Details of the Target

General Information of Target

Target ID LDTP02361
Target Name Platelet-derived growth factor receptor beta (PDGFRB)
Gene Name PDGFRB
Gene ID 5159
Synonyms
PDGFR; PDGFR1; Platelet-derived growth factor receptor beta; PDGF-R-beta; PDGFR-beta; EC 2.7.10.1; Beta platelet-derived growth factor receptor; Beta-type platelet-derived growth factor receptor; CD140 antigen-like family member B; Platelet-derived growth factor receptor 1; PDGFR-1; CD antigen CD140b
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTFVLTCSGSAPV
VWERMSQEPPQEMAKAQDGTFSSVLTLTNLTGLDTGEYFCTHNDSRGLETDERKRLYIFV
PDPTVGFLPNDAEELFIFLTEITEITIPCRVTDPQLVVTLHEKKGDVALPVPYDHQRGFS
GIFEDRSYICKTTIGDREVDSDAYYVYRLQVSSINVSVNAVQTVVRQGENITLMCIVIGN
EVVNFEWTYPRKESGRLVEPVTDFLLDMPYHIRSILHIPSAELEDSGTYTCNVTESVNDH
QDEKAINITVVESGYVRLLGEVGTLQFAELHRSRTLQVVFEAYPPPTVLWFKDNRTLGDS
SAGEIALSTRNVSETRYVSELTLVRVKVAEAGHYTMRAFHEDAEVQLSFQLQINVPVRVL
ELSESHPDSGEQTVRCRGRGMPQPNIIWSACRDLKRCPRELPPTLLGNSSEEESQLETNV
TYWEEEQEFEVVSTLRLQHVDRPLSVRCTLRNAVGQDTQEVIVVPHSLPFKVVVISAILA
LVVLTIISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPMQLPYDSTWELPRDQL
VLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGP
HLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQHHSDKRRPPSAELYSNAL
PVGLPLPSHVSLTGESDGGYMDMSKDESVDYVPMLDMKGDVKYADIESSNYMAPYDNYVP
SAPERTCRATLINESPVLSYMDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLV
KICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLG
GTPYPELPMNEQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFEIRPPFSQLVLLLER
LLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGFHGLRSPLDTSSVLYTAVQPNEGDND
YIIPLPDPKPEVADEGPLEGSPSLASSTLNEVNTSSTISCDSPLEPQDEPEPEPQLELQV
EPEPELEQLPDSGCPAPRAEAEDSFL
Target Type
Successful
Target Bioclass
Enzyme
Family
Protein kinase superfamily, Tyr protein kinase family, CSF-1/PDGF receptor subfamily
Subcellular location
Cell membrane
Function
Tyrosine-protein kinase that acts as a cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic development, cell proliferation, survival, differentiation, chemotaxis and migration. Plays an essential role in blood vessel development by promoting proliferation, migration and recruitment of pericytes and smooth muscle cells to endothelial cells. Plays a role in the migration of vascular smooth muscle cells and the formation of neointima at vascular injury sites. Required for normal development of the cardiovascular system. Required for normal recruitment of pericytes (mesangial cells) in the kidney glomerulus, and for normal formation of a branched network of capillaries in kidney glomeruli. Promotes rearrangement of the actin cytoskeleton and the formation of membrane ruffles. Binding of its cognate ligands - homodimeric PDGFB, heterodimers formed by PDGFA and PDGFB or homodimeric PDGFD -leads to the activation of several signaling cascades; the response depends on the nature of the bound ligand and is modulated by the formation of heterodimers between PDGFRA and PDGFRB. Phosphorylates PLCG1, PIK3R1, PTPN11, RASA1/GAP, CBL, SHC1 and NCK1. Activation of PLCG1 leads to the production of the cellular signaling molecules diacylglycerol and inositol 1,4,5-trisphosphate, mobilization of cytosolic Ca(2+) and the activation of protein kinase C. Phosphorylation of PIK3R1, the regulatory subunit of phosphatidylinositol 3-kinase, leads to the activation of the AKT1 signaling pathway. Phosphorylation of SHC1, or of the C-terminus of PTPN11, creates a binding site for GRB2, resulting in the activation of HRAS, RAF1 and down-stream MAP kinases, including MAPK1/ERK2 and/or MAPK3/ERK1. Promotes phosphorylation and activation of SRC family kinases. Promotes phosphorylation of PDCD6IP/ALIX and STAM. Receptor signaling is down-regulated by protein phosphatases that dephosphorylate the receptor and its down-stream effectors, and by rapid internalization of the activated receptor.
