19094-55-4Relevant articles and documents
INHIBITORS OF PROTEIN ARGININE DEIMINASE 1 AND METHODS OF PREPARATION AND USE THEREOF
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, (2021/01/23)
The invention provides novel inhibitors or inactivators of protein arginine deiminase 1, pharmaceutical compositions and methods of use thereof. The invention also relates to molecular probes based on such compounds and methods of use thereof.
Dual protonophore-chitinase inhibitors dramatically affect O. Volvulus molting
Gooyit, Major,Tricoche, Nancy,Lustigman, Sara,Janda, Kim D.
, p. 5792 - 5799 (2014/08/05)
The L3-stage-specific chitinase OvCHT1 has been implicated in the development of Onchocerca volvulus, the causative agent of onchocerciasis. Closantel, a known anthelmintic drug, was previously discovered as a potent and specific OvCHT1 inhibitor. As closantel is also a known protonophore, we performed a simple scaffold modulation to map out the structural features that are relevant for its individual or dual biochemical roles. Furthermore, we present that either OvCHT1 inhibition or protonophoric activity was capable of affecting O. volvulus L3 molting and that the presence of both activities in a single molecule yielded more potent inhibition of the nematode's developmental process.