On-flow enzymatic inhibitor screening: The emerging success of liquid chromatography-based assays
- Biology, ChemistryFrontiers in Analytical Science
This review covers articles from the last decade that combine the use of varied immobilization methods on different solid supports and several equipment setups in on-flow systems, emphasizing the performance and capacity of recognizing and identifying biologically active compounds in various matrices.
Inhibitory activities of grape bioactive compounds against enzymes linked with human diseases
- BiologyApplied Microbiology and Biotechnology
This review crisply encapsulates enzyme inhibitory activities of various grape polyphenols towards different key human-ailment-associated enzymes: xanthine oxidase (gout), tyrosinase (hyperpigmentation), α-amylase and α-glucosidase (diabetes mellitus), pancreatic lipase (obesity), cholinesterase (Alzheimer’s disease), angiotensin i-converting enzymes (hypert
A Comprehensive Guide for Assessing Covalent Inhibition in Enzymatic Assays Illustrated with Kinetic Simulations
- Biology, ChemistryCurrent protocols
Four stepwise protocols to assess the biochemical potency of (ir)reversible covalent enzyme inhibitors targeting a nucleophilic active site residue are included, with accompanying data analysis tailored to the covalENT binding mode.
A review on benefits of mass spectrometry for the small molecule drug discovery
- Biology, Chemistry
The current review describes MS strategies which are used to enhance and accelerate drug identification besides degradation linked impurities in active pharmaceutical ingredients (API) or articulated products.
How Do Enveloped Viruses Exploit the Secretory Proprotein Convertases to Regulate Infectivity and Spread?
Arguments whereby the PCSKs could represent a powerful arsenal to limit viral infections causing the present and future pandemics are presented.
Tanacetum vulgare L. (Tansy) as an effective bioresource with promising pharmacological effects from natural arsenal.
- BiologyFood and chemical toxicology : an international journal published for the British Industrial Biological Research Association
Protein Folding Interdiction Strategy for Therapeutic Drug Development in Viral Diseases: Ebola VP40 and Influenza A M1
- BiologyInternational journal of molecular sciences
The FITR strategy opens a potential new avenue for the design of therapeutic drugs that promises to be effective against infectious diseases, as well as some challenges likely to be found when designing effective therapeutic drugs from the proposed peptide candidates.
Physicochemical Insights on Terahertz Wave Diminished Side Effects of Drugs from Slow Dissociation.
- PsychologyACS nano
Dopamine D2 receptors (D2Rs) are one of the most intensely investigated and well-established drug targets for neuropsychiatric disorders. Selective D2R antagonists have been developed as efficacious…
Metabolomics-Based Pharmacodynamic Analysis of Zhuang Yao Shuang Lu Tong Nao Granules in a Rat Model of Ischemic Cerebral Infarction
- Biology, PsychologyAnalytical cellular pathology
This metabolomics-based study showed that YHT could be used to treat ischemic stroke by modulating changes in endogenous metabolites in rats with cerebral ischemia.
Renewable processes of synthesis of biolubricants catalyzed by lipases
- ChemistryJournal of Environmental Chemical Engineering
SHOWING 1-10 OF 110 REFERENCES
Defining Balanced Conditions for Inhibitor Screening Assays That Target Bisubstrate Enzymes
- Biology, ChemistryJournal of biomolecular screening
A theoretical analysis is provided, on the basis of the Cheng-Prusoff derivation, of the IC50/K i relationship of bisubstrate enzyme reactions following various sequential kinetic mechanisms, as well as the application and limitations of this information for defining optimal screening conditions for such enzymes.
Pharmacological Chaperones: Design and Development of New Therapeutic Strategies for the Treatment of Conformational Diseases.
- BiologyACS chemical biology
This work reviews therapeutic strategies, clinical potentials, and cost-benefit impacts of several classes of pharmacological chaperones for the treatment of a series of conformational diseases.
Statistical Mechanics of Allosteric Enzymes.
- Biology, ChemistryThe journal of physical chemistry. B
This work models allosteric enzymes and their interaction with two key molecular players-allosteric regulators and competitive inhibitors and applies this model to characterize existing data on enzyme activity, comment on how enzyme parameters can be experimentally tuned, and make novel predictions on how to control phenomena such as substrate inhibition.
Structural basis for ligand binding to an enzyme by a conformational selection pathway
- Chemistry, BiologyProceedings of the National Academy of Sciences
A molecular description of a high-energy enzyme state in a conformational selection pathway is presented by an experimental strategy centered on NMR spectroscopy, protein engineering, and X-ray crystallography and it is discovered that the structural sampling of the substrate free enzyme corresponds to the complete amplitude that is associated with formation of the closed and catalytically active state.
High performance enzyme kinetics of turnover, activation and inhibition for translational drug discovery
- BiologyExpert opinion on drug discovery
In vivo enzyme and substrate abundance and their dynamics, binding modality, drug binding kinetics and enzyme’s position in metabolic networks should be assessed to gauge the translational impact on drug efficacy and safety and integrating these factors in a systems biology and systems pharmacology model should facilitate translational drug discovery.
Protein Allostery in Rational Drug Design.
- BiologyAdvances in experimental medicine and biology
This chapter focuses on protein kinases that transfer the phosphate group of ATP to the hydroxyl group of a substrate protein, and a protein kinase inhibitor bound to the allosteric region is advantageous in terms of selectivity compared to the traditional ATP-competitive one.
Targeted protein degradation as a powerful research tool in basic biology and drug target discovery
- BiologyNature Structural & Molecular Biology
This Review summarizes recent developments in this field, with a particular focus on the use of degraders as research tools to interrogate complex biological problems.
Targeted protein degradation and the enzymology of degraders.
- BiologyCurrent opinion in chemical biology
Mechanism of Selective Enzyme Inhibition through Uncompetitive Regulation of an Allosteric Agonist.
- Biology, ChemistryJournal of the American Chemical Society
It is discovered that CE3F4R binds within the EPAC cAMP-binding domain (CBD) at a subdomain interface distinct from the cAMP binding site, acting as a wedge that stabilizes a cAMP -bound mixed-intermediate.
Activity-based protein profiling: from enzyme chemistry to proteomic chemistry.
- BiologyAnnual review of biochemistry
The basic technology of ABPP, the enzyme classes addressable by this method, and the biological discoveries attributable to its application are reviewed.