Proteins > Serine/threonine-protein kinase receptor R3
Page last updated: 2024-08-07 23:27:43
Serine/threonine-protein kinase receptor R3
A serine/threonine-protein kinase receptor R3 that is encoded in the genome of human. [PRO:CNA, UniProtKB:P37023]
Synonyms
SKR3;
EC 2.7.11.30;
Activin receptor-like kinase 1;
ALK-1;
TGF-B superfamily receptor type I;
TSR-I
Research
Bioassay Publications (9)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (22.22) | 29.6817 |
| 2010's | 6 (66.67) | 24.3611 |
| 2020's | 1 (11.11) | 2.80 |
Compounds (105)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML).Blood, , Oct-01, Volume: 114, Issue:14, 2009
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
ASR352, A potent anticancer agent: Synthesis, preliminary SAR, and biological activities against colorectal cancer bulk, 5-fluorouracil/oxaliplatin resistant and stem cells.European journal of medicinal chemistry, , Jan-01, Volume: 161, 2019
Identification of the First Selective Activin Receptor-Like Kinase 1 Inhibitor, a Reversible Version of L-783277.Journal of medicinal chemistry, , 02-23, Volume: 60, Issue:4, 2017
Synthesis and structure-activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo[1.5-a]pyrimidine scaffold of dorsomorphin: the discovery of ML347 as an ALK2 versus ALK3 selective MLPCN Bioorganic & medicinal chemistry letters, , Jun-01, Volume: 23, Issue:11, 2013
Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-β type I receptor kinase as cancer immunotherapeutic/Journal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
The target landscape of clinical kinase drugs.Science (New York, N.Y.), , 12-01, Volume: 358, Issue:6367, 2017
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
A quantitative analysis of kinase inhibitor selectivity.Nature biotechnology, , Volume: 26, Issue:1, 2008
Enables
This protein enables 13 target(s):
| Target | Category | Definition |
|---|
| protein serine/threonine kinase activity | molecular function | Catalysis of the reactions: ATP + protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:bf, MetaCyc:PROTEIN-KINASE-RXN, PMID:2956925] |
| transmembrane receptor protein serine/threonine kinase activity | molecular function | Combining with a signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity by catalysis of the reaction: ATP protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [EC:2.7.11.30] |
| transforming growth factor beta receptor activity | molecular function | Combining with a transforming growth factor beta (TGFbeta) and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity by catalysis of the reaction: ATP protein serine = ADP + protein serine phosphate, and ATP + protein threonine = ADP + protein threonine phosphate. [GOC:mah, GOC:signaling] |
| transforming growth factor beta receptor activity, type I | molecular function | Combining with a complex of transforming growth factor beta and a type II TGF-beta receptor to initiate a change in cell activity; upon binding, acts as a downstream transducer of TGF-beta signals. [GOC:mah, Reactome:R-HSA-170846] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| ATP binding | molecular function | Binding to ATP, adenosine 5'-triphosphate, a universally important coenzyme and enzyme regulator. [ISBN:0198506732] |
| activin receptor activity, type I | molecular function | Combining with activin-bound type II activin receptor to initiate a change in cell activity; upon binding, acts as a downstream transducer of activin signals. [GOC:mah, PMID:8622651] |
| protein kinase binding | molecular function | Binding to a protein kinase, any enzyme that catalyzes the transfer of a phosphate group, usually from ATP, to a protein substrate. [GOC:jl] |
| SMAD binding | molecular function | Binding to a SMAD signaling protein. [GOC:ai] |
| metal ion binding | molecular function | Binding to a metal ion. [GOC:ai] |
| activin binding | molecular function | Binding to activin, a dimer of inhibin-beta subunits. [GOC:jid, GOC:mah] |
| transforming growth factor beta binding | molecular function | Binding to TGF-beta, transforming growth factor beta, a multifunctional peptide that controls proliferation, differentiation and other functions in many cell types. [ISBN:0198506732] |
| BMP receptor activity | molecular function | Combining with a member of the bone morphogenetic protein (BMP) family, and transmitting a signal across the plasma membrane to initiate a change in cell activity. [GOC:BHF, GOC:dos] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| cell surface | cellular component | The external part of the cell wall and/or plasma membrane. [GOC:jl, GOC:mtg_sensu, GOC:sm] |
| dendrite | cellular component | A neuron projection that has a short, tapering, morphology. Dendrites receive and integrate signals from other neurons or from sensory stimuli, and conduct nerve impulses towards the axon or the cell body. In most neurons, the impulse is conveyed from dendrites to axon via the cell body, but in some types of unipolar neuron, the impulse does not travel via the cell body. [GOC:aruk, GOC:bc, GOC:dos, GOC:mah, GOC:nln, ISBN:0198506732] |
| neuronal cell body | cellular component | The portion of a neuron that includes the nucleus, but excludes cell projections such as axons and dendrites. [GOC:go_curators] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Part Of
This protein is part of 1 target(s):
| Target | Category | Definition |
|---|
