Articles with "pharmacological characterization" as a keyword



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Pharmacological Characterization of the RPMI 2650 Model as a Relevant Tool for Assessing the Permeability of Intranasal Drugs.

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Published in 2018 at "Molecular pharmaceutics"

DOI: 10.1021/acs.molpharmaceut.8b00087

Abstract: The RPMI 2650 cell line has been described as a potent model of the human nasal mucosa. Nevertheless, pharmacological data are still insufficient, and the role of drug efflux transporters has not been fully elucidated.… read more here.

Keywords: pharmacological characterization; model; rpmi 2650; tool assessing ... See more keywords
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Pharmacological characterization of linzagolix, a novel, orally active, non‐peptide antagonist of gonadotropin‐releasing hormone receptors

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Published in 2022 at "Clinical and Experimental Pharmacology and Physiology"

DOI: 10.1111/1440-1681.13688

Abstract: Control of gonadotropin‐releasing hormone (GnRH) signalling is an effective strategy for the treatment of sex hormone‐dependent diseases. GnRH analogues have been widely used for treating these diseases; however, initial stimulation or complete suppression of GnRH… read more here.

Keywords: releasing hormone; gonadotropin releasing; hormone; pharmacological characterization ... See more keywords
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Identification and pharmacological characterization of succinate receptor agonists

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Published in 2017 at "British Journal of Pharmacology"

DOI: 10.1111/bph.13738

Abstract: The succinate receptor (formerly GPR91 or SUCNR1) is described as a metabolic sensor that may be involved in homeostasis. Notwithstanding its implication in important (patho)physiological processes, the function of succinate receptors has remained ill‐defined because… read more here.

Keywords: pharmacological characterization; succinate receptor; identification pharmacological; succinate ... See more keywords
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Abstract 4418: Pharmacological characterization of a preclinical candidate covalently inhibiting CDK12

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Published in 2019 at "Cancer Research"

DOI: 10.1158/1538-7445.sabcs18-4418

Abstract: Cyclin-dependent kinase 12 (CDK12) is a transcription-associated protein that plays a critical role in DNA damage response, splicing, pre-mRNA processing and is crucial for maintaining genomic stability. CDK12 associated with Cyclin K (CycK) regulates transcription… read more here.

Keywords: cdk12; preclinical candidate; characterization preclinical; cancer ... See more keywords

Integrated molecular and pharmacological characterization of patient-derived xenografts from bladder and ureteral cancers identifies new potential therapies

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Published in 2022 at "Frontiers in Oncology"

DOI: 10.3389/fonc.2022.930731

Abstract: Background Muscle-invasive bladder cancer (MIBC) and upper urinary tract urothelial carcinoma (UTUC) are molecularly heterogeneous. Despite chemotherapies, immunotherapies or anti-FGFR treatments, these tumors are still of poor outcome. Our objective was to develop a bank… read more here.

Keywords: derived xenografts; pharmacological characterization; pdxs; patient ... See more keywords
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Identification and Pharmacological Characterization of Two Serotonin Type 7 Receptor Isoforms from Mythimna separata

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Published in 2022 at "International Journal of Molecular Sciences"

DOI: 10.3390/ijms24010655

Abstract: Serotonin (5-hydroxytryptamine, 5-HT) is an important neuroactive molecule, as neurotransmitters regulate various biological functions in vertebrates and invertebrates by binding and activating specific 5-HT receptors. The pharmacology and tissue distribution of 5-HT receptors have been… read more here.

Keywords: pharmacology; pharmacological characterization; receptor isoforms; mythimna separata ... See more keywords
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Design, Pharmacological Characterization, and Molecular Docking of Minimalist Peptidomimetic Antagonists of α4β1 Integrin

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Published in 2023 at "International Journal of Molecular Sciences"

DOI: 10.3390/ijms24119588

Abstract: Integrin receptors mediate cell–cell interactions via the recognition of cell-adhesion glycoproteins, as well as via the interactions of cells with proteins of the extracellular matrix, and upon activation they transduce signals bi-directionally across the cell… read more here.

Keywords: molecular docking; design pharmacological; cell; docking minimalist ... See more keywords