SARS‐CoV‐2‐encoded inhibitors of human LINE‐1 retrotransposition
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medical Virology"
DOI: 10.1002/jmv.28135
Abstract: The ongoing pandemic of severe acute respiratory coronavirus 2 (SARS‐CoV‐2) is causing a devastating impact on public health worldwide. However, details concerning the profound impact of SARS‐CoV‐2 on host cells remain elusive. Here, we investigated… read more here.
Keywords: inhibitors human; human line; cov encoded; line retrotransposition ... See more keywords
Discovery of novel inhibitors of human galactokinase by virtual screening
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Computer-Aided Molecular Design"
DOI: 10.1007/s10822-019-00190-3
Abstract: Classic Galactosemia is a potentially lethal autosomal recessive metabolic disorder caused by deficient galactose-1-phosphate uridyltransferase (GALT) that results in the buildup of galactose-1-phosphate (gal-1-p) in cells. Galactokinase (GALK1) is the enzyme responsible for converting galactose… read more here.
Keywords: virtual screening; inhibitors human; discovery novel; novel inhibitors ... See more keywords
Novel venom‐derived inhibitors of the human EAG channel, a putative antiepileptic drug target
Sign Up to like & getrecommendations! Published in 2018 at "Biochemical Pharmacology"
DOI: 10.1016/j.bcp.2018.08.038
Abstract: &NA; Recently, we and other groups revealed that gain‐of‐function mutations in the human ether à go‐go voltage‐gated potassium channel hEAG1 (Kv10.1) lead to developmental disorders with associated infantile‐onset epilepsy. However, the physiological role of hEAG1… read more here.
Keywords: derived inhibitors; human eag; inhibitors human; channel ... See more keywords
Design and synthesis of 3,5-substituted 1,2,4-oxadiazoles as catalytic inhibitors of human DNA topoisomerase IIα.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.103828
Abstract: Cancer constitutes a group of diseases linked to abnormal cell growth that can potentially spread to other parts of the body and is one of the most common causes of death. The molecular motors -… read more here.
Keywords: design synthesis; inhibitors human; synthesis substituted; catalytic inhibitors ... See more keywords
Structure-Based Prototyping of Allosteric Inhibitors of Human Uridine/Cytidine Kinase 2 (UCK2).
Sign Up to like & getrecommendations! Published in 2022 at "Biochemistry"
DOI: 10.1021/acs.biochem.2c00451
Abstract: Pyrimidine nucleotide biosynthesis in humans is a promising chemotherapeutic target for infectious diseases caused by RNA viruses. Because mammalian cells derive pyrimidine ribonucleotides through a combination of de novo biosynthesis and salvage, combined inhibition of… read more here.
Keywords: inhibitors human; kinase uck2; cytidine kinase; uridine cytidine ... See more keywords
Sulfonamide Inhibitors of Human Carbonic Anhydrases Designed through a Three-Tails Approach: Improving Ligand/Isoform Matching and Selectivity of Action
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.0c00733
Abstract: The “tail approach” has become a milestone in human carbonic anhydrase inhibitor (hCAI) design for various therapeutics, including antiglaucoma agents. Besides the classical hydrophobic/hydrophilic division of hCAs active site, several subpockets have been identified at… read more here.
Keywords: human carbonic; inhibitors human; carbonic anhydrases; sulfonamide inhibitors ... See more keywords
Human Neuraminidases: Structures and Stereoselective Inhibitors.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01612
Abstract: This Perspective describes the classification, structures, substrates, mechanisms of action, and implications of human neuraminidases (hNEUs) in various pathologies. Some inhibitors have been developed for each isoform, leading to more precise interactions with hNEUs. Although… read more here.
Keywords: inhibitors human; structures stereoselective; inhibition; human neuraminidases ... See more keywords
Synthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c01913
Abstract: Novel analogues of C-2-substituted thienopyrimidine-based bisphosphonates (C2-ThP-BPs) are described that are potent inhibitors of the human geranylgeranyl pyrophosphate synthase (hGGPPS). Members of this class of compounds induce target-selective apoptosis of multiple myeloma (MM) cells and… read more here.
Keywords: inhibitors human; geranylgeranyl pyrophosphate; thienopyrimidine based; pyrophosphate synthase ... See more keywords
Chirality-Driven Mode of Binding of α-Aminophosphonic Acid-Based Allosteric Inhibitors of the Human Farnesyl Pyrophosphate Synthase (hFPPS).
Sign Up to like & getrecommendations! Published in 2019 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.9b01104
Abstract: Thienopyrimidine-based allosteric inhibitors of the human farnesyl pyrophosphate synthase (hFPPS), characterized by a chiral α-aminophosphonic acid moiety, were synthesized as enantiomerically enriched pairs and their binding mode was investigated by X-ray crystallography. A general consensus… read more here.
Keywords: farnesyl pyrophosphate; based allosteric; human farnesyl; allosteric inhibitors ... See more keywords
Discovery and Optimization of Rationally Designed Bicyclic Inhibitors of Human Arginase to Enhance Cancer Immunotherapy.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.0c00058
Abstract: The action of arginase, a metalloenzyme responsible for the hydrolysis of arginine to urea and ornithine, is hypothesized to suppress immune-cell activity within the tumor microenvironment, and thus its inhibition may constitute a means by… read more here.
Keywords: optimization rationally; discovery optimization; inhibitors human; human arginase ... See more keywords
Identification of new inhibitors against human Great wall kinase using in silico approaches
Sign Up to like & getrecommendations! Published in 2018 at "Scientific Reports"
DOI: 10.1038/s41598-018-23246-0
Abstract: Microtubule associated serine/threonine kinase (MASTL) is an important Ser/Thr kinase belonging to the family of AGC kinases. It is the human orthologue of Greatwall kinase (Gwl) that plays a significant role in mitotic progression and… read more here.
Keywords: identification new; human great; kinase; inhibitors human ... See more keywords