378,533 results match your criteria inhibition enzymes


Nitrile-based peptoids as cysteine protease inhibitors.

Bioorg Med Chem 2021 May 10;41:116211. Epub 2021 May 10.

Medicinal and Biological Chemistry Group (NEQUIMED), Institute of Chemistry of São Carlos, University of São Paulo, São Carlos/SP, Brazil.

Peptidomimetics of the class of dipeptidyl nitrile analog peptoids were synthesized as inhibitors of mammalian cysteine proteases of the papain superfamily. The dipeptidyl nitrile side chains were attached to the peptide backbone's nitrogen atom, not to the α-carbons. Synthesized nitrile-based peptoid analogs that lack the hydrogen amide at P2-P3 are responsible for many of the secondary structure elements in peptides and proteins, making them resistant to proteolysis. Read More

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In-vitro evaluation of antioxidant and anticholinesterase activities of novel pyridine, quinoxaline and s-triazine derivatives.

Environ Res 2021 May 12:111320. Epub 2021 May 12.

Department of Chemistry, Organic and Biomolecular Chemistry Laboratories, Yogi Vemana University, Kadapa-516005, Andhra Pradesh, India.

Cholinesterase enzymes such as acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) cause hydrolysis of acetylcholine (ACh), a neurotransmitter responsible for the cognitive functions of the brain such as acquiring knowledge and comprehension. Therefore, inhibition of these enzymes is an effective process to curb the progressive and fatal neurological Alzheimer's disease (AD). Herein, we explored the potential inhibitory activities of various pyridine, quinoxaline, and triazine derivatives (3a-k, 6a-j and 11a-h) against AChE and BuChE enzymes by following the modified Ellman's method. Read More

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In vitro production of coenzyme A using thermophilic enzymes.

Appl Environ Microbiol 2021 May 14. Epub 2021 May 14.

International Center for Biotechnology, Osaka University, Yamadaoka 2-1, Suita, Osaka, 565-0871, Japan

Coenzyme A (CoA) is an essential cofactor present in all domains of life and is involved in numerous metabolic pathways, including fatty acid metabolism, pyruvate oxidation through the TCA cycle, and production of secondary metabolites. This characteristic makes CoA a commercially valuable compound in the pharmaceutical, cosmetic, and clinical industries. However, CoA is difficult to accumulate in living cells at a high level as it is consumed in multiple metabolic pathways, hampering its manufacturing by typical cell cultivation and extraction approaches. Read More

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The regulation of protein acetylation influences the redox homeostasis to protect the heart.

Life Sci 2021 May 11:119599. Epub 2021 May 11.

Department of Cardiovascular Biomedicine, National Institute of Cardiology, Ignacio Chávez, 14080 Mexico City, Mexico. Electronic address:

The cellular damage caused by redox imbalance is involved in the pathogenesis of many cardiovascular diseases. Besides, redox imbalance is related to the alteration of protein acetylation processes, causing not only chromatin remodeling but also disturbances in so many processes where protein acetylation is involved, such as metabolism and signal transduction. The modulation of acetylases and deacetylases enzymes aids in maintaining the redox homeostasis, avoiding the deleterious cellular effects associated with the dysregulation of protein acetylation. Read More

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Comprehensive Understanding of the Relationship between Bioactive Compounds of Black Tea and its Angiotensin Converting Enzyme (ACE) Inhibition and Antioxidant Activity.

Plant Foods Hum Nutr 2021 May 14. Epub 2021 May 14.

College of Food Engineering and Nutritional Science, Shaanxi Normal University, Xi'an, 710119, People's Republic of China.

Long term regular intake of black tea (BT) can lower blood pressure, which is probably due to its antioxidant activity and angiotensin converting enzymes (ACE) inhibitory activity. This study achieves a comprehensive understanding of the relationship between bioactive compounds of BT and its ACE inhibitory activity and antioxidant activity. Phenolic compounds are closely related to antioxidant activity and ACE inhibitory activity. Read More

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[Mechanism of microRNA-29a regulating steatosis in the human hepatocyte via targeting silent mating type information regulation 2 homolog-1].

Wei Sheng Yan Jiu 2021 Mar;50(2):284-288

Key Laboratory of Trace Element Nutrition, National Health Commission of the People's Republic of China;National Institute for Nutrition and Health, Chinese Center for Disease Control and Prevention, Beijing 100050, China.

