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Updated November 2019

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Nomenclature

Short Name:
LYN
Full Name:
Tyrosine-protein kinase Lyn
Alias:
  • EC 2.7.10.2
  • FLJ13161
  • LYN
  • V-yes-1 Yamaguchi sarcoma viral related oncogene
  • FLJ26625
  • JTK8
  • Kinase Lyn
  • KPM

Classification

Type:
Protein-tyrosine kinase
Group:
TK
Family:
Src
SubFamily:
NA
 
 

Specific Links

BioCarta Entry: bcr pathway
Entrez-Gene Entry: 4067
Entrez-Protein Entry: NP_002341
GeneCards Entry: JTK8
KinBASE Entry: LYN
OMIM Entry: 165120
Pfam Entry: P07948
PhosphoNET Entry: P07948
Phosphosite Plus Entry: 618
Protein Data Bank Entry: 1W1F
ScanSite Entry: P07948
Source Entry: LYN
UCSD-Nature Entry: A001441
UniProt Entry: P07948
Kinexus Products: LYN
Yes-related protein-tyrosine kinase; Tyrosine-protein kinase Lyn pan-specific antibody AB-NK095-2
Yes-related protein-tyrosine kinase; Tyrosine-protein kinase Lyn Y508 phosphosite-specific antibody AB-PK688
CDK1 (6-20) KinSub - Cyclin-dependent kinase 1 (CDC2) (K6-K20, human) peptide; Src protein kinase substrate peptide - Powder PE-01ADT95
Yes-related protein-tyrosine kinase / Tyrosine-protein kinase Lyn (G16-R34, human) peptide - Powder PE-01BDP80
LynSubtide - Lyn protein kinase substrate peptide - Powder PE-01BHY99
Yes-related protein-tyrosine kinase / Tyrosine-protein kinase Lyn (E505-Q511, human) pY508 phosphopeptide - Powder PE-04ANN90

General Links

ClustalW2
GPS-Cuckoo
Human Protein Atlas
Kinase.com
Kinase Research
Kinasource
Kinomer
Netphorest
NetworKIN
Phosida
PhosphoElm
Protein Blast
ScanSite
String

Structure

Mol. Mass (Da):
58574
# Amino Acids:
512
# mRNA Isoforms:
2
mRNA Isoforms:
58,574 Da (512 AA; P07948); 56,033 Da (491 AA; P07948-2)
4D Structure:
Interacts with phosphorylated LIME1 and with CD79A upon BCR activation. Interacts with Epstein-Barr virus LMP2A. Interacts with TGFB1I1. Interaction, via the SH2 and SH3, domains with MUC1 is stimulated by IL7 and, the subsequent phosphorylation increases the binding between MUC1 and CTNNB1/beta-catenin. Interacts with PPP1R15A and PDE4A via the SH3 domain. Interacts with Herpesvirus saimiri tyrosine kinase interacting protein (Tip). Interacts with ADAM15. Interacts with NDFIP2 and more weakly with NDFIP1.
1D Structure:
Retrieve Gene Sequence
Retrieve Full Protein Sequence
Retrieve Catalytic Domain Sequence
 
3D Image (rendered using PV Viewer):

PDB ID
3A4O

Subfamily Alignment
subfamily domain
 
Domain Distribution:
Start End Domain
63 123 SH3
129 226 SH2
246 496 TyrKc
247 499 Pkinase
 

Kinexus Products

Click on entries below for direct links to relevant products from Kinexus for this protein kinase.
hiddentext
○ Yes-related protein-tyrosine kinase; Tyrosine-protein kinase Lyn pan-specific antibody AB-NK095-2
○ Yes-related protein-tyrosine kinase; Tyrosine-protein kinase Lyn Y508 phosphosite-specific antibody AB-PK688
○ CDK1 (6-20) KinSub - Cyclin-dependent kinase 1 (CDC2) (K6-K20, human) peptide; Src protein kinase substrate peptide - Powder PE-01ADT95
○ Yes-related protein-tyrosine kinase / Tyrosine-protein kinase Lyn (G16-R34, human) peptide - Powder PE-01BDP80
○ LynSubtide - Lyn protein kinase substrate peptide - Powder PE-01BHY99
○ Yes-related protein-tyrosine kinase / Tyrosine-protein kinase Lyn (E505-Q511, human) pY508 phosphopeptide - Powder PE-04ANN90
 

