- Structure-based design and synthesis of phosphinate isosteres of phosphotyrosine for incorporation in Grb2-SH2 domain inhibitors. Part 1
-
Based on X-ray crystal structure information, mono charged phosphinate isosteres of phosphotyrosine have been designed and incorporated in a short inhibitory peptide sequence of the Grb2-SH2 domain. The resulting compounds, by exploiting additional interactions, inhibit binding to the Grb2-SH2 domain as potently as the corresponding doubly charged (phosphonomethyl)phenylalanine analogue. (C) 2000 Elsevier Science Ltd.
- Furet, Pascal,Caravatti, Giorgio,Denholm, Alastair A.,Faessler, Alex,Fretz, Heinz,Garcia-Echeverria, Carlos,Gay, Brigitte,Irving, Ed,Press, Neil J.,Rahuel, Joseph,Schoepfer, Joseph,Walker, Clive V.
-
-
Read Online
- Indole nitriles
-
Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.
- -
-
-
- Benzamide nitriles
-
Compounds of the formula (I) wherein m, n, A, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.
- -
-
-
- 1, 2-Disubstituted cyclohexane derived tripeptide aldehydes as novel selective thrombin inhibitors
-
A series of tripeptide arginine aldehydes was synthesized by replacement of proline with 1,2-disubstituted cyclohexane derivatives in the sequence of D-MePhe-Pro-Arg-H. Based on molecular modeling, further modification of the D-MePhe residue resulted in a potent and selective thrombin inhibitor.
- Harmat, Nicholas J.S.,Di Bugno, Cristina,Criscuoli,Giorgi, Raffaello,Lippi, Annalisa,Martinelli, Adriano,Monti, Susanna,Subissi
-
p. 1249 - 1254
(2007/10/03)
-