| BMP receptor complex | cellular component | A protein complex that acts as a receptor for bone morphogenetic proteins (BMPs); a homo- or heterodimer of type I and/or type II BMP receptor subunits. [GOC:mah, GOC:mh, PMID:19377468] |
Involved In
This protein is involved in 50 target(s):
| Target | Category | Definition |
|---|
| angiogenesis | biological process | Blood vessel formation when new vessels emerge from the proliferation of pre-existing blood vessels. [ISBN:0878932453] |
| response to hypoxia | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:hjd] |
| in utero embryonic development | biological process | The process whose specific outcome is the progression of the embryo in the uterus over time, from formation of the zygote in the oviduct, to birth. An example of this process is found in Mus musculus. [GOC:go_curators, GOC:mtg_sensu] |
| regulation of endothelial cell proliferation | biological process | Any process that modulates the frequency, rate, or extent of endothelial cell proliferation. [GOC:add] |
| negative regulation of endothelial cell proliferation | biological process | Any process that stops, prevents, or reduces the rate or extent of endothelial cell proliferation. [GOC:add] |
| positive regulation of endothelial cell proliferation | biological process | Any process that activates or increases the rate or extent of endothelial cell proliferation. [GOC:add] |
| lymphangiogenesis | biological process | Lymph vessel formation when new vessels emerge from the proliferation of pre-existing vessels. [GOC:dph, PMID:11596157] |
| blood vessel maturation | biological process | A developmental process, independent of morphogenetic (shape) change, that is required for a blood vessel to attain its fully functional state. [GOC:dph] |
| blood vessel remodeling | biological process | The reorganization or renovation of existing blood vessels. [GOC:hjd] |
| blood vessel endothelial cell proliferation involved in sprouting angiogenesis | biological process | The multiplication or reproduction of blood vessel endothelial cells, resulting in the expansion of a cell population contributing to sprouting angiogenesis. [GOC:dph, GOC:tb, PMID:16391003] |
| endocardial cushion morphogenesis | biological process | The process in which the anatomical structure of the endocardial cushion is generated and organized. The endocardial cushion is a specialized region of mesenchymal cells that will give rise to the heart septa and valves. [GOC:mtg_heart] |
| regulation of DNA replication | biological process | Any process that modulates the frequency, rate or extent of DNA replication. [GOC:go_curators] |
| regulation of DNA-templated transcription | biological process | Any process that modulates the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| negative regulation of cell adhesion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell adhesion. [GOC:go_curators] |
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| transforming growth factor beta receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a transforming growth factor beta receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:BHF, GOC:mah, GOC:signaling] |
| blood circulation | biological process | The flow of blood through the body of an animal, enabling the transport of nutrients to the tissues and the removal of waste products. [GOC:mtg_heart, ISBN:0192800825] |
| regulation of blood pressure | biological process | Any process that modulates the force with which blood travels through the circulatory system. The process is controlled by a balance of processes that increase pressure and decrease pressure. [GOC:dph, GOC:mtg_cardio, ISBN:0721643949] |
| negative regulation of cell population proliferation | biological process | Any process that stops, prevents or reduces the rate or extent of cell proliferation. [GOC:go_curators] |
| negative regulation of endothelial cell migration | biological process | Any process that decreases the rate, frequency, or extent of the orderly movement of an endothelial cell into the extracellular matrix to form an endothelium. [GOC:BHF, GOC:dph, GOC:tb] |
| negative regulation of gene expression | biological process | Any process that decreases the frequency, rate or extent of gene expression. Gene expression is the process in which a gene's coding sequence is converted into a mature gene product (protein or RNA). [GOC:txnOH-2018] |
| negative regulation of cell growth | biological process | Any process that stops, prevents, or reduces the frequency, rate, extent or direction of cell growth. [GOC:go_curators] |
| negative regulation of cell migration | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell migration. [GOC:go_curators] |
| BMP signaling pathway | biological process | The series of molecular signals initiated by the binding of a member of the BMP (bone morphogenetic protein) family to a receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:signaling, ISBN:0878932437, PMID:17428827] |
| positive regulation of BMP signaling pathway | biological process | Any process that activates or increases the frequency, rate or extent of BMP signaling pathway activity. [GOC:go_curators] |
| positive regulation of chondrocyte differentiation | biological process | Any process that activates or increases the frequency, rate or extent of chondrocyte differentiation. [GOC:mah] |
