Proteins > Receptor tyrosine-protein kinase erbB-3
Page last updated: 2024-08-07 23:22:07
Receptor tyrosine-protein kinase erbB-3
A receptor tyrosine-protein kinase erbB-3 that is encoded in the genome of human. [PRO:DNx, UniProtKB:P21860]
Synonyms
EC 2.7.10.1;
Proto-oncogene-like protein c-ErbB-3;
Tyrosine kinase-type cell surface receptor HER3
Research
Bioassay Publications (24)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (8.33) | 29.6817 |
| 2010's | 22 (91.67) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
Compounds (82)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Synthesis and biological evaluation of new [1,2,4]triazolo[4,3-a]pyridine derivatives as potential c-Met inhibitors.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor.European journal of medicinal chemistry, , Aug-08, Volume: 118, 2016
Toward discovery of mutant EGFR inhibitors; Design, synthesis and in vitro biological evaluation of potent 4-arylamino-6-ureido and thioureido-quinazoline derivatives.Bioorganic & medicinal chemistry, , 08-15, Volume: 24, Issue:16, 2016
Combination of 4-anilinoquinazoline, arylurea and tertiary amine moiety to discover novel anticancer agents.Bioorganic & medicinal chemistry, , Jan-15, Volume: 24, Issue:2, 2016
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.Journal of medicinal chemistry, , Oct-22, Volume: 58, Issue:20, 2015
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
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
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR MutantsJournal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 26, Issue:2, 2016
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Discovery of selective and noncovalent diaminopyrimidine-based inhibitors of epidermal growth factor receptor containing the T790M resistance mutation.Journal of medicinal chemistry, , Dec-11, Volume: 57, Issue:23, 2014
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.Bioorganic & medicinal chemistry, , Dec-15, Volume: 21, Issue:24, 2013
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Synthesis and biological evaluation of 4-anilinoquinolines as potent inhibitors of epidermal growth factor receptor.Journal of medicinal chemistry, , Apr-08, Volume: 53, Issue:7, 2010
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
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
Design, synthesis and biological evaluation of novel 4-anilinoquinazolines with C-6 urea-linked side chains as inhibitors of the epidermal growth factor receptor.Bioorganic & medicinal chemistry, , Dec-15, Volume: 21, Issue:24, 2013
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Comprehensive analysis of kinase inhibitor selectivity.Nature biotechnology, , Oct-30, Volume: 29, Issue:11, 2011
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.European journal of medicinal chemistry, , May-15, Volume: 170, 2019
Discovery of AZD8931, an Equipotent, Reversible Inhibitor of Signaling by EGFR, HER2, and HER3 Receptors.ACS medicinal chemistry letters, , Aug-08, Volume: 4, Issue:8, 2013
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
Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR MutantsJournal of medicinal chemistry, , 04-13, Volume: 60, Issue:7, 2017
Recent progress on third generation covalent EGFR inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Synthesis and evaluation of 2,9-disubstituted 8-phenylthio/phenylsulfinyl-9H-purine as new EGFR inhibitors.Bioorganic & medicinal chemistry, , 05-01, Volume: 26, Issue:8, 2018
Recent progress on third generation covalent EGFR inhibitors.Bioorganic & medicinal chemistry letters, , Apr-15, Volume: 26, Issue:8, 2016
Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.Journal of medicinal chemistry, , Mar-10, Volume: 59, Issue:5, 2016
Discovery of a potent and selective EGFR inhibitor (AZD9291) of both sensitizing and T790M resistance mutations that spares the wild type form of the receptor.Journal of medicinal chemistry, , Oct-23, Volume: 57, Issue:20, 2014
Enables
This protein enables 11 target(s):
| Target | Category | Definition |
|---|
| transmembrane signaling receptor activity | molecular function | Combining with an extracellular or intracellular signal and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity or state as part of signal transduction. [GOC:go_curators, Wikipedia:Transmembrane_receptor] |
| 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] |
| growth factor binding | molecular function | Binding to a growth factor, proteins or polypeptides that stimulate a cell or organism to grow or proliferate. [GOC:curators] |
| protein tyrosine kinase activator activity | molecular function | Increases the activity of a protein tyrosine kinase, an enzyme which phosphorylates a tyrosyl phenolic group on a protein. [GOC:ai, ISBN:0198506732] |
| ubiquitin protein ligase binding | molecular function | Binding to a ubiquitin protein ligase enzyme, any of the E3 proteins. [GOC:vp] |
| neuregulin binding | molecular function | Binding to a neuregulin, a member of the EGF family of growth factors. [GOC:bf, GOC:signaling] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| ErbB-3 class receptor binding | molecular function | Binding to the protein-tyrosine kinase receptor ErbB-3/HER3. [GOC:jl] |