Objective: To investigate the expression of microRNA-29 a(miR-29 a) in the human steatotic hepatocyte model and the mechanism of targeting silent mating type information regulation 2 homolog-1(Sirt1)to regulate fat deposition of steatotic hepatocyte.

Methods: The nonalcoholic fatty liver cell model was induced by a mixture of oleic acid and palmitic acid. After successful validation model, the expression of miR-29 a and Sirt1 was measured by PCR. Read More

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Toxic response of the freshwater green algae Chlorella pyrenoidosa to combined effect of flotation reagent butyl xanthate and nickel.

Environ Pollut 2021 May 3;286:117285. Epub 2021 May 3.

School of Water Resources and Environment, Research Center of Environmental Science and Engineering, China University of Geosciences (Beijing), 29 Xueyuan Road, Haidian District, 100083, Beijing, China.

Butyl Xanthate (BX) is a typical flotation reagent used to extract non-ferrous nickel ores, discharged into the surrounding environment of mining areas in large quantities. However, few studies have focused on the toxicity of combined pollution of BX and nickel (Ni) on aquatic plants, especially phytoplankton, the main producer of aquatic ecosystems. The toxicity and potential mechanism of single and combined pollution of BX and Ni at different concentrations (0-20 mg L) on typical freshwater algae (Chlorella pyrenoidosa) were studied. Read More

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Improving the quality and in vitro fertilization rate of frozen-thawed semen of buffalo (Bubalus bubalis) bulls with the inclusion of vitamin B in the cryopreservation medium.

Anim Reprod Sci 2021 May 5;229:106761. Epub 2021 May 5.

Department of Zoology, Kabal Degree College, Swat, KP, Pakistan.

This study was designed to evaluate the effects of vitamin B in cryopreservation medium on frozen-thawed semen of buffalo (Bubalus Bubalis) bulls. Semen from five bulls (fertility-proven) were diluted in five aliquots not supplemented (control), or supplemented with 1, 2, 4, or 5 mg/mL of vitamin B and evaluated using the Computer Assisted Sperm motion Analysis, antioxidant enzymes, lipid peroxidation (LPO), reactive oxygen species (ROS), ATP concentrations, and in vitro fertilization rate (%). Sperm progressive motility, rapid velocity (%), mitochondrial potential, and acrosome integrity were greater (P < 0. Read More

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Promising anti-SARS-CoV-2 drugs by effective dual targeting against the viral and host proteases.

Bioorg Med Chem Lett 2021 May 10:128099. Epub 2021 May 10.

Research Institute for Medical and Health sciences, University of Sharjah, P.O. Box 27272, Sharjah, UAE; College of Pharmacy, University of Sharjah, P.O. Box 27272, Sharjah, UAE. Electronic address:

SARS-CoV-2 caused dramatic health, social and economic threats to the globe. With this threat, the expectation of future outbreak, and the shortage of anti-viral drugs, scientists were challenged to develop novel antivirals. The objective of this study is to develop novel anti-SARS-CoV-2 compounds with dual activity by targeting valuable less-mutated enzymes. Read More

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Huprine Y - tryptophan heterodimers with potential implication to Alzheimer's disease treatment.

Bioorg Med Chem Lett 2021 May 10:128100. Epub 2021 May 10.

Biomedical Research Centre, University Hospital Hradec Kralove, Sokolska 581, 500 05 Hradec Kralove, Czech Republic; Department of Toxicology and Military Pharmacy, Faculty of Military Health Sciences, Trebesska 1575, 500 01 Hradec Kralove, Czech Republic. Electronic address:

The search for novel and effective therapeutics for Alzheimer's disease (AD) is the main quest that remains to be resolved. The goal is to find a disease-modifying agent able to confront the multifactorial nature of the disease positively. Herewith, a family of huprineY-tryptophan heterodimers was prepared, resulting in inhibition of cholinesterase and neuronal nitric oxide synthase enzymes, with effect against amyloid-beta (Aβ) and potential ability to cross the blood-brain barrier. Read More

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A new mechanism of obeticholic acid on NASH treatment by inhibiting NLRP3 inflammasome activation in macrophage.

Metabolism 2021 May 10:154797. Epub 2021 May 10.

Laboratory of Anti-inflammation, Shanghai, Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, PR China. Electronic address:

Objective: Obeticholic acid (OCA) has been proved to play potential therapeutic effect on nonalcoholic steatohepatitis (NASH). Up to now, the study of OCA on NLRP3 inflammasome activation in macrophage is still blank and merits great attention. Here, we aimed to better characterize the role and mechanism of OCA on NASH treatment focusing on NLRP3 inflammasome activation in macrophages. Read More

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PanD Structure-Function Analysis and Identification of a Potent Pyrazinoic Acid-Derived Enzyme Inhibitor.

