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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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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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The SH2 (Src Homology 2) domains play key roles in different kinase-mediated intracellular signal transduction pathways and many human diseases are associated with their dysregulation [1-3].
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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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Epigenetic targets are a major new category for successful drug research. Among them the protein methyltransferases (PMTs) which have crucial roles in gene transcription are an important group of enzymes that play key parts in normal physiology and human diseases. There has been a significant increase in attention towards protein arginine methyltransferases (PRMTs) which catalyze methylation of nitrogen of specific arginine residues in proteins and impact on numerous essential biological pathways by methylating different nuclear, cytoplasmic and membrane protein substrates.
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