| protein heterodimerization activity | molecular function | Binding to a nonidentical protein to form a heterodimer. [GOC:ai] |
| neuregulin receptor activity | molecular function | Combining with a neuregulin, a member of the EGF family of growth factors, and transmitting the signal from one side of the membrane to the other to initiate a change in cell activity. [GOC:bf, GOC:signaling, PMID:16460914, PMID:20672328] |
Located In
This protein is located in 5 target(s):
| Target | Category | Definition |
|---|
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
| 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] |
| basolateral plasma membrane | cellular component | The region of the plasma membrane that includes the basal end and sides of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
| apical plasma membrane | cellular component | The region of the plasma membrane located at the apical end of the cell. [GOC:curators] |
| lateral plasma membrane | cellular component | The portion of the plasma membrane at the lateral side of the cell. In epithelial cells, lateral plasma membranes are on the sides of cells which lie at the interface of adjacent cells. [GOC:hb, GOC:mah, GOC:pr] |
Active In
This protein is active in 2 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] |
| basal plasma membrane | cellular component | The region of the plasma membrane located at the basal end of the cell. Often used in reference to animal polarized epithelial membranes, where the basal membrane is the part attached to the extracellular matrix, or in plant cells, where the basal membrane is defined with respect to the zygotic axis. [GOC:go_curators] |
Part Of
This protein is part of 2 target(s):
| Target | Category | Definition |
|---|
| ERBB3:ERBB2 complex | cellular component | A heterodimeric complex between the tyrosine kinase receptor ERBB2 and a ligand-activated receptor ERBB3. ERBB2, which does not bind any known ligand, is activated through formation of a heterodimer with another ligand-activated ERBB family member such as ERBB3. [GOC:signaling, PMID:16460914, PMID:8665853, Reactome:R-HSA-1247502, Reactome:R-HSA-1963573, Reactome:R-HSA-1963589] |
| receptor complex | cellular component | Any protein complex that undergoes combination with a hormone, neurotransmitter, drug or intracellular messenger to initiate a change in cell function. [GOC:go_curators] |
Involved In
This protein is involved in 30 target(s):
| Target | Category | Definition |
|---|
| endocardial cushion development | biological process | The progression of a cardiac cushion over time, from its initial formation to the mature structure. The endocardial cushion is a specialized region of mesenchymal cells that will give rise to the heart septa and valves. [GOC:mtg_heart] |
| 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] |
| cell surface receptor protein tyrosine kinase signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor on the surface of the target cell where the receptor possesses tyrosine kinase activity, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:ceb, GOC:signaling] |
| peripheral nervous system development | biological process | The process whose specific outcome is the progression of the peripheral nervous system over time, from its formation to the mature structure. The peripheral nervous system is one of the two major divisions of the nervous system. Nerves in the PNS connect the central nervous system (CNS) with sensory organs, other organs, muscles, blood vessels and glands. [GOC:go_curators, UBERON:0000010] |
| 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] |
| negative regulation of signal transduction | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of signal transduction. [GOC:sm] |
| positive regulation of gene expression | biological process | Any process that increases 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] |
| Schwann cell differentiation | biological process | The process in which a relatively unspecialized cell acquires the specialized features of a Schwann cell. Schwann cells are found in the peripheral nervous system, where they insulate neurons and axons, and regulate the environment in which neurons function. [GOC:ef] |
| Schwann cell development | biological process | The process aimed at the progression of a Schwann cell over time, from initial commitment of the cell to a specific fate, to the fully functional differentiated cell. Schwann cells are found in the peripheral nervous system, where they insulate neurons and axons, and regulate the environment in which neurons function. [GOC:dgh, GOC:ef] |
| cranial nerve development | biological process | The process whose specific outcome is the progression of the cranial nerves over time, from its formation to the mature structure. The cranial nerves are composed of twelve pairs of nerves that emanate from the nervous tissue of the hindbrain. These nerves are sensory, motor, or mixed in nature, and provide the motor and general sensory innervation of the head, neck and viscera. They mediate vision, hearing, olfaction and taste and carry the parasympathetic innervation of the autonomic ganglia that control visceral functions. [GO_REF:0000021, GOC:cls, GOC:dgh, GOC:dph, GOC:jid, ISBN:0838580343] |
