Aldehyde‐Based Inhibitors of the Peptidoglycan O‐Acetylesterase Ape
Sign Up to like & getrecommendations! Published in 2023 at "ChemBioChem"
DOI: 10.1002/cbic.202300205
Abstract: The O‐acetylation of the muramic acid residues in peptidoglycan (PG) is a modification that protects the bacteria from lysis due to the action of lysozyme. In Gram‐negative bacteria, deacetylation is required to allow lytic transglycosylases… read more here.
Keywords: inhibitors peptidoglycan; ape; peptidoglycan acetylesterase; acetylesterase ape ... See more keywords
Structure-Activity Relationships of Metal-Based Inhibitors of the Mitochondrial Calcium Uniporter.
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DOI: 10.1002/cmdc.202300106
Abstract: The mitochondrial calcium uniporter (MCU) is a transmembrane protein that is responsible for mediating mitochondrial calcium (mCa2+) uptake. Given this critical function, the MCU has been implicated as an important target for addressing various human… read more here.
Keywords: calcium uniporter; metal based; metal; mitochondrial calcium ... See more keywords
Thiazole‐Based IL‐17 Inhibitors Discovered by Scaffold Morphing
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DOI: 10.1002/cmdc.202400851
Abstract: The pro‐inflammatory cytokine interleukin‐17A (IL‐17) plays an important role in the body's defense against bacterial and fungal infections. However, overexpression of IL‐17 has been associated with several diseases, including rheumatoid arthritis, asthma, psoriasis, and even… read more here.
Keywords: based inhibitors; scaffold morphing; discovered scaffold; thiazole based ... See more keywords
Involvement of sialoglycans in SARS‐COV‐2 infection: Opportunities and challenges for glyco‐based inhibitors
Sign Up to like & getrecommendations! Published in 2022 at "Iubmb Life"
DOI: 10.1002/iub.2692
Abstract: Viral infections have been the causes of global pandemics, including the ongoing coronavirus disease 2019, which prompted the investigation into the infection mechanisms to find treatment and aid the vaccine design. Betacoronaviruses use spike glycoprotein… read more here.
Keywords: challenges glyco; infection; glyco based; opportunities challenges ... See more keywords
Molecular design, synthesis and biological evaluation of cage compound-based inhibitors of hepatitis C virus p7 ion channels.
Sign Up to like & getrecommendations! Published in 2018 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2018.08.009
Abstract: The hepatitis C caused by the hepatitis C virus (HCV) is an acute and/or chronic liver disease ranging in severity from a mild brief ailment to a serious lifelong illness that affects up to 3%… read more here.
Keywords: ion; hepatitis virus; compound based; cage compound ... See more keywords
Development of phosphorus-based inhibitors for PCDD/Fs suppression.
Sign Up to like & getrecommendations! Published in 2020 at "Waste management"
DOI: 10.1016/j.wasman.2020.09.019
Abstract: Inhibition mechanisms of sulfur-, nitrogen- and phosphorus- based inhibitors on the de novo synthesis of polychlorinated dibenzo-p-dioxins, and dibenzofurans (PCDD/F) were studied by exploring speciation evolution of carbon, chorine and copper in fly ash under… read more here.
Keywords: phosphorus based; development phosphorus; inhibition; phosphorus ... See more keywords
Optimized Ebselen-Based Inhibitors of Bacterial Ureases with Nontypical Mode of Action
Sign Up to like & getrecommendations! Published in 2023 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01799
Abstract: Screening of 25 analogs of Ebselen, diversified at the N-aromatic residue, led to the identification of the most potent inhibitors of Sporosarcina pasteurii urease reported to date. The presence of a dihalogenated phenyl ring caused… read more here.
Keywords: ureases nontypical; ebselen based; bacterial ureases; inhibitors bacterial ... See more keywords
Selectivity analysis of diaminopyrimidine-based inhibitors of MTHFD1, MTHFD2 and MTHFD2L
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DOI: 10.1038/s41598-024-71879-1
Abstract: The mitochondrial enzyme methylenetetrahydrofolate dehydrogenase (MTHFD2) is involved in purine and thymidine synthesis via 1C metabolism. MTHFD2 is exclusively overexpressed in cancer cells but absent in most healthy adult human tissues. However, the two close… read more here.
Keywords: inhibitors mthfd2; mthfd2l; mthfd1 mthfd2; based inhibitors ... See more keywords
Phosphinic acid-based inhibitors of tubulin polyglycylation.
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DOI: 10.1039/d2cc01783k
Abstract: Tubulin polyglycylation is a posttranslational modification that occurs primarily on the axonemes of flagella and cilia and has been shown to be essential for proper sperm motility. Inhibitors of both the initiase and elongase ligases… read more here.
Keywords: tubulin polyglycylation; polyglycylation; acid based; phosphinic acid ... See more keywords
Examination of sulfonamide-based inhibitors of MMP3 using the conditioned media of invasive glioma cells
Sign Up to like & getrecommendations! Published in 2020 at "Journal of Enzyme Inhibition and Medicinal Chemistry"
DOI: 10.1080/14756366.2020.1715387
Abstract: Abstract Glioblastoma multiforme (GBM) is the deadliest and the most common primary malignant brain tumour. The median survival for patients with GBM is around one year due to the nature of glioma cells to diffusely… read more here.
Keywords: conditioned media; glioma; sulfonamide based; glioma cells ... See more keywords
An overview: metal-based inhibitors of urease.
Sign Up to like & getrecommendations! Published in 2022 at "Journal of enzyme inhibition and medicinal chemistry"
DOI: 10.1080/14756366.2022.2150182
Abstract: Urease is a kind of nickel-dependent metalloenzyme, which exists in the biological world widely, and can catalyse the hydrolysis of urea into ammonia and carbon dioxide to provide a nitrogen source for organisms. Urease has… read more here.
Keywords: inhibition; inhibitors urease; metal based; overview metal ... See more keywords