Publications by authors named "Lap H Tse"
Article Synopsis
- Activin receptor-like kinases 1-7 (ALK1-7) play a crucial role in regulating both SMAD-dependent and SMAD-independent signaling pathways, particularly in bone morphogenetic protein (BMP) signaling.
- Current inhibitors for studying these pathways lack sufficient selectivity, making it difficult to validate cellular targets effectively.
- The study identifies two new selective inhibitors of ALK1 and ALK2 that block the BMP pathway effectively in cells and demonstrate good in vivo profiles, with one showing high penetration into the brain, providing valuable tools for research in BMP signaling.
Article Synopsis
- Melatonin is a hormone that regulates circadian rhythms and acts on two types of receptors (MT and MT) to influence cAMP levels in cells.
- Recent research using a luminescent biosensor showed that activating the MT receptor enhances cAMP production, while both receptors generally inhibit cAMP synthesis when stimulated by certain pathways.
- The study suggests a complex interaction between MT and G proteins, allowing for varied regulation of cAMP levels depending on the receptor types and combinations present in the cells.
Melatonin receptors are Class A G protein-coupled receptors (GPCRs) that regulate a plethora of physiological activities in response to the rhythmic secretion of melatonin from the pineal gland. Melatonin is a key regulator in the control of circadian rhythm and has multiple functional roles in retinal physiology, memory, immunomodulation and tumorigenesis. The two subtypes of human melatonin receptors, termed MT and MT, utilize overlapping signaling pathways although biased signaling properties have been reported in some cellular systems.
View Article and Find Full Text PDFMelatonin MT and MT receptors represent attractive drug targets for the treatment of various disorders. However, the high conservation of the melatonin binding pocket has hindered the development of subtype-selective compounds. By leveraging on the recently resolved crystal structures of MT and MT receptors, this study aims to elucidate the structural basis of MT-selectivity of a panel of isoquinolinone derivatives.
View Article and Find Full Text PDFG protein-coupled receptors (GPCRs) constitute the largest superfamily of integral membrane protein receptors. As signal detectors, the several 100 known GPCRs are responsible for sensing the plethora of endogenous ligands that are critical for the functioning of our endocrine system. Although GPCRs are typically considered as detectors for first messengers in classical signal transduction pathways, they seldom operate in isolation in complex biological systems.
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