59279-58-2Relevant articles and documents
An irreversible inhibitor of peptidyl-prolyl cis/trans isomerase Pin1 and evaluation of cytotoxicity
Ieda, Naoya,Itoh, Kaoru,Inoue, Yasumichi,Izumiya, Yusuke,Kawaguchi, Mitusyasu,Miyata, Naoki,Nakagawa, Hidehiko
, p. 353 - 356 (2019)
Pin1 (protein interacting with never in mitosis A-1) is a member of the peptidyl prolyl isomerase (PPIase) family, and catalyzes cis-trans isomerization of pThr/Ser-Pro amide bonds. Because Pin1 is overexpressed in various cancer cell lines and promotes c
Synthesis of l -Kynurenine and Homo- l -Kynurenine via an Aza-Fries Rearrangement
Bonilla-Reyes, Edgar,Sánchez-Carrillo, Adrian,Vázquez, Alfredo
, p. 3473 - 3479 (2020/09/15)
l -Kynurenine, a non-proteinogenic amino acid, is the primary metabolite of tryptophan via the kynurenine pathway. Kynurenine is involved in a variety of biological processes occurring in the human body, notably in the central nervous system. Thus, the st
Oxadiazole-Based Cell Permeable Macrocyclic Transition State Inhibitors of Norovirus 3CL Protease
Damalanka, Vishnu C.,Kim, Yunjeong,Alliston, Kevin R.,Weerawarna, Pathum M.,Galasiti Kankanamalage, Anushka C.,Lushington, Gerald H.,Mehzabeen, Nurjahan,Battaile, Kevin P.,Lovell, Scott,Chang, Kyeong-Ok,Groutas, William C.
, p. 1899 - 1913 (2016/03/22)
Human noroviruses are the primary causative agents of acute gastroenteritis and a pressing public health burden worldwide. There are currently no vaccines or small molecule therapeutics available for the treatment or prophylaxis of norovirus infections. Norovirus 3CL protease plays a vital role in viral replication by generating structural and nonstructural proteins via the cleavage of the viral polyprotein. Thus, molecules that inhibit the viral protease may have potential therapeutic value. We describe herein the structure-based design, synthesis, and in vitro and cell-based evaluation of the first class of oxadiazole-based, permeable macrocyclic inhibitors of norovirus 3CL protease.