Beta-arrestins (ß-arrestin 1 and ß-arrestin 2) play central roles in the mechanisms regulating G protein-coupled receptors signalling and trafficking. They participate in agonist-mediated desensitization of GPCR and cause specific dampening of cellular responses to stimuli such as sensory signals, hormones or neurotransmitters [1].
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Transporters are proteins that span the plasma membrane and regulate the traffic of small molecules in and out of the cell. They play a particularly important role in chemical signalling between neurons in the CNS, where they act to control the concentration of neurotransmitters in the synapse. Another key role for transporters is in excluding undesirable xenobiotics from the cell, whilst allowing key molecules required for the cell life cycle to enter. The majority of transporters are targets for drug discovery.
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Caspase 2 (CASP2, CASP-2, ICH1, NEDD-2, NEDD2, PPP1R57) is an initiator caspase for cellular apoptosis. It is also involved in several other vital processes including oxidative stress responses, regulation of cell cycle checkpoints, autophagy and senescence. Disorders of CASP2 activity are observed at obesity, metabolic syndrome, nonalcoholic fatty liver disease and cancer [1, 2]. Therefore, small molecule compounds modulating CASP2 activity may have significant therapeutic potential.
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Nuclear estrogen receptors (ERα and Erβ) are members of the nuclear receptor family of intracellular receptors. Estrogen receptors (ERs) are involved in modulation of biological activities, such as reproductive organ development, bone modeling, cardiovascular system functioning, metabolism and behavior in both females and males.
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Estrogen-related receptor gamma (ERRγ) is involved in energy metabolism, mitochondrial functions, biogenesis and tissue repair. Disorders of ERRγ are observed at type 2 diabetes, hypoxia, metabolic syndrome and cancer. Therefore, small molecule compounds modulating ERRγ activity may have significant therapeutic potential.
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