ACS Chem Biol 2021 May 13. Epub 2021 May 13.

School of Biological Sciences, Nanyang Technological University, 60 Nanyang Drive, Singapore 637551, Republic of Singapore.

A common strategy employed in antibacterial drug discovery is the targeting of biosynthetic processes that are essential and specific for the pathogen. Specificity in particular avoids undesirable interactions with potential enzymatic counterparts in the human host, and it ensures on-target toxicity. Synthesis of pantothenate (Vitamine B5), which is a precursor of the acyl carrier coenzyme A, is an example of such a pathway. Read More

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Ras Signaling in Breast Cancer.

Authors:
Aree Moon

Adv Exp Med Biol 2021 ;1187:81-101

College of Pharmacy, Duksung Women's University, Seoul, South Korea.

Ras proteins mediate extracellular and cytoplasmic signaling networks via receptor tyrosine kinase. The Ras pathway induces activation of signaling molecules involved in cell proliferation and growth, cell survival and apoptosis, metabolism, and motility. Although Ras mutations in breast cancer are not frequently reported, hyperactivation of Ras signaling plays an important role in breast cancer growth and progression. Read More

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January 2021

Potential Environmental Health Risk Analysis of Neonicotinoids and a Synergist.

Environ Sci Technol 2021 May 13. Epub 2021 May 13.

State Key Laboratory of Food Science and Technology, Jiangnan University, Wuxi, Jiangsu 214122, People's Republic of China.

The extensive use of neonicotinoid pesticides has led to their widespread presence in the environment, resulting in considerable safety risks to the ecosystem and human health. In this study, we investigated the biotransformation behavior of a cocktail of multiple neonicotinoids and piperonyl butoxide (PBO) synergist and their potential environmental health risk. It was found that neonicotinoids with a cyano group, such as acetamiprid and thiacloprid, tended to accumulate in liver and spleen tissues, while others with nitro groups (imidacloprid, thiamethoxam, clothianidin, dinotefuran, and nitenpyram) were mostly excreted in urine. Read More

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[Study on drug-target binding kinetics profiles of flavonoids in Chrysanthemum morifolium and xanthine oxidase].

Zhongguo Zhong Yao Za Zhi 2021 Apr;46(7):1822-1831

Institute of Information on Traditional Chinese Medicine, China Academy of Chinese Medical Sciences Beijing 100700, China.

Based on the target occupancy mathematical model, the binding kinetic process of potential active ingredients of lowering uric acid in Chrysanthemum morifolium with xanthine oxidase(XOD) was evaluated. The potential active ingredients of lowering uric acid in Ch. morifolium were screened by UPLC-Q-Exactivems MS technology, reference substance identification and in vitro enzymatic kinetics experiments. Read More

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Dual-Knockout of Mutant Isocitrate Dehydrogenase 1 and 2 Subtypes towards Glioma Therapy: Structural Mechanistic insights on the role of Vorasidenib.

Chem Biodivers 2021 May 12. Epub 2021 May 12.

University of KwaZulu-Natal, Westville, School of Health Sciences, School of Health Sciences, University of, Not Available, 4001, Durban, SOUTH AFRICA.

Mutant isocitrate dehydrogenase enzymes 1 and 2 (mIDH1/2) are reported to competitively trigger the conversion of alpha ketoglutarate (αKG) in the presence of NADPH, into 2-hydroxyglutarate (2-HG), an oncogenic stimulator. Although some available FDA-approved drugs have been successful in targeting the mIDH1 and mIDH2, their limited brain penetration capabilities have resulted in a low potential efficacy against glioma. Recently, Vorasidenib (AG-881) has been reported as a therapeutic alternative that exerts potent dual inhibitory activity against mIDH1/2 towards the treatment of low-grade glioma. Read More

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biological activity of Mill. infusion against amyloid -peptide-induced toxicity and inhibition of GSK-3, CK-1, and BACE-1 enzymes relevant to Alzheimer's disease.

Saudi Pharm J 2021 Mar 3;29(3):236-243. Epub 2021 Feb 3.

Department of Pharmacognosy, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey.

species have been traditionally used to improve cognition and have been proved to be a potential natural treatment for Alzheimer's disease. Mill. (Turkish sage or Greek sage) demonstrated to have anticholinergic effects . Read More

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