| ERBB2-ERBB3 signaling pathway | biological process | The series of molecular signals initiated by binding of a ligand to a ERBB3 receptor on the surface of a cell, followed by transmission of the signal by a heterodimeric complex of ERBB2 and ERBB3. ERBB2, which does not bind any known ligand, is activated through formation of a heterodimer with another ligand-activated ERBB family member such as ERBB3. ERBB3 also has impaired kinase activity and relies on ERBB2 for activation and signal transmission. [GOC:signaling, PMID:16460914, Reactome:R-HSA-1963589] |
| wound healing | biological process | The series of events that restore integrity to a damaged tissue, following an injury. [GOC:bf, PMID:15269788] |
| regulation of cell population proliferation | biological process | Any process that modulates the frequency, rate or extent of cell proliferation. [GOC:jl] |
| myelination | biological process | The process in which myelin sheaths are formed and maintained around neurons. Oligodendrocytes in the brain and spinal cord and Schwann cells in the peripheral nervous system wrap axons with compact layers of their plasma membrane. Adjacent myelin segments are separated by a non-myelinated stretch of axon called a node of Ranvier. [GOC:dgh, GOC:mah] |
| phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | An intracellular signaling cassette that starts with phosphatidylinositol 3-kinase (PI3K) activation, production of phosphatidylinositol 3-phosphate (PI3P), activation of PDK1, which recruits and ending with the activation of protein kinase B (PKB, also known as Akt). PI3K is activated by cell surface receptors. Note that PTEN is an inhibitor of the pathway. [PMID:20517722, PMID:22952397] |
| negative regulation of neuron apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process in neurons. [GOC:go_curators, GOC:mtg_apoptosis] |
| negative regulation of secretion | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of the controlled release of a substance from a cell or a tissue. [GOC:ai] |
| neuron apoptotic process | biological process | Any apoptotic process in a neuron, the basic cellular unit of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the nervous system. [CL:0000540, GOC:mtg_apoptosis] |
| positive regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction | biological process | Any process that activates or increases the frequency, rate or extent of phosphatidylinositol 3-kinase/protein kinase B signal transduction. [GOC:ai] |
| positive regulation of cardiac muscle tissue development | biological process | Any process that activates, maintains or increases the frequency, rate or extent of cardiac muscle tissue development. [GOC:vk] |
| positive regulation of calcineurin-NFAT signaling cascade | biological process | Any process that activates or increases the frequency, rate or extent of signaling via the calcineurin-NFAT signaling cascade. [GOC:mah] |
| motor neuron apoptotic process | biological process | Any apoptotic process in a motor neuron, an efferent neuron that passes from the central nervous system or a ganglion toward or to a muscle and conducts an impulse that causes movement. [CL:0000100, GOC:BHF, GOC:mtg_apoptosis, PMID:14523086] |
| extrinsic apoptotic signaling pathway in absence of ligand | biological process | The series of molecular signals in which a signal is conveyed from the cell surface to trigger the apoptotic death of a cell. The pathway starts with withdrawal of a ligand from a cell surface receptor, and ends when the execution phase of apoptosis is triggered. [GOC:mtg_apoptosis, PMID:15044679, PMID:20816705] |
| negative regulation of motor neuron apoptotic process | biological process | Any process that stops, prevents or reduces the frequency, rate or extent of motor neuron apoptotic process. [GOC:mtg_apoptosis, GOC:obol] |
| negative regulation of apoptotic process | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cell death by apoptotic process. [GOC:jl, GOC:mtg_apoptosis] |
| neurogenesis | biological process | Generation of cells within the nervous system. [GO_REF:0000021, GOC:cls, GOC:curators, GOC:dgh, GOC:dph, GOC:jid] |
| positive regulation of cell population proliferation | biological process | Any process that activates or increases the rate or extent of cell proliferation. [GOC:go_curators] |
| positive regulation of kinase activity | biological process | Any process that activates or increases the frequency, rate or extent of kinase activity, the catalysis of the transfer of a phosphate group, usually from ATP, to a substrate molecule. [GOC:mah] |
| multicellular organism development | biological process | The biological process whose specific outcome is the progression of a multicellular organism over time from an initial condition (e.g. a zygote or a young adult) to a later condition (e.g. a multicellular animal or an aged adult). [GOC:dph, GOC:ems, GOC:isa_complete, GOC:tb] |