657)

Chemistry: molecular biology and microbiology

Measuring or testing process involving enzymes or...

Involving hydrolase

C435S018000

Reexamination Certificate

active

07897364

ABSTRACT:
The invention relates to a method for determining whether a compound is a neurotrypsin inhibitor, characterized in that the compound is incubated together with neurotrypsin, a variant thereof or a fragment comprising the protease domain and with a protein or peptide comprising agrin, a variant thereof or a fragment comprising the α- or the β-cleavage site of agrin, in an aqueous buffer solution, and the amount of cleavage of agrin is measured. Additionally, the invention relates to inhibitors of neurotrypsin found by this method, in particular to compounds of formulawherein Hal1and Hal2are fluorine, chlorine or bromine, and the use of such inhibitors for the treatment and/or prophylaxis of diseases caused by deficiency of synapses, for example skeletal muscle atrophy, schizophrenia, and cognitive disturbance.

REFERENCES:
patent: 6783949 (2004-08-01), Muller et al.
patent: 98/49322 (1998-11-01), None
patent: 2004/035810 (2004-04-01), None
Molinari F. et al. Truncating neurotrypsin mutation in autosomal recessive nonsyndromic mental retardation, Science, 29thNov. 2002, vol. 298, pp. 1779-1781.
Tseng C-N et al. Calcium plays a critical role in determining the AChR-clustering activities of alternatively spliced isoforms of agrin, JBC Papers in Press, Published on Mar. 5, 2003 as Manuscript M300282200, pp. 1-27 and figures 1-9.
Reif R. et al. Specific cleavage of agrin by neurotrypsin, a synaptic protease linked to mental retardation, FASEB Journal, Research Communication, Published online Jun. 22, 2007, pp. 1-11.
International Search Report issued in the International (PCT) Application of which the present application is the U.S. National Stage, mailed on Dec. 22, 2006.

Affiliated with

Also associated with

Rating

Method for determining inhibitors of neurotrypsin does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Method for determining inhibitors of neurotrypsin, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Method for determining inhibitors of neurotrypsin will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-2770695