Designing better coumarin-based fluorogenic substrates for PTP1B.
As part of a program to develop better PTP1B fluorogenic substrates that more closely mimic the functionality found in the natural substrate, we have prepared and evaluated nine novel analogs of 4-methylumbelliferone phosphate (MUP) with a variety of additional groups occupying the second phosphate binding pocket.
Holmes
Christopher P
CP
Affymax, Inc., Department of Chemistry, 4001 Miranda Avenue, Palo Alto, CA 94304, USA. chris_holmes@affymax.com
Macher
Natalie
N
Grove
J Russell
JR
Jang
Larry
L
Irvine
Jennifer D
JD
D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D005456:Fluorescent Dyes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D018716:Molecular Mimicry; D015394:Molecular Structure; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1 / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D003374:Coumarins; D004791:Enzyme Inhibitors; D005456:Fluorescent Dyes; D054562:Protein Tyrosine Phosphatase, Non-Receptor Type 1