Journal of the American Chemical Society p. 9925 - 9938 (1993)
Update date:2022-08-03
Topics:
Holt, Dennis A.
Luengo, Juan I.
Yamashita, Dennis S.
Oh, Hye-Ja
Konialian, Arda L.
Yen, Hwa-Kwo
Rozamus, Leonard W.
Brandt, Martin
Bossard, Mary J.
Levy, Mark A.
Eggleston, Drake S.
Liang, Jun
Wayne Schultz
Stout, Thomas J.
Clardy, Jon
The design and synthesis of high-affinity FKBP12 ligands is described. These compounds potently inhibit the cis-trans-peptidylprolyl isomerase (rotamase) activity catalyzed by FKBP12 with inhibition constants (Ki,app) as low as 1 nM, yet they possess remarkable structural simplicity relative to FK506 and rapamycin, from which they are conceptually derived. The atomic structures of three FKBP12-ligand complexes and of one unbound ligand were determined by X-ray crystallography and are compared to the FKBP12-FK506 and FKBP12-rapamycin complexes.
View MoreChangzhou LanXu Chemical Co.,ltd.(expird)
Contact:86-0519-86330911,13656129734,15261186386
Address:Room 524, Depart.Chemical, Changzhou Science and Eductaion town, Jiangsu, China;Factory: Haian Fine Chemical Industry Park,Nantong,Jiangsu,China
JiYi Chemical (Beijing) Co., Ltd.
Contact:+86-10-89385733
Address:Shilou Town of Fangshan District， Beijing
Shanghai Sharing technologies Co., Ltd.
Contact:86-021-66787223
Address:No11, Lane 225, Jinxiang Road,Pudong district
Beijing Mediking Biopharm Co., Ltd.
Contact:+86-10-89753524/81760121/81769521
Address:Hongxianghong Incubator, Beiqijia Town, Changping district, Beijing, China
NanJing KaiHeng Chemical CO., LTD.
Contact:+86-25-85768391
Address:RM.1704, D, WANDA PLAZA, NO.110, MIDDLE JIANGDONG ROAD, NANJING, CHINA
Doi:10.1021/jo961012z
(1996)Doi:10.1016/S0957-4166(00)80420-6
(1993)Doi:10.1016/0223-5234(93)90096-W
(1993)Doi:10.1016/0022-328X(93)80359-J
(1993)Doi:10.1021/jo00080a024
(1994)Doi:10.1002/hlca.19790620407
(1979)