Post-translation Modifications

For detailed information on phosphorylation of this kinase go to PhosphoNET
Myristoylated:
G2.
Palmitoylated:
C3.
Serine phosphorylated:

S11, S13, S115, S149, S158, S164, S228, S246, S269, S283, S326.
Threonine phosphorylated:

T58, T135, T276, T281, T296, T319, T398+, T438, T448, T502-, T503-, T504.
Tyrosine phosphorylated:

Y32, Y117, Y193, Y194, Y265, Y266-, Y306, Y316, Y321, Y397+, Y439, Y460, Y473, Y501, Y508-.
Ubiquitinated:
K9, K20, K59, K477.
 

Distribution

Based on gene microarray analysis from the NCBI
Human Tissue Distribution
% Max Expression:

Mean Expression:

Number of Samples:

Standard Deviation:
% Max Expression:

Mean Expression:

Number of Samples:

Standard Deviation:
  • adipose
    46

    1143

    42

    1267

  • adrenal
    4

    95

    23

    45

  • bladder
    3

    86

    14

    56

  • brain
    18

    442

    147

    928

  • breast
    34

    847

    36

    660

  • cervix
    5

    126

    111

    89

  • colon
    17

    411

    51

    558

  • heart
    44

    1079

    69

    2719

  • intestine
    40

    988

    24

    632

  • kidney
    3

    78

    141

    50

  • liver
    4

    93

    50

    70

  • lung
    31

    768

    282

    695

  • lymphnode
    10

    246

    47

    111

  • ovary
    2

    46

    21

    29

  • pancreas
    4

    90

    41

    88

  • pituitary
    4

    99

    24

    41

  • prostate
    4

    94

    366

    747

  • salivarygland
    4

    101

    28

    57

  • skeletalmuscle"
    2

    44

    134

    26

  • skin
    22

    538

    162

    552

  • spinalcord
    4

    87

    39

    45

  • spleen
    21

    513

    45

    335

  • stomach
    6

    153

    25

    98

  • testis
    2

    39

    29

    35

  • thymus
    3

    79

    39

    55

  • thyroid
    23

    574

    89

    657

  • tonsil
    15

    372

    50

    164

  • trachea
    8

    192

    29

    83

  • uterus
    3

    64

    29

    35

  • reticulocytes"
    4

    106

    42

    82

  • t-lymphocytes
    24

    590

    30

    599

  • b-lymphocytes
    39

    972

    51

    754

  • neutrophils
    100

    2474

    88

    2512

  • macrophages
    67

    1648

    83

    600

  • sperm
    20

    498

    48

    993

 

Evolution

Species Conservation
PhosphoNET % Identity:
PhosphoNET % Similarity:
Homologene %
Identity:
PhosphoNET % Identity:
PhosphoNET % Similarity:
Homologene %
Identity:
  • tableheader
    100

    100

    100
  • tableheader
    57.3

    68.5

    100
  • tableheader
    80

    81.5

    99
  • tableheader
    -

    -

    97
  • tableheader
    -

    -

    98
  • tableheader
    97

    99.2

    97
  • tableheader
    -

    -

    -
  • tableheader
    96

    98.8

    96
  • tableheader
    96

    98.8

    96
  • tableheader
    -

    -

    -
  • tableheader
    93.1

    96.6

    -
  • tableheader
    63

    77.7

    88
  • tableheader
    56.7

    72

    86
  • tableheader
    76.3

    86.9

    77.5
  • tableheader
    -

    -

    -
  • tableheader
    51.4

    69.2

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
  • tableheader
    -

    -

    -
For a wider analysis go to PhosphoNET Evolution in PhosphoNET
 

Regulation

Activation:
NA
Inhibition:
Phosphorylation of Thr-503 inhibits phosphotransferase activity.
Synthesis:
NA
Degradation:
NA
 

