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Boron-containing small molecules for inhibiting activity of a receptor-like protein tyrosine phosphatase
专利权人:
The Penn State Research Foundation
发明人:
Benkovic, Stephen,Tonks, Nicholas K.,Liu, Chun Yu,Krishnan, Navasona,Liu, Chunliang
申请号:
AU2018230580
公开号:
AU2018230580A1
申请日:
2018.03.02
申请国别(地区):
AU
年份:
2019
代理人:
摘要:
A method is disclosed for altering the redox equilibrium of a transmembrane receptor-like protein tyrosine phosphatase (RPTP), particularly a type Ila RPTP, by chemically modulating the activity through contact of such an enzyme with a diaryl boron compound that preferentially reacts with an RPTP in an oxidized state (CyS-OH). This redox modulation is most readily observed and put to use by assaying the inhibition of the phosphatase activity of the RPTP. Such an assay can be carried out on an enzyme in vitro or by contacting the enzyme in a living organism (in vivo). A useful diaryl boron compound corresponds in structure to Formula I in which Ar-1, [Formula should be inserted here] Ar-2, R
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