General Information of the Protein
Protein ID
PT01237
Protein Name
Tyrosine-protein kinase Fyn
Secondarily
Protein Name
Proto-oncogene Syn
Proto-oncogene c-Fyn
Src-like kinase
p59-Fyn
Gene Name
FYN
Sequence
MGCVQCKDKEATKLTEERDGSLNQSSGYRYGTDPTPQHYPSFGVTSIPNYNNFHAAGGQGLTVFGGVNSSSHTGTLRTRGGTGVTLFVALYDYEARTEDDLSFHKGEKFQILNSSEGDWWEARSLTTGETGYIPSNYVAPVDSIQAEEWYFGKLGRKDAERQLLSFGNPRGTFLIRESETTKGAYSLSIRDWDDMKGDHVKHYKIRKLDNGGYYITTRAQFETLQQLVQHYSERAAGLCCRLVVPCHKGMPRLTDLSVKTKDVWEIPRESLQLIKRLGNGQFGEVWMGTWNGNTKVAIKTLKPGTMSPESFLEEAQIMKKLKHDKLVQLYAVVSEEPIYIVTEYMNKGSLLDFLKDGEGRALKLPNLVDMAAQVAAGMAYIERMNYIHRDLRSANILVGNGLICKIADFGLARLIEDNEYTARQGAKFPIKWTAPEAALYGRFTIKSDVWSFGILLTELVTKGRVPYPGMNNREVLEQVERGYRMPCPQDCPISLHELMIHCWKKDPEERPTFEYLQSFLEDYFTATEPQYQPGENL
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Kinase
>
Protein Kinase
>
TK protein kinase group
>
Tyrosine protein kinase Src family
Function
Non-receptor tyrosine-protein kinase that plays a role in many biological processes including regulation of cell growth and survival, cell adhesion, integrin-mediated signaling, cytoskeletal remodeling, cell motility, immune response and axon guidance. Inactive FYN is phosphorylated on its C-terminal tail within the catalytic domain. Following activation by PKA, the protein subsequently associates with PTK2/FAK1, allowing PTK2/FAK1 phosphorylation, activation and targeting to focal adhesions. Involved in the regulation of cell adhesion and motility through phosphorylation of CTNNB1 (beta-catenin) and CTNND1 (delta-catenin). Regulates cytoskeletal remodeling by phosphorylating several proteins including the actin regulator WAS and the microtubule-associated proteins MAP2 and MAPT. Promotes cell survival by phosphorylating AGAP2/PIKE-A and preventing its apoptotic cleavage. Participates in signal transduction pathways that regulate the integrity of the glomerular slit diaphragm (an essential part of the glomerular filter of the kidney) by phosphorylating several slit diaphragm components including NPHS1, KIRREL1 and TRPC6. Plays a role in neural processes by phosphorylating DPYSL2, a multifunctional adapter protein within the central nervous system, ARHGAP32, a regulator for Rho family GTPases implicated in various neural functions, and SNCA, a small pre-synaptic protein. Participates in the downstream signaling pathways that lead to T-cell differentiation and proliferation following T-cell receptor (TCR) stimulation. Phosphorylates PTK2B/PYK2 in response to T-cell receptor activation. Also participates in negative feedback regulation of TCR signaling through phosphorylation of PAG1, thereby promoting interaction between PAG1 and CSK and recruitment of CSK to lipid rafts. CSK maintains LCK and FYN in an inactive form. Promotes CD28-induced phosphorylation of VAV1. In mast cells, phosphorylates CLNK after activation of immunoglobulin epsilon receptor signaling (By similarity).
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Uniprot ID
Primary ID:
P06241

Secondarily ID:
B5BU57
E1P557
H0UI48
Q16248
Q5R3A6
Q5R3A7
Q8N5D7
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Ensembl ID
ENSG00000010810
HGNC ID
HGNC:4037
Subcellular Location
Cytoplasm
Nucleus
Cell membrane
Perikaryon
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000045 , A-375
Compound ID Compound Name Compound Formula
CP0672877
1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea
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C23H29FN6O
 1
1
IC50 = 91 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0005166
BMS-354825
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C22H26ClN7O2S
 5
1 IC50 = 0.2 nM
2 IC50 < 0.5 nM
3 IC50 = 1.6 nM
4 Kd = 0.79 nM
5 Kd = 0.8 nM
CP0004106
(2S,3R,4R,6R)-3-methoxy-2-methyl-4-(methylamino)-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-16-one
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C28H26N4O3
 6
1 IC50 = 1.1 nM
2 IC50 = 2 nM
3 IC50 = 2.06 nM
4 IC50 = 4.4 nM
5 Kd = 33 nM
6 Kd = 51 nM
CP0578545
2-N-benzyl-4-N-(5-cyclopropyl-1H-pyrazol-3-yl)thieno[3,2-d]pyrimidine-2,4-diamine
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C19H18N6S
 1
1 IC50 = 2.17 nM
CP0025272
3-(4-chlorophenyl)-1-(2-chloro-2-phenylethyl)pyrazolo[3,4-d]pyrimidin-4-amine
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C19H15Cl2N5
 1
1 Ki = 70 nM
Clinical Information about the Protein
Target 1 ( Fyn tyrosine protein kinase (FYN) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 Chronic myelogenous leukaemia [ICD-11: 2A20.0]
Approved Drug(s) 1 Approved Drug  1
1 Dasatinib Approved
Chronic myelogenous leukaemia