Current Enzyme Inhibition - Volume 17, Issue 3, 2021

Despite the significant number of irreversible inhibitors developed over the years, strong prejudices remain for this type of therapeutic molecule, particularly in the area of drug development. New generations of covalent targeted inhibitors are, however, in development, and interest is increasingly growing. In fact, the new generation of covalent inhibitors has a weakly reactive species (warhead) that is able, in a particul Read More

Background: Overactivity of fibroblast growth factor receptor 1 (FGFR1) is associated with various tumors, particularly breast cancer, prostate cancer, non-small-cell lung carcinoma, myeloproliferative diseases, which makes this protein kinase a promising therapeutic target for anticancer therapy. Objective: The main aim of this study is to identify novel FGFR1 inhibitors. Methods: In order to find FGFR1 inhibitors, virtual scre Read More

Background and Aims: This study aims to alleviate the microbiologically affected corrosion that occurred by sulfate-reducing bacteria (SRB) through synthesizing a bio-based polyurethane polymer and its nanocomposite coating, silver nanoparticles (PU-Ag). Moreover, it will also evaluate the effect of PU alone and PU-Ag as inhibitors for adenylyl sulfate reductase (APS), the main enzyme for sulfate reduction. Methods: In this s Read More

Background: Plants are the main source of drugs for the therapy of a large number of diseases. Objective: The aim of the present work is to evaluate the in vitro antioxidant and anti-α-amylase and anti- peroxidases (HPR) potentials of phenolic extracts obtained from three spontaneous plants growing in the South of Algeria, namely Chamomilla pubescens, Pulicaria crispa, and Rhanterium adpressum. This is the first repo Read More

Background: The amino acid sequence of an α-amylase of the yeast Saccharomycopsis fibuligera R64 (SfamyR64) contains two putative N-linked glycosylation sites N153 and N224. N224 is hypothetically responsible for the binding of starch substrate because it is highly conserved among SfamyR64 homologs. Objective: To test whether N224 plays a key role in enzyme activity and stability. Methods: N224Q substitution was i Read More

Background: Garlic, being a well-known medicinal plant, is the most commonly used culinary spice worldwide. Investigation of protease inhibitor isolated from garlic leads to a promising contender in pharmacognostic and pharmacological studies. Objective/Introduction: Protease Inhibitor (PI) from 'garlic' (Allium sativum) was analyzed for its biological role as an antioxidant, antimicrobial, and anti-inflammatory agent. Methods: Read More

Background: A series of bis(indolyl)methanes (3a-3o) have been synthesized using a greener and new approach using the reaction of different substituted aldehydes and indole in the presence of an easily available and biodegradable base such as piperidine in acetic acid at room temperature and characterized with UV (Ultraviolet-visible spectroscopy), Gas Chromatography-Mass Spectrometry (GCMS), Proton Nucl Read More

Background: Obesity is a growing global health problem. Obesity leads to cardiovascular disorders, musculoskeletal disorders, diabetes, and certain types of cancer. One of the approaches to controlling and treating obesity has involved inhibition of dietary lipid digestion by pancreatic lipase inhibitors. Microbes and plant sources provide a rich source of enzyme inhibitors, including pancreatic lipase inhibitors that can be devel Read More

Background: Inhibition of α-amylase and α-glucosidase is considered as an important therapeutic target to manage type 2 diabetes mellitus (T2DM), reducing postprandial hyperglycemia (PPHG). Objective: The present work explored the antidiabetic activities of five artificial food colorings by α- amylase and α-glucosidase enzyme inhibition in vitro and in Silico. Methods: In this study, inhibition of α-amylase and α-glucosidas Read More