Results 51 to 60 of about 27,225 (279)

Small-Molecule Inhibitors of Carboxylesterase Notum

open access: yesFuture Medicinal Chemistry, 2021
Notum has recently been identified as a negative regulator of Wnt signaling through the removal of an essential palmitoleate group from Wnt proteins. There are emerging reports that Notum plays a role in human disease, with published data suggesting that targeting Notum could represent a new therapeutic approach for treating cancer, osteoporosis and ...
Yuguang Zhao   +4 more
openaire   +3 more sources

Understanding and Overcoming Antibody‐Drug Conjugate Resistance: Biological Mechanisms and Emerging Analytical Frameworks in Breast Cancer

open access: yesAdvanced Science, EarlyView.
Antibody–drug conjugates (ADCs) transform breast cancer therapy, yet resistance limits their durability. Emerging evidence reveals that ADC failure is not solely tumor‐intrinsic but shaped by dynamic tumor–microenvironment interactions that alter drug delivery, processing, and response.
Minji Seo, Jangsoon Lee, Naoto T. Ueno
wiley   +1 more source

Malathion Resistance in Larvae of Some Southern Minnesota Populations of the Indianmeal Moth,\u3ci\u3e Plodia Interpunctella\u3c/i\u3e (Lepidoptera: Pyralidae), Infesting Bulk-Stored Shelled Corn [PDF]

open access: yes, 2017
Larvae of 21 field collected populations of the Indianmeal moth, Plodia interpunctella, infesting stored shelled corn in southern Minnesota were tested for their susceptibility to malathion in the laboratory.
Harein, P. K   +2 more
core   +1 more source

Modulation of paraoxonase 1 and 3 expression after moderate exercise training in the rat

open access: yesJournal of Lipid Research, 2009
Paraoxonases (PONs) are a small family of antioxidant enzymes whose antiatherogenic activity is well known. The aim of the present study was the evaluation of the effects of moderate aerobic training on their expression using a rat model.
Rita Romani   +8 more
doaj   +1 more source

A genomic amplification affecting a carboxylesterase gene cluster confers organophosphate resistance in the mosquito Aedes aegypti: From genomic characterization to high‐throughput field detection

open access: yesEvolutionary Applications, 2021
By altering gene expression and creating paralogs, genomic amplifications represent a key component of short‐term adaptive processes. In insects, the use of insecticides can select gene amplifications causing an increased expression of detoxification ...
Julien Cattel   +13 more
doaj   +1 more source

The quantitative impact of metabolism‐inhibiting drugs on the occurrence of adverse drug reactions—A backward selection approach

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Abstract Aim The quantitative effect of several inhibitory drugs on the development of adverse drug reactions (ADRs) is currently difficult to estimate. Our aim was to identify metabolic pathways, which, when inhibited, increase the risk for certain ADRs, and to use this system to consider comedication at individual level. Methods Data of a prospective
Judith Berres   +8 more
wiley   +1 more source

Identification, Characterization, and Preliminary X-ray Diffraction Analysis of a Novel Esterase (ScEst) from Staphylococcus chromogenes

open access: yesCrystals, 2022
Ester prodrugs can develop novel antibiotics and have potential therapeutic applications against multiple drug-resistant bacteria. The antimicrobial activity of these prodrugs is activated after being cleaved by the esterases produced by the pathogen ...
Jisub Hwang   +8 more
doaj   +1 more source

Structural and biochemical characterisation of Archaeoglobus fulgidus esterase reveals a bound CoA molecule in the vicinity of the active site [PDF]

open access: yes, 2016
A new carboxyl esterase, AF-Est2, from the hyperthermophilic archaeon Archaeoglobus fulgidus has been cloned, over-expressed in Escherichia coli and biochemically and structurally characterized. The enzyme has high activity towards short- to medium-chain
Finnigan, W   +7 more
core   +1 more source

The interplay between molecular architecture, pharmacology, and suspected adverse drug reactions associated with nonsteroidal androgen antagonists in the United Kingdom

open access: yesBritish Journal of Clinical Pharmacology, EarlyView.
Aims This work aimed to correlate potential links between the suspected adverse drug reaction (ADR) profile of licensed nonsteroidal androgen receptor antagonists (NSARA) with their unique chemical properties and known off‐target polypharmacology. Methods Physicochemical and polypharmacology data were curated from the Electronic Medicines Compendium ...
Simrit Dhillon   +2 more
wiley   +1 more source

A carboxylesterase, Esterase-6, modulates sensory physiological and behavioral response dynamics to pheromone in Drosophila

open access: yesBMC Biology, 2012
Background Insects respond to the spatial and temporal dynamics of a pheromone plume, which implies not only a strong response to 'odor on', but also to 'odor off'. This requires mechanisms geared toward a fast signal termination.
Chertemps Thomas   +6 more
doaj   +1 more source

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