|
|
|
|
Mining a cathepsin inhibitor library for new antiparasitic drug leads
|
|
|
|
|
|
|
|
نویسنده
|
ang k.k.h. ,ratnam j. ,gut j. ,legac j. ,hansell e. ,mackey z.b. ,skrzypczynska k.m. ,debnath a. ,engel j.c. ,rosenthal p.j. ,mckerrow j.h. ,arkin m.r. ,renslo a.r.
|
|
منبع
|
plos neglected tropical diseases - 2011 - دوره : 5 - شماره : 5
|
|
چکیده
|
The targeting of parasite cysteine proteases with small molecules is emerging as a possible approach to treat tropical parasitic diseases such as sleeping sickness,chagas' disease,and malaria. the homology of parasite cysteine proteases to the human cathepsins suggests that inhibitors originally developed for the latter may be a source of promising lead compounds for the former. we describe here the screening of a unique ~2,100-member cathepsin inhibitor library against five parasite cysteine proteases thought to be relevant in tropical parasitic diseases. compounds active against parasite enzymes were subsequently screened against cultured plasmodium falciparum,trypanosoma brucei brucei and/or trypanosoma cruzi parasites and evaluated for cytotoxicity to mammalian cells. the end products of this effort include the identification of sub-micromolar cell-active leads as well as the elucidation of structure-activity trends that can guide further optimization efforts. © 2011 ang et al.
|
|
|
|
|
آدرس
|
the small molecule discovery center,university of california san francisco,san francisco,ca, United States, the small molecule discovery center,university of california san francisco,san francisco,ca, United States, department of medicine,san francisco general hospital,university of california san francisco,san francisco,ca, United States, department of medicine,san francisco general hospital,university of california san francisco,san francisco,ca, United States, the sandler center for drug discovery,university of california san francisco,san francisco,ca, United States, the sandler center for drug discovery,university of california san francisco,san francisco,ca, United States, the sandler center for drug discovery,university of california san francisco,san francisco,ca, United States, the sandler center for drug discovery,university of california san francisco,san francisco,ca, United States, the sandler center for drug discovery,university of california san francisco,san francisco,ca, United States, department of medicine,san francisco general hospital,university of california san francisco,san francisco,ca, United States, the sandler center for drug discovery,university of california san francisco,san francisco,ca,united states,department of pathology,university of california san francisco,san francisco,ca, United States, the small molecule discovery center,university of california san francisco,san francisco,ca,united states,department of pharmaceutical chemistry,university of california san francisco,san francisco,ca, United States, the small molecule discovery center,university of california san francisco,san francisco,ca,united states,department of pharmaceutical chemistry,university of california san francisco,san francisco,ca, United States
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Authors
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|