TTD ID
T59102
Uniprot ID
P09619
DrugMap ID
TT317EC
Ensemble ID
ENST00000261799.9
HGNC ID
HGNC:8804
ChEMBL ID
CHEMBL1913

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
8505C SNV: p.V221M .
ETK1 SNV: p.G1093W .
HCC1395 SNV: p.T882I .
HCC1806 SNV: p.A916V .
HT115 SNV: p.A203V .
Ishikawa (Heraklio) 02 ER SNV: p.D166G .
KMCH1 SNV: p.N777S DBIA    Probe Info 
LOXIMVI Substitution: p.R439Q .
MDAMB157 SNV: p.T1057P .
MELJUSO SNV: p.P774L DBIA    Probe Info 
MEWO SNV: p.P1001S
Substitution: p.P1001L		 .
MFE319 SNV: p.Q155Ter; p.G320R .
NCIH1793 SNV: p.T369R .
NCIH2286 SNV: p.G181V; p.L883M .
OZ SNV: p.V51F .
SNU1196 SNV: p.T36P .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C835(1.60)  LDD3351  [1]
IA-alkyne
 Probe Info  		C843(0.80)  LDD2207  [2]
Acrolein
 Probe Info  		N.A.  LDD0222  [3]
IPM
 Probe Info  		N.A.  LDD0147  [4]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [3]
Methacrolein
 Probe Info  		N.A.  LDD0218  [3]
NAIA_5
 Probe Info  		N.A.  LDD2223  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [3]
 LDCM0022  KB02 42-MG-BA C835(3.52)  LDD2244  [1]
 LDCM0023  KB03 42-MG-BA C835(5.39)  LDD2661  [1]
 LDCM0024  KB05 NCI-H196 C835(1.60)  LDD3351  [1]
 LDCM0628  OTUB2-COV-1 HEK-293T C843(0.80)  LDD2207  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Vascular endothelial growth factor receptor 2 (KDR) Tyr protein kinase family P35968
Tyrosine-protein kinase Fyn (FYN) Tyr protein kinase family P06241
Tyrosine-protein phosphatase non-receptor type 1 (PTPN1) Protein-tyrosine phosphatase family P18031
Tyrosine-protein phosphatase non-receptor type 11 (PTPN11) Protein-tyrosine phosphatase family Q06124
Tyrosine-protein phosphatase non-receptor type 12 (PTPN12) Protein-tyrosine phosphatase family Q05209
Receptor-type tyrosine-protein phosphatase eta (PTPRJ) Protein-tyrosine phosphatase family Q12913
Phosphatidylinositol 3,4,5-trisphosphate 3-phosphatase and dual-specificity protein phosphatase PTEN (PTEN) PTEN phosphatase protein family P60484
1-phosphatidylinositol 4,5-bisphosphate phosphodiesterase gamma-1 (PLCG1) . P19174
Transporter and channel
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Amyloid-beta precursor protein (APP) APP family P05067
Na(+)/H(+) exchange regulatory cofactor NHE-RF1 (NHERF1) . O14745
Immunoglobulin
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Leucine-rich repeats and immunoglobulin-like domains protein 2 (LRIG2) . O94898
Cytokine and receptor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Interleukin-1 receptor type 1 (IL1R1) Interleukin-1 receptor family P14778
Other
Click To Hide/Show 14 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Centrosomal protein of 76 kDa (CEP76) CEP76 family Q8TAP6
Growth factor receptor-bound protein 7 (GRB7) GRB7/10/14 family Q14451
Keratin, type I cuticular Ha1 (KRT31) Intermediate filament family Q15323
Keratin, type I cuticular Ha4 (KRT34) Intermediate filament family O76011
Keratin-associated protein 10-9 (KRTAP10-9) KRTAP type 10 family P60411
Keratin-associated protein 12-3 (KRTAP12-3) KRTAP type 12 family P60328
