Non-peptide ITAM mimics as ZAP-70 antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 7, Issue 22, 1997, Pages 2875-2878

  Revesz, Laszlo ^a   Blum, Ernst ^a   Manning, Ute ^a   Demange, B Jachez ^a   Widmer, Armin ^a   Zuber, Jean François ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

PROTEIN TYROSINE KINASE; T LYMPHOCYTE RECEPTOR;

AMINO ACID SEQUENCE; AMINO ACID SUBSTITUTION; ARTICLE; BINDING SITE; DIMERIZATION; LIGAND BINDING; PEPTIDE SYNTHESIS; SIGNAL TRANSDUCTION; X RAY CRYSTALLOGRAPHY;

EID: 0030697349     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0960-894X(97)10102-0     Document Type: Article

References (8)

1. Wange R.L.; Isakov, N.; Burke, T.R.; Otaka, A.; Roller, P.P.; Watts, J.D.; Aebersold, R. and Samelson, L.E. J.Biol.Chem. 1995, 270, 944.
2. Hatada, H.H.; Lu, X.; Laird, E.R.; Green, J.; Morgenstern, J.P.; Lou, M.; Marr, C.S.; Phillips, T.B.; Ram, M.K.; Theriault, K.; Zoller, M.J. and Karas, J.L. Nature 1995, 377, 32.
3. Liu, W.-Q.; Carreaux, F.; Meudal, H.; Roques, B.P.; Garbay-Jaureguiberry, C. Tetrahedron 1996, 52, 4411. Solas, D.; Hale R.L. and Patel, D.V. J.Org.Chem. 1996, 61, 1537.
4. Liu, W.-Q.; Carreaux, F.; Meudal, H.; Roques, B.P.; Garbay-Jaureguiberry, C. Tetrahedron 1996, 52, 4411. Solas, D.; Hale R.L. and Patel, D.V. J.Org.Chem. 1996, 61, 1537.
5. 50 values; ie., the inhibitor concentrations causing a signal decrease of 50 percent. The sensorchip surfaces were very stable and could after sample injection be regenerated using 0.05 % (w/v) SDS.
6. 2. After activation, plates were centrifuged for 10 minutes at 200g and the supernatants were removed by flicking. Cells were lysed by addition of 20 μl lysis buffer containing 25 mM Tris-phosphate (pH 7.8), 2 mM DTT, 2 mM 1.2-diaminocyclohexane-N,N,N',N'-tetraacetic acid, 10% (v/v) Glycerol and 1% (v/v) Triton X-100. Plates were shaken for 10 minutes on a Titertek shaker. Then plates were scanned in a Luminoskan (Labsystem) where 50 μl of luciferase assay buffer (20 mM Tricine, 1.07 mM magnesium carbonate, 2.67 mM magnesium sulfate, 0.1 mM EDTA, 33.3 mM DTT, 270 μM CoenzymeA, 470 μM Luciferin, 530 μM ATP, pH 7.8) are automatically added.
7. von Bonin, A.; Wienands, J.; Manning, U.; Zuber, J.-F.; and Baumann, G. J. Biol. Chem. 1994, 269, 33035.
8. Müller, K.; Gombert, F.; Manning, U.; Grossmüller, F.; Graff, P.; Zaegel, H.; Zuber, J.-F.; Freuler, F.; Tschopp, C.; and Baumann, G. J. Biol. Chem. 1996, 271, 16500.