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Designing better coumarin-based fluorogenic substrates for PTP1B.

Holmes CP, Macher N, Grove JR, Jang L, Irvine JD.

Affymax, Inc., Department of Chemistry, 4001 Miranda Avenue, Palo Alto, CA 94304, USA. chris_holmes@affymax.com

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.

PMID: 18442911 [PubMed - indexed for MEDLINE]