Low-density lipoprotein receptor-related protein 6 (LRP6) LDLR family O75581
Platelet-derived growth factor subunit B (PDGFB) PDGF/VEGF growth factor family P01127
Phosphatidylinositol 3-kinase regulatory subunit alpha (PIK3R1) PI3K p85 subunit family P27986
Thyroid receptor-interacting protein 6 (TRIP6) Zyxin/ajuba family Q15654
Kelch-like protein 12 (KLHL12) . Q53G59
Keratinocyte proline-rich protein (KPRP) . Q5T749
Ras GTPase-activating protein 1 (RASA1) . P20936
Src-like-adapter (SLA) . Q13239

The Drug(s) Related To This Target

Approved
Click To Hide/Show 17 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Dasatinib Small molecular drug DB01254
Fostamatinib Small molecular drug DB12010
Imatinib Small molecular drug DB00619
Midostaurin Small molecular drug DB06595
Nintedanib Small molecular drug DB09079
Pazopanib Small molecular drug DB06589
Regorafenib Small molecular drug DB08896
Romiplostim Small molecular drug D01PZD
Sorafenib Small molecular drug D0W5HK
Sunitinib Small molecular drug DB01268
Tivozanib Small molecular drug DB11800
Becaplermin . D0T5QT
Erdafitinib . DB12147
Foreskin Fibroblast (Neonatal) . DB10770
Pexidartinib . DB12978
Pralsetinib . DB15822
Ripretinib . DB14840
Phase 3
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
E-3810 Small molecular drug D02WVT
Phase 2
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Famitinib Small molecular drug D0Z6MT
Mk-2461 Small molecular drug D00DRL
Snn-0031 . D0GB2L
Xl-820 . D00NSD
Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Tak-593 Small molecular drug D0T2ER
Investigative
Click To Hide/Show 110 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Xb-387 Antibody D00YNJ
(1h-indol-2-yl)(5-methoxy-1h-indol-2-yl)Methanone Small molecular drug D09OLH
(1h-indol-2-yl)(5-phenoxy-1h-indol-2-yl)Methanone Small molecular drug D0G0KQ
(1h-indol-2-yl)(6-methoxy-1h-indol-2-yl)Methanone Small molecular drug D0D7ZL
(2,4-dihydroindeno[1,2-c]Pyrazol-3-yl)Phenylamine Small molecular drug D05WTI
(5-fluoro-1h-indol-2-yl)-(1h-indol-2-yl)Methanone Small molecular drug D0H7MF
(5-hydroxy-1h-indol-2-yl)(1h-indol-2-yl)Methanone Small molecular drug D0XS9E
(Benzo[B]Furan-2-yl)-(1h-indol-2-yl)Methanone Small molecular drug D0I7QX
1-phenyl-1h-benzoimidazol-5-ol Small molecular drug D00YCU
1-phenyl-1h-benzoimidazole Small molecular drug D01FWD
2-(1h-indazol-3-yl)-1h-benzo[D]Imidazole Small molecular drug D0XC6G
3-((E)-styryl)-quinoline Small molecular drug D07JDY
3-(1h-indol-3-yl)-6,7-dimethoxy-quinoline Small molecular drug D06MCJ
3-(1h-indol-3-yl)-quinoline Small molecular drug D0GN3E
3-(2-cyclohexyl-ethyl)-6,7-dimethoxy-quinoline Small molecular drug D0K9ON
3-(3,4-dichloro-phenyl)-6,7-dimethoxy-quinoline Small molecular drug D0P0RD
3-(3,4-difluoro-phenyl)-6,7-dimethoxy-quinoline Small molecular drug D0AO6T
3-(3,4-dimethoxy-phenyl)-6,7-dimethoxy-quinoline Small molecular drug D08SUH
3-(3-fluoro-phenyl)-6,7-dimethoxy-quinoline Small molecular drug D0A6YP
3-(4-dimethylamino-benzylidenyl)-2-indolinone Small molecular drug D00QPG
3-(4-fluoro-phenyl)-6,7-dimethoxy-quinoline Small molecular drug D0I0GL
