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The development of small-molecule modulators for ClpP protease activity
Molecular BioSystems, 2017Deregulating ClpP activity either through inhibition or overactivation could lead to antibacterial activity.
Fei, Ye, Jiahui, Li, Cai-Guang, Yang
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Selektive Aktivierung der humanen caseinolytischen Protease P (ClpP)
Angewandte Chemie, 2018AbstractDie caseinolytische Protease P (ClpP) ist die proteolytische Komponente des Protein‐Abbau‐Komplexes ClpXP. Ihre genaue Funktion und Regulation sind größtenteils unerforscht. Hier stellen wir eine niedermolekulare Verbindung (D9) vor, die durch Nachahmung des natürlichen Chaperons ClpX als potenter und Spezies‐selektiver Aktivator der humanen ...
Matthias Stahl +9 more
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P-104: Targeting the mitochondrial protease CLPP in Multiple Myeloma
Clinical Lymphoma Myeloma and Leukemia, 2021Background Mitochondria are enticing potential targets against cancer, owing to their role as signaling hubs orchestrating key homeostatic functions. Of special interest is ClpP, a resident mitochondrial protease suggested to maintain OXPHOS by degrading damaged protein components and regulating the assembly of mito-ribosomes.
Tommaso Perini +9 more
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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
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A pH-Dependent Conformational Switch Controls N. meningitidis ClpP Protease Function
Journal of the American Chemical Society, 2020ClpPs are a conserved family of serine proteases that collaborate with ATP-dependent translocases to degrade protein substrates. Drugs targeting these enzymes have attracted interest for the treatment of cancer and bacterial infections due to their critical role in mitochondrial and bacterial proteostasis, respectively.
Zev A. Ripstein +3 more
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The Role of ClpP Protease in Bacterial Pathogenesis and Human Diseases
ACS Chemical Biology, 2018In prokaryotic cells and eukaryotic organelles, the ClpP protease plays an important role in proteostasis. The disruption of the ClpP function has been shown to influence the infectivity and virulence of a number of bacterial pathogens. More recently, ClpP has been found to be involved in various forms of carcinomas and in Perrault syndrome, which is ...
Vaibhav Bhandari +5 more
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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.
Malte Gersch +4 more
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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.
Malte Gersch +4 more
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Der Inhibitionsmechanismus der caseinolytischen Protease (ClpP)
Angewandte Chemie, 2013Gersch, M. +9 more
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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
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