Results 141 to 150 of about 5,725 (156)

Disruption of Oligomerization and Dehydroalanine Formation as Mechanisms for ClpP Protease Inhibition

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, Roman Kolb, Ferdinand Alte, Michael Groll, Stephan A. Sieber   +4 more
openaire   +2 more sources

A novel class of Plasmodial ClpP protease inhibitors as potential antimalarial agents

Bioorganic & Medicinal Chemistry, 2017
The 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.
Sourabh, Mundra, Vandana, Thakur, Angelica M, Bello, Sumit, Rathore, Mohd, Asad, Lianhu, Wei, Jane, Yang, Sai Kumar, Chakka, Radhakrishnan, Mahesh, Pawan, Malhotra, Asif, Mohmmed, Lakshmi P, Kotra   +11 more
openaire   +2 more sources

Der Inhibitionsmechanismus der caseinolytischen Protease (ClpP)

Angewandte Chemie, 2013
Gersch, M., Gut, F., Korotkov, V., Lehmann, J., Böttcher, T., Rusch, M., Hedberg, C., Waldmann, H., Klebe, G., Sieber, S.   +9 more
openaire   +2 more sources

The mitochondrial protease ClpP is a promising target for multiple myeloma treatment

Biochemical Pharmacology
Drug 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, Jinlong, Gu, Song, Liu, Jingcao, Huang, Linfeng, Li, Fangfang, Wang, Siyao, He, Ziyue, Mi, Yue, Zhang, Jingjing, Wen, Qianwen, Gao, Haonan, Yang, Yu, Feng, Hongmei, Luo, Xinyu, Zhai, Li, Zhang, Yuhuan, Zheng, Youfu, Luo, Ting, Niu   +18 more
openaire   +2 more sources

Aberrant human ClpP activation disturbs mitochondrial proteome homeostasis to suppress pancreatic ductal adenocarcinoma

Cell Chemical Biology, 2022
Cai-Guang Yang
exaly  

Mitochondrial ClpP-Mediated Proteolysis Induces Selective Cancer Cell Lethality

Cancer Cell, 2019
Jo Ishizawa, Ondrej Halgas, Ran Zhao
exaly  

Inhibition of the Mitochondrial Protease ClpP as a Therapeutic Strategy for Human Acute Myeloid Leukemia

Cancer Cell, 2015
Etienne Coyaud, Veronique Voisin, Ashwin Ramakrishnan   +2 more
exaly  

UNDERSTANDING THE ACTIVATION OF BACTERIAL PROTEASE CLPP BY ACYLDEPSIPEPTIDE ANTIBIOTIC

2014
Acyldepsipeptide (ADEP1) is an antibiotic that binds to Escherichia coli ClpP, mimicking the interaction that the protease typically establishes with ClpA/ClpX ATPases in bacterial cells. Binding of ADEP1 causes the N-terminal end of the ClpP to adopt a structured β-hairpin and triggers opening of the axial gate in the tetradecameric ClpP.
openaire   +1 more source

The antibiotic ADEP reprogrammes ClpP, switching it from a regulated to an uncontrolled protease

EMBO Molecular Medicine, 2009
Janine Kirstein, Heike Brötz-Oesterhelt, Axel Mogk   +2 more
exaly  

Acyldepsipeptide Analogs Dysregulate Human Mitochondrial ClpP Protease Activity and Cause Apoptotic Cell Death

Cell Chemical Biology, 2018
Keith S Wong, Thiago Vargas Seraphim, Kamran Rizzolo   +2 more
exaly