| activin receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to an activin receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:rl, GOC:signaling] |
| wound healing, spreading of epidermal cells | biological process | The migration of an epidermal cell along or through a wound gap that contributes to the reestablishment of a continuous epidermis. [GOC:bf, PMID:15269788] |
| dorsal aorta morphogenesis | biological process | The process in which the anatomical structures of the dorsal aorta are generated and organized. The dorsal aorta is a blood vessel in a single-pass circulatory system that carries oxygenated blood from the gills to the rest of the body. In a single-pass circulatory system blood passes once through the heart to supply the body once. [GOC:bf, GOC:dgh, UBERON:0005805, Wikipedia:Aorta, ZFA:0000014] |
| regulation of blood vessel endothelial cell migration | biological process | Any process that modulates the frequency, rate or extent of the migration of the endothelial cells of blood vessels. [GOC:go_curators] |
| negative regulation of blood vessel endothelial cell migration | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the migration of the endothelial cells of blood vessels. [GOC:go_curators] |
| negative regulation of endothelial cell differentiation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of endothelial cell differentiation. [GOC:go_curators] |
| positive regulation of endothelial cell differentiation | biological process | Any process that activates or increases the frequency, rate or extent of endothelial cell differentiation. [GOC:go_curators] |
| positive regulation of angiogenesis | biological process | Any process that activates or increases angiogenesis. [GOC:go_curators] |
| positive regulation of DNA-templated transcription | biological process | Any process that activates or increases the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
| positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
| negative regulation of focal adhesion assembly | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of focal adhesion assembly, the establishment and maturation of focal adhesions. [GOC:ai] |
| positive regulation of SMAD protein signal transduction | biological process | Any process that increases the rate, frequency or extent of SMAD protein signal transduction. [GOC:BHF, GOC:dph, GOC:tb] |
| lymphatic endothelial cell differentiation | biological process | The process in which a venous blood vessel endothelial cell acquires specialized features of a lymphatic vessel endothelial cell, a thin flattened cell that lines the inside surfaces of lymph vessels. [GOC:dph, GOC:sdb_2009, GOC:tb] |
| artery development | biological process | The progression of the artery over time, from its initial formation to the mature structure. An artery is a blood vessel that carries blood away from the heart to a capillary bed. [GOC:dph, GOC:sdb_2009, GOC:tb] |
| venous blood vessel development | biological process | The progression of the venous blood vessel over time from its initial formation to the mature structure. Venous blood vessels carry blood back to the heart after the capillary bed. [GOC:dph, GOC:sdb_2009, GOC:tb] |
| endothelial tube morphogenesis | biological process | The process in which the anatomical structures of a tube are generated and organized from an endothelium. Endothelium refers to the layer of cells lining blood vessels, lymphatics, the heart, and serous cavities, and is derived from bone marrow or mesoderm. Corneal endothelium is a special case, derived from neural crest cells. [GOC:dph, GOC:yaf] |
| retina vasculature development in camera-type eye | biological process | The process whose specific outcome is the progression of the vasculature of the retina over time, from its formation to the mature structure. [GOC:BHF, GOC:dph] |
| cellular response to transforming growth factor beta stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a transforming growth factor beta stimulus. [GOC:ecd, PMID:15451575] |
| cellular response to BMP stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a bone morphogenetic protein (BMP) stimulus. [GOC:mah, GOC:yaf] |
| positive regulation of bicellular tight junction assembly | biological process | Any process that activates or increases the frequency, rate or extent of tight junction assembly. [GO_REF:0000058, GOC:jz, GOC:TermGenie, PMID:25050009] |
| protein phosphorylation | biological process | The process of introducing a phosphate group on to a protein. [GOC:hb] |
| dorsal/ventral pattern formation | biological process | The regionalization process in which the areas along the dorsal/ventral axis are established that will lead to differences in cell differentiation. The dorsal/ventral axis is defined by a line that runs orthogonal to both the anterior/posterior and left/right axes. The dorsal end is defined by the upper or back side of an organism. The ventral end is defined by the lower or front side of an organism. [GOC:dph, GOC:go_curators, GOC:isa_complete, GOC:tb] |
| heart development | biological process | The process whose specific outcome is the progression of the heart over time, from its formation to the mature structure. The heart is a hollow, muscular organ, which, by contracting rhythmically, keeps up the circulation of the blood. [GOC:jid, UBERON:0000948] |
| cellular response to growth factor stimulus | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a growth factor stimulus. [GOC:mah] |