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Showing 1 to 5 of 5 for “"Receptor variants"”.

  1. Modelling fitness and stability of G protein-coupled receptor variants

    G protein-coupled receptors (GPCRs) are the molecular targets of more than a third of approved drugs1 used in a wide variety of diseases2. Protein-altering genetic variants have complex effects on the biophysical and functional properties of GPCRs. Understanding the biophysical and functional …

    cambridge Repository record for Modelling fitness and stability of G protein-coupled receptor variants (opens in a new tab)

  2. Characterisation of Androgen Receptor Variants in Breast Cancer and the Development of Thieno[2,3-b] Pyridines as Novel Anti-Cancer Compounds

    In Breast Cancer(BCa), steroid receptors play a key role in the progression of the majority tumours. Oestrogen Receptor-α (ERα), for example,drives the growth of approximately 70% of tumours and is therefore a useful therapeutic target for this disease.Interestingly, the Androgen Receptor (AR) is …

    essex Repository record for Characterisation of Androgen Receptor Variants in Breast Cancer and the Development of Thieno[2,3-b] Pyridines as Novel Anti-Cancer Compounds (opens in a new tab)

  3. Cocaine Dependence: The Role of Serotonin Genes In

    … effects of pharmacological agents on serotonin receptors 2a (5-HT2A) and 2c (5-HT2C), have yielded results suggesting that selective 5-HT2A antagonists and 5-HT2C agonists promote the disruption of cocaine-associated memories. One measure of cocaine related cues in humans is attentional bias, in …

    uthsc Repository record for Cocaine Dependence: The Role of Serotonin Genes In (opens in a new tab)

  4. Exploring the therapeutic potential of the apelin receptor signalling axis, and angiotensin-converting enzyme 2 (ACE2) as the SARS-CoV-2 viral entry receptor, in the cardiovascular system

    The apelin receptor is a class A GPCR that binds two endogenous peptide ligands, apelin and elabela/Toddler (ELA), to induce positive cardiac inotropy and vasodilatation in the cardiovascular system. The apelin receptor provides a tractable therapeutic target for multiple cardiovascular diseases, …

    cambridge Repository record for Exploring the therapeutic potential of the apelin receptor signalling axis, and angiotensin-converting enzyme 2 (ACE2) as the SARS-CoV-2 viral entry receptor, in the cardiovascular system (opens in a new tab)

  5. The binding and activation of the glucagon-like peptide-1 receptor by exendin-4

    … through coupling to the glucagon like peptide-1 receptor (GLP-1R) with similar affinity and potency. Unlike N-terminally truncated GLP-1, (GLP-1(15-36)amide), the equivalently truncated EX4(9-39) binds GLP-1R without significant loss of affinity; furthermore, GLP-1(15-36) is a partial agonist …

    whiterose Repository record for The binding and activation of the glucagon-like peptide-1 receptor by exendin-4 (opens in a new tab)