Design and synthesis of phosphotyrosine mimetics

Bioorganic and Medicinal Chemistry Letters

Volumn 13, Issue 12, 2003, Pages 2083-2085

  Yan, Zheng ^a   Kahn, Michael ^b,c   Qabar, Maher ^a   Urban, Jan ^a   Kim, Hwa Ok ^a   Blaskovich, Mark A ^a,d  

^a Molecumetics Ltd   (United States)

^b UNIVERSITY OF WASHINGTON   (United States)

^c PACIFIC NORTHWEST RESEARCH INSTITUTE   (United States)

^d CEPTYR Inc   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

PHENYLALANINE DERIVATIVE; PHOSPHOTYROSINE; PROTEIN TYROSINE PHOSPHATASE INHIBITOR;

ARTICLE; COMBINATORIAL LIBRARY; DRUG DESIGN; DRUG POTENCY; DRUG SYNTHESIS;

EID: 0037763868     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(03)00253-1     Document Type: Article

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25. Samples were preincubated with 0.2 units/mL enzyme in buffer (100 mM HEPES, 1 mM EDTA, 5 mM DTT, 0.05% Tween-20, 0.01% BSA) for 20 min at rt in black 96-well plates. DiFMUP was then added (final concentration 3.6 μM for PTP1B, 2.1 μM for TCPTP, 15 μM for LAR and 200 μM for CD45) and the plates read on a Fluoroskan (abs. 358, em. 452).
26. i values for the most active compounds against the various enzymes in order to determine selectivity.