We investigated and characterized the ATP-dependent protease in human erythroleukemia, K562 cells. The succinyl-leucyl-leucyl-valyl-tyrosine-methylcoumarinamide hydrolytic activity in a K562 lysate at pH 9 rose more than 10-fold with the addition of 1 mM ATP. The effect of ATP on the protease activity was dose-dependent and inhibited by the addition of ADP. This activity was not inhibited by EDTA, L-3-carboxy-trans-2,3-epoxypropionyl-leucylamide-(4-guanidin o)butane or leupeptin, but was strongly inhibited by chymostatin and diisopropylfluorophosphate. The protease activity was eluted just after the void volume from a G3000SW HPLC column. The above results suggest that this protease is identical to the high-molecular-mass protease, ingensin, previously reported by us. The ATP-dependent increase in the protease activity was due to prevention of the inactivation of the protease by ATP, and not to activation of the protease itself in the reaction mixture at 37 degrees C. The depressed succinyl-leucyl-leucyl-valyl-tyrosine-methylcoumarinamide hydrolytic activity in the ATP-depleted lysate was restored to the same level by the detergent, SDS. Therefore, we conclude that the inactivation of ingensin occurring on preincubation is not irreversible.
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http://dx.doi.org/10.1111/j.1432-1033.1988.tb14371.x | DOI Listing |
Background: Neurological disorders are at epidemic levels in the world today. Various proteins are being targeted for the development of novel molecular therapeutics; however, no small-molecule inhibitors have been discovered. Recent studies suggest that there are few molecules in clinical trials for various secretase (α, β, and γ), caspase, and calpain inhibitors.
View Article and Find Full Text PDFJ Chem Inf Model
January 2025
Molecular Simulations and Design Group, Max Planck Institute for Dynamics of Complex Technical Systems, Sandtorstrasse 1, 39106 Magdeburg, Germany.
Cezanne-2 (Cez2) is a deubiquitinylating (DUB) enzyme involved in the regulation of ubiquitin-driven cellular signaling and selectively targets Lys11-linked polyubiquitin chains. As a representative member of the ovarian tumor (OTU) subfamily DUBs, it performs cysteine proteolytic isopeptide bond cleavage; however, its exact catalytic mechanism is not yet resolved. In this work, we used different computational approaches to get molecular insights into the Cezanne-2 catalytic mechanism.
View Article and Find Full Text PDFInt J Med Sci
January 2025
Department of Respiratory and Critical Medicine, the Eighth Affiliated Hospital, Sun Yat-Sen University, Shenzhen 518000, Guangdong Province, China.
Chronic Obstructive Pulmonary Disease (COPD) is a heterogeneous respiratory disorder characterized by persistent airflow limitation. The diverse pathogenic mechanisms underlying COPD progression remain incompletely understood. Macrophages, serving as the most representative immune cells in the respiratory tract, constitute the first line of innate immune defense and maintain pulmonary immunological homeostasis.
View Article and Find Full Text PDFLab Chip
January 2025
Institute of Translational Medicine, Department of Health Sciences and Technology, ETH Zürich, 8092 Zürich, Switzerland.
Proteases, an important class of enzymes that cleave proteins and peptides, carry a wealth of potentially useful information. Devices to enable routine and cost effective measurement of their activity could find frequent use in clinical settings for medical diagnostics, as well as some industrial contexts such as detecting on-line biological contamination. In particular, devices that make use of readouts involving magnetic particles may offer distinct advantages for continuous sensing because material they release can be magnetically captured downstream and their readout is insensitive to optical properties of the sample.
View Article and Find Full Text PDFSheng Li Xue Bao
December 2024
Department of Orthopaedics, the First Hospital of Lanzhou University, Lanzhou 730000, China.
The maintenance of skeletal muscle quality involves various signal pathways that interact with each other. Under normal physiological conditions, these intersecting signal pathways regulate and coordinate the hypertrophy and atrophy of skeletal muscles, balancing the protein synthesis and degradation of muscle. When the total rate of protein synthesis exceeds that of protein degradation, the muscle gradually becomes enlarged, while when the total rate of protein synthesis is lower than that of protein degradation, the muscle shrinks.
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