3-(6,7-dimethoxy-quinolin-4-yloxy)-phenol Small molecular drug D0K3CJ
3-(6,7-dimethoxy-quinolin-4-yloxy)-phenylamine Small molecular drug D02QBH
3-benzimidazol-2-ylhydroquinolin-2-one Small molecular drug D07QMC
3-benzyloxy-6,7-dimethoxy-quinoline Small molecular drug D06VNR
3-cyclohexylethynyl-6,7-dimethoxy-quinoline Small molecular drug D08KWL
3-cyclopent-1-enyl-6,7-dimethoxy-quinoline Small molecular drug D0KF3N
3-cyclopentyl-6,7-dimethoxy-quinoline Small molecular drug D00LRC
3-pyridin-3-yl-quinoline-6,7-diol Small molecular drug D0IR5I
3-pyridin-4-yl-quinolin-7-ol Small molecular drug D0H9TO
3-pyridin-4-yl-quinoline Small molecular drug D0Q3DS
3-pyridin-4-yl-quinoline-5,7-diol Small molecular drug D0K9VE
3-thiophen-3-yl-quinoline Small molecular drug D05GBY
4-(2,3-dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Small molecular drug D0F1RU
4-(3,4-dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Small molecular drug D0YE1X
4-(3,5-dimethoxy-phenoxy)-6,7-dimethoxy-quinoline Small molecular drug D0C2KK
4-(3-bromo-phenoxy)-6,7-dimethoxy-quinazoline Small molecular drug D03HLH
4-(3-bromo-phenoxy)-6,7-dimethoxy-quinoline Small molecular drug D05QMN
4-(3-ethoxy-phenoxy)-6,7-dimethoxy-quinoline Small molecular drug D0Y1CJ
4-(3-ethyl-phenoxy)-6,7-dimethoxy-quinoline Small molecular drug D03FCU
4-(3-fluoro-phenoxy)-6,7-dimethoxy-quinoline Small molecular drug D03IPZ
4-(5-methoxy-benzoimidazol-1-yl)-phenylamine Small molecular drug D0K2YG
4-(6,7-dimethoxy-quinolin-3-yl)-benzoic Acid Small molecular drug D03MQI
4-(6,7-dimethoxy-quinolin-3-yl)-phenol Small molecular drug D0H4JB
4-benzoimidazol-1-yl-phenylamine Small molecular drug D01MUN
5,6,7-trimethoxy-3-pyridin-4-yl-quinoline Small molecular drug D0SG0G
5,7-dimethoxy-3-pyridin-4-yl-quinoline Small molecular drug D0P0WT
5,7-dimethoxy-3-thiophen-3-yl-quinoline Small molecular drug D0RD5S
5,7-dimethyl-3-thiophen-3-yl-quinoline Small molecular drug D07ZWN
5-(6,7-dimethoxy-quinolin-3-yl)-1h-pyridin-2-one Small molecular drug D01UYS
5-methoxy-1-phenyl-1h-benzoimidazole Small molecular drug D02XKJ
6,7-dichloro-3-thiophen-3-yl-quinoline Small molecular drug D0CF9B
6,7-difluoro-3-thiophen-3-yl-quinoline Small molecular drug D0QT4X
6,7-dimethoxy-3-((E)-styryl)-quinoline Small molecular drug D06LLF
6,7-dimethoxy-3-(3-methoxy-phenyl)-quinoline Small molecular drug D07CFT
6,7-dimethoxy-3-(4-methoxy-phenyl)-quinoline Small molecular drug D0G0KN
6,7-dimethoxy-3-(4-nitro-phenyl)-quinoline Small molecular drug D08JGS
6,7-dimethoxy-3-p-tolyl-quinoline Small molecular drug D0C1BE
6,7-dimethoxy-3-phenyl-quinoline Small molecular drug D0G6SA
6,7-dimethoxy-3-phenylethynyl-quinoline Small molecular drug D0WW8M
6,7-dimethoxy-3-pyridin-3-yl-quinoline Small molecular drug D00RBV
6,7-dimethoxy-3-pyridin-4-yl-quinoline Small molecular drug D0T9FQ
6,7-dimethoxy-3-thiophen-2-yl-quinoline Small molecular drug D0G0ZQ
6,7-dimethoxy-4-(2-methoxy-phenoxy)-quinoline Small molecular drug D01XDV
6,7-dimethoxy-4-(3-methoxy-phenoxy)-quinoline Small molecular drug D09QTC
6,7-dimethoxy-4-(3-nitro-phenoxy)-quinoline Small molecular drug D0ZS3F
6,7-dimethoxy-4-(4-methoxy-phenoxy)-quinoline Small molecular drug D0R8BC
6,7-dimethoxy-4-m-tolyloxy-quinoline Small molecular drug D0VJ5W
6,7-dimethoxy-4-phenoxy-quinoline Small molecular drug D0CW1Q
6-methoxy-3-pyridin-4-yl-quinoline Small molecular drug D04PQX
6-methoxy-3-thiophen-3-yl-quinoline Small molecular drug D0W7IN
7-chloro-3-pyridin-4-yl-quinoline Small molecular drug D0Z4HV
7-fluoro-3-thiophen-3-yl-quinoline Small molecular drug D05SNG
7-methoxy-3-pyridin-4-yl-quinoline Small molecular drug D02PZZ
7-methoxy-3-thiophen-3-yl-quinoline Small molecular drug D0V8QI
7-thiophen-3-yl-[1,3]Dioxolo[4,5-g]Quinoline Small molecular drug D0A6AA
Agl 2043 Small molecular drug D0U3WQ
Benzyl-(6,7-dimethoxy-quinolin-3-yl)-amine Small molecular drug D02CUF
Bis(5-acetoxybenzo[B]Furan-2-yl)Methanone Small molecular drug D0L0MZ
Bis(5-aminobenzo[B]Furan-2-yl)Methanone Small molecular drug D07AXL
Bis(5-hydroxybenzo[B]Furan-2-yl)Methanone Small molecular drug D02OBA
Bis(5-methoxybenzo[B]Furan-2-yl)Methanone Small molecular drug D09PUW
Bis(6-hydroxybenzo[B]Furan-2-yl)Methanone Small molecular drug D03VAA
Bis(Benzo[B]Furan-2-yl)Methanone Small molecular drug D0Z3DW
Bis-(5-hydroxy-1h-indol-2-yl)-methanone Small molecular drug D0I3XZ
Bms-536924 Small molecular drug D0M4SY
Cp-673451 Small molecular drug D05QBZ
Di(1h-indol-2-yl)Methanone Small molecular drug D0G5YI
Gtp-14564 Small molecular drug D0UN9O
Hki-9924129 Small molecular drug D0D5EW
Jnj-10198409 Small molecular drug D0YZ7H
Ki-11502 Small molecular drug D06ZUA
Ki-20227 Small molecular drug D08BJR
Pd-0166326 Small molecular drug D0P3JW
Pd-0173952 Small molecular drug D0S1KJ
Pd-0173955 Small molecular drug D03NPX
Pd-0173956 Small molecular drug D0GW4Q
Pd-0173958 Small molecular drug D0Z7GH
Pd-0179483 Small molecular drug D0OH3J
Pdgf Receptor Tyrosine Kinase Inhibitor Iii Small molecular drug D0BW4G
Pmid22765894c8h Small molecular drug D0C2GE
Ro-4396686 Small molecular drug D09XIL
Rpr-101511 Small molecular drug D0W9BF
Rpr-108514a Small molecular drug D0FH3M
Su-11652 Small molecular drug D09LPL
Tg-100435 Small molecular drug D0H1OK
Trapidil Small molecular drug DB09283
Polaprezinc . DB09221
Xl820 . DB05146
Xl999 . DB05014
Patented
Click To Hide/Show 4 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid25656651-compound-21a Small molecular drug D0D3FB
Pmid25656651-compound-21b Small molecular drug D0XQ5F
Pmid28460551-compound-2 Small molecular drug D0YX2B
Pyridine Derivative 18 Small molecular drug D0AK1F
Discontinued
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ag1295 Small molecular drug D06GBK
Rg-13022 Small molecular drug D03WTT
Sri-62-834 Small molecular drug D00QCB
Cdp-860 . D08PAV
Cep-2563 . D0KX1E

References

1 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
2 Rapid Covalent-Probe Discovery by Electrophile-Fragment Screening. J Am Chem Soc. 2019 Jun 5;141(22):8951-8968. doi: 10.1021/jacs.9b02822. Epub 2019 May 22.
3 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
4 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
5 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264