Quinoline‐Conjugated Ruthenacarboranes: Toward Hybrid Drugs with a Dual Mode of Action
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DOI: 10.1002/cmdc.201900349
Abstract: The role of autophagy in cancer is often complex, ranging from tumor‐promoting to ‐suppressing effects. In this study, two novel hybrid molecules were designed, containing a ruthenacarborane fragment conjugated with a known modulator of autophagy,… read more here.
Keywords: dual mode; quinoline conjugated; conjugated ruthenacarboranes; mode action ... See more keywords
Elucidation of an Allosteric Mode of Action for a Thienopyrazole RORγt Inverse Agonist
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DOI: 10.1002/cmdc.202000044
Abstract: The demand for allosteric targeting of nuclear receptors is high, but examples are limited, and structural information is scarce. The retinoic acid‐related orphan receptor gamma t (RORγt) is an important transcriptional regulator for the differentiation… read more here.
Keywords: allosteric mode; elucidation allosteric; ror; thienopyrazole ror ... See more keywords
Discovery and structure-activity relationships of the quinolinequinones: Promising antimicrobial agents and mode of action evaluation.
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DOI: 10.1002/ddr.21893
Abstract: In our pursuit of developing the novel, potent, and selective antimicrobial agents, we managed to obtain the quinolinequinone for their antimicrobial profile with minimal inhibitory concentrations (MICs) determined against a panel of seven bacterial strains… read more here.
Keywords: activity; structure activity; mode action; antimicrobial agents ... See more keywords
Mode of action and human relevance assessment of male CD‐1 mouse renal adenocarcinoma associated with lifetime exposure to empagliflozin
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Applied Toxicology"
DOI: 10.1002/jat.4329
Abstract: Inhibition of sodium‐glucose cotransporter‐2 (SGLT2) has been shown to be a safe and efficacious approach to support managing Type 2 diabetes. In the 2‐year carcinogenicity study with the SGLT2 inhibitor empagliflozin in CD‐1 mice, an… read more here.
Keywords: mouse renal; male mouse; mode action; mice ... See more keywords
Synthesis, bioactivity and mode of action of 5A 5B 6C tricyclic spirolactones as novel antiviral lead compounds.
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DOI: 10.1002/ps.5115
Abstract: BACKGROUND Plant viral diseases cause tremendous decreases in yield and quality. Natural polycyclic compounds such as those containing carbocycles are often very important lead compounds for drug and pesticide development. Tricyclic spiranoid lactones with 5A… read more here.
Keywords: lead compounds; synthesis bioactivity; tricyclic spirolactones; mode action ... See more keywords
Pyrethroid neurotoxicity studies with bifenthrin indicate a mixed Type I/II mode of action†
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DOI: 10.1002/ps.5300
Abstract: Abstract BACKGROUND Bifenthrin is usually considered a Type I pyrethroid, because it lacks an α‐CN group present in Type II pyrethroids, but some previous studies suggest a mixed Type I/II mode‐of‐action. Results are presented for… read more here.
Keywords: bifenthrin; mixed type; mode action; type ... See more keywords
Aclonifen targets the solanesyl diphosphate synthase, representing a novel mode of action for herbicides.
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DOI: 10.1002/ps.5781
Abstract: BACKGROUND Aclonifen is a unique diphenyl ether herbicide. Despite its structural similarities to known inhibitors of the protoporphyrinogen oxidase (e.g., acifluorfen, bifenox or oxadiazon), which result in leaf necrosis, aclonifen causes a different phenotype that… read more here.
Keywords: representing novel; solanesyl diphosphate; mode action; diphosphate synthase ... See more keywords
Bacillus thuringiensis Vegetative Insecticidal Protein Family Vip3A and Mode of Action against Pest Lepidopteran.
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DOI: 10.1002/ps.5804
Abstract: Vip3A proteins are widely used for controlling pest Lepidoptera. Different binding sites with different receptors in the insect midgut membrane and lack of cross-resistance with Cry proteins enhance their applicability, as both single proteins and… read more here.
Keywords: insecticidal; vip3a; vip3a proteins; protein family ... See more keywords
Activity, selection response and molecular mode of action of the isoxazoline afoxolaner in Tetranychus urticae.
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DOI: 10.1002/ps.7187
Abstract: BACKGROUND Afoxolaner is a novel representative of the isoxazolines, a class of ectoparasiticides which has been commercialised for the control of tick and flea infestations in dogs. In this study, the biological efficacy of afoxolaner… read more here.
Keywords: afoxolaner; tetranychus urticae; mode action; molecular mode ... See more keywords
Determining the Mode of Action of Antimalarial Drugs Using Time-Resolved LC-MS-Based Metabolite Profiling.
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DOI: 10.1007/978-1-4939-8757-3_12
Abstract: Methods for assessing the mode of action of new antimalarial compounds identified in high throughput phenotypic screens are needed to triage and facilitate lead compound development and to anticipate potential resistance mechanisms that might emerge.… read more here.
Keywords: time; determining mode; time resolved; action antimalarial ... See more keywords
An evaluation of the molecular mode of action of trans-resveratrol in the Porphyromonas gingivalis lipopolysaccharide challenged neuronal cell model.
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DOI: 10.1007/s11033-020-06024-y
Abstract: Porphyromonas gingivalis triggers a range of innate immune responses in the host that may contribute to the development of periodontitis and dementing diseases including Alzheimer's disease (AD). This study aimed to assess the mode of… read more here.
Keywords: action trans; porphyromonas gingivalis; mode action; gingivalis lipopolysaccharide ... See more keywords