Author/Authors :
Douglas E. Wilkinson، نويسنده , , Bert E. Thomas IV، نويسنده , , David C. Limburg، نويسنده , , Agnes Holmes، نويسنده , , Hansjorg Sauer، نويسنده , , Douglas T Ross، نويسنده , , Raj Soni، نويسنده , , Yi Chen، نويسنده , , Hong Guo، نويسنده , , Pamela Howorth، نويسنده , , Heather Valentine، نويسنده , , Dawn Spicer، نويسنده , , Mike Fuller، نويسنده , , Joseph P. Steiner، نويسنده , , Gregory S Hamilton، نويسنده , , Yong-Qian Wu، نويسنده ,
Abstract :
Nonimmunosuppressant ligands, exemplified by GPI 1046 (1), for the peptidyl-prolyl isomerase FKBP12 have been found to unexpectedly possess powerful neuroprotective and neuroregenerative effects in vitro and in vivo. We have extensively explored the therapeutic utility of FKBP12 ligands based on analogues of proline and pipecolic acid. As part of our ongoing program to explore novel structural classes of FKBP12 ligands, we herein wish to report a new class of FKBP12 ligands containing aza-proline and aza-pipecolic acid analogues. Details of the synthetic studies, together with biological activity will be presented.