Kinections Map

Click here to download a PPT of the image below
 
Kinections GIF
 

Known Upstream Kinases

For further details on these substrates click on the Substrate Short Name or UniProt ID. Phosphosite Location is hyperlinked to PhosphoNET predictions.
Based on in vitro and/or in vivo phosphorylation data

Kinase Short Name UniProt ID (Human) Phosphosite Location Phosphosite Sequence Effect of Phosphorylation
LYN P07948 Y397 RVIEDNEYTAREGAK +
CSK P41240 T503 LDDFYTATEGQYQQQ -
CTK P42679 Y508 YTATEGQYQQQP___ -
CSK P41240 Y508 YTATEGQYQQQP___ -
 

Known Downstream Substrates

For further details on these substrates click on the Substrate Short Name or UniProt ID. Phosphosite Location is hyperlinked to PhosphoNET predictions.
Based on in vitro and/or in vivo phosphorylation data

Substrate Short Name UniProt ID (Human) Phosphosite Location Phosphosite Sequence Effect of Phosphorylation
Abl1 P00519 Y115 QGWVPSNYITPVNSL
Abl1 P00519 Y128 SLEKHSWYHGPVSRN
Abl1 P00519 Y139 VSRNAAEYLLSSGIN +
Abl1 P00519 Y172 LRYEGRVYHYRINTA
Abl1 P00519 Y185 TASDGKLYVSSESRF
Abl1 P00519 Y215 GLITTLHYPAPKRNK
Abl1 P00519 Y226 KRNKPTVYGVSPNYD +
Abl1 P00519 Y393 RLMTGDTYTAHAGAK +
Abl1 P00519 Y70 PNLFVALYDFVASGD +
Abl1 iso2 P00519-2 Y134 QGWVPSNYITPVNSL
Abl1 iso2 P00519-2 Y147 SLEKHSWYHGPVSRN
Abl1 iso2 P00519-2 Y158 VSRNAAEYLLSSGIN +
Abl1 iso2 P00519-2 Y191 LRYEGRVYHYRINTA
Abl1 iso2 P00519-2 Y204 TASDGKLYVSSESRF
Abl1 iso2 P00519-2 Y234 GLITTLHYPAPKRNK
Abl1 iso2 P00519-2 Y245 KRNKPTVYGVSPNYD +
Abl1 iso2 P00519-2 Y412 RLMTGDTYTAHAGAK +
Abl1 iso2 P00519-2 Y89 PNLFVALYDFVASGD +
Bcr P11274 Y177 ADAEKPFYVNVEFHH +
Btk Q06187 Y223 LKKVVALYDYMPMNA +
Btk Q06187 Y551 RYVLDDEYTSSVGSK +
Caspase 8 Q14790 Y380 TDSEEQPYLEMDLSS
Caspase 8 Q14790 Y448 TILTEVNYEVSNKDD
CD19 P15391 Y500 TSLGSQSYEDMRGIL
CD19 P15391 Y531 HEEDADSYENMDNPD
CDK2 P24941 Y15 EKIGEGTYGVVYKAR -
CDK4 P11802 Y17 AEIGVGAYGTVYKAR -
CK2a1 (CSNK2A1) P68400 S194 EYNVRVASRYFKGPE +
CK2a1 (CSNK2A1) P68400 S2 ______MSGPVPSRA
CK2a1 (CSNK2A1) P68400 Y255 VLGTEDLYDYIDKYN
CSF2RB P32927 Y466 ALRFCGIYGYRLRRK
CSF2RB P32927 Y468 RFCGIYGYRLRRKWE
CSF2RB P32927 Y822 VLQQVGDYