Results 161 to 170 of about 152,432 (174)
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Journal of the American Chemical Society, 2013
Over 100 protease inhibitors are currently used in the clinics, and most of them use blockage of the active site for their mode of inhibition. Among the protease drug targets are several enzymes for which the correct multimeric assembly is crucial to their activity, such as the proteasome and the HIV protease.
Gersch, Malte +4 more
openaire +4 more sources
Over 100 protease inhibitors are currently used in the clinics, and most of them use blockage of the active site for their mode of inhibition. Among the protease drug targets are several enzymes for which the correct multimeric assembly is crucial to their activity, such as the proteasome and the HIV protease.
Gersch, Malte +4 more
openaire +4 more sources
Human ClpP protease, a promising therapy target for diseases of mitochondrial dysfunction
Drug Discovery Today, 2021Human caseinolytic protease P (HsClpP), an ATP-dependent unfolding peptidase protein in the mitochondrial matrix, controls protein quality, regulates mitochondrial metabolism, and maintains the integrity and enzyme activity of the mitochondrial respiratory chain (RC).
Baozhu Luo +4 more
openaire +2 more sources
Barrel-shaped ClpP Proteases Display Attenuated Cleavage Specificities
ACS Chemical Biology, 2015ClpP is a self-compartmentalizing protease with crucial roles in bacterial and mitochondrial protein quality control. Although the ClpP homocomplex is composed of 14 equivalent active sites, it degrades a multitude of substrates to small peptides, demonstrating its capability to carry out diverse cleavage reactions.
Gersch, Malte +6 more
openaire +2 more sources
A Novel Class of Plasmodial ClpP Protease Inhibitors as Potential Antimalarial Agents
Bioorganic and Medicinal Chemistry, 2017The prokaryotic ATP-dependent ClpP protease, localized in the relict plastid of malaria parasite, represents a potential drug target. In the present study, we utilized in silico structure-based screening and medicinal chemistry approaches to identify a novel pyrimidine series of compounds inhibiting P.
Asif Mohmmed +2 more
exaly +3 more sources
The mitochondrial protease ClpP is a promising target for multiple myeloma treatment
Biochemical PharmacologyDrug resistance and relapse are the major obstacles in multiple myeloma (MM) treatment, driving the search for novel therapeutics. The chemoactivation of mitochondrial caseinolytic protease P (ClpP) has shown to have anticancer effects on many tumors, but has seldom been elucidated in MM.
Xiang, Liu +18 more
openaire +2 more sources
Lon and ClpP proteases participate in the physiological disintegration of bacterial inclusion bodies
Journal of Biotechnology, 2005Aggregated protein is solubilized by the combined activity of chaperones ClpB, DnaK and small heat-shock proteins, and this could account, at least partially, for the physiological disintegration of bacterial inclusion bodies. In vivo, the involvement of proteases in this process had been suspected but not investigated.
Andrea, Vera +4 more
openaire +2 more sources
Proteolytic Regulation in the Biosynthesis of Natural Product Via a ClpP Protease System
ACS Chemical BiologyProtein degradation is a tightly regulated biological process that maintains bacterial proteostasis. ClpPs are a highly conserved family of serine proteases that associate with the AAA + ATPase (an ATPase associated with diverse cellular activities) to degrade protein substrates. Identification and biochemical characterization of protein substrates for
Fumihiro Ishikawa +2 more
openaire +2 more sources
Development of Antibiotics That Dysregulate the Neisserial ClpP Protease
ACS Infectious Diseases, 2020Robert A. Batey +2 more
exaly