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- PDB-8e1x: FGFR2 kinase domain in complex with a Pyrazolo[1,5-a]pyrimidine a... -
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Basic information
Entry | Database: PDB / ID: 8e1x | ||||||
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Title | FGFR2 kinase domain in complex with a Pyrazolo[1,5-a]pyrimidine analog (Compound 29) | ||||||
![]() | Fibroblast growth factor receptor 2 | ||||||
![]() | STRUCTURAL PROTEIN / FGFR / inhibitor / kinase / gatekeeper / hyperphosphatemia | ||||||
Function / homology | ![]() Signaling by FGFR2 amplification mutants / Signaling by FGFR2 fusions / fibroblast growth factor receptor signaling pathway involved in negative regulation of apoptotic process in bone marrow cell / fibroblast growth factor receptor signaling pathway involved in hemopoiesis / fibroblast growth factor receptor signaling pathway involved in positive regulation of cell proliferation in bone marrow / fibroblast growth factor receptor signaling pathway involved in mammary gland specification / lateral sprouting from an epithelium / mammary gland bud formation / branch elongation involved in salivary gland morphogenesis / mesenchymal cell differentiation involved in lung development ...Signaling by FGFR2 amplification mutants / Signaling by FGFR2 fusions / fibroblast growth factor receptor signaling pathway involved in negative regulation of apoptotic process in bone marrow cell / fibroblast growth factor receptor signaling pathway involved in hemopoiesis / fibroblast growth factor receptor signaling pathway involved in positive regulation of cell proliferation in bone marrow / fibroblast growth factor receptor signaling pathway involved in mammary gland specification / lateral sprouting from an epithelium / mammary gland bud formation / branch elongation involved in salivary gland morphogenesis / mesenchymal cell differentiation involved in lung development / lacrimal gland development / otic vesicle formation / prostate gland morphogenesis / regulation of smooth muscle cell differentiation / regulation of morphogenesis of a branching structure / orbitofrontal cortex development / squamous basal epithelial stem cell differentiation involved in prostate gland acinus development / embryonic organ morphogenesis / branching morphogenesis of a nerve / endochondral bone growth / morphogenesis of embryonic epithelium / epidermis morphogenesis / bud elongation involved in lung branching / positive regulation of epithelial cell proliferation involved in lung morphogenesis / pyramidal neuron development / membranous septum morphogenesis / reproductive structure development / limb bud formation / lung lobe morphogenesis / gland morphogenesis / fibroblast growth factor receptor signaling pathway involved in orbitofrontal cortex development / ventricular zone neuroblast division / embryonic digestive tract morphogenesis / epithelial cell proliferation involved in salivary gland morphogenesis / mesenchymal cell differentiation / branching involved in prostate gland morphogenesis / mesenchymal cell proliferation involved in lung development / branching involved in labyrinthine layer morphogenesis / FGFR2b ligand binding and activation / FGFR2c ligand binding and activation / Activated point mutants of FGFR2 / regulation of osteoblast proliferation / Phospholipase C-mediated cascade; FGFR2 / fibroblast growth factor receptor activity / embryonic pattern specification / branching involved in salivary gland morphogenesis / outflow tract septum morphogenesis / positive regulation of phospholipase activity / lung-associated mesenchyme development / mesodermal cell differentiation / regulation of smoothened signaling pathway / embryonic cranial skeleton morphogenesis / digestive tract development / bone morphogenesis / skeletal system morphogenesis / odontogenesis / positive regulation of mesenchymal cell proliferation / ventricular cardiac muscle tissue morphogenesis / ureteric bud development / regulation of osteoblast differentiation / Signaling by FGFR2 IIIa TM / inner ear morphogenesis / midbrain development / organ growth / hair follicle morphogenesis / lung alveolus development / prostate epithelial cord arborization involved in prostate glandular acinus morphogenesis / PI-3K cascade:FGFR2 / bone mineralization / fibroblast growth factor binding / prostate epithelial cord elongation / positive regulation of cell division / excitatory synapse / positive regulation of Wnt signaling pathway / PI3K Cascade / negative regulation of keratinocyte proliferation / epithelial to mesenchymal transition / fibroblast growth factor receptor signaling pathway / cell fate commitment / embryonic organ development / SHC-mediated cascade:FGFR2 / positive regulation of cell cycle / cellular response to retinoic acid / positive regulation of cardiac muscle cell proliferation / FRS-mediated FGFR2 signaling / cellular response to transforming growth factor beta stimulus / positive regulation of vascular associated smooth muscle cell proliferation / Signaling by FGFR2 in disease / epithelial cell differentiation / regulation of ERK1 and ERK2 cascade / axonogenesis / post-embryonic development / positive regulation of epithelial cell proliferation / animal organ morphogenesis / Negative regulation of FGFR2 signaling / lung development / bone development / receptor protein-tyrosine kinase / peptidyl-tyrosine phosphorylation / Constitutive Signaling by Aberrant PI3K in Cancer Similarity search - Function | ||||||
Biological species | ![]() | ||||||
Method | ![]() ![]() ![]() | ||||||
![]() | Lei, H.-T. / Epling, L.B. / Deller, M.C. | ||||||
Funding support | ![]()
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![]() | ![]() Title: Discovery of Potent and Selective Inhibitors of Wild-Type and Gatekeeper Mutant Fibroblast Growth Factor Receptor (FGFR) 2/3. Authors: Shvartsbart, A. / Roach, J.J. / Witten, M.R. / Koblish, H. / Harris, J.J. / Covington, M. / Hess, R. / Lin, L. / Frascella, M. / Truong, L. / Leffet, L. / Conlen, P. / Beshad, E. / Klabe, R. ...Authors: Shvartsbart, A. / Roach, J.J. / Witten, M.R. / Koblish, H. / Harris, J.J. / Covington, M. / Hess, R. / Lin, L. / Frascella, M. / Truong, L. / Leffet, L. / Conlen, P. / Beshad, E. / Klabe, R. / Katiyar, K. / Kaldon, L. / Young-Sciame, R. / He, X. / Petusky, S. / Chen, K.J. / Horsey, A. / Lei, H.T. / Epling, L.B. / Deller, M.C. / Vechorkin, O. / Yao, W. | ||||||
History |
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Structure viewer | Molecule: ![]() ![]() |
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PDBx/mmCIF format | ![]() | 286.7 KB | Display | ![]() |
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PDB format | ![]() | 191.7 KB | Display | ![]() |
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-Validation report
Arichive directory | ![]() ![]() | HTTPS FTP |
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-Related structure data
Related structure data | ![]() 4qqtS S: Starting model for refinement |
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Similar structure data | Similarity search - Function & homology ![]() |
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Assembly
Deposited unit | ![]()
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Noncrystallographic symmetry (NCS) | NCS domain:
NCS domain segments: Ens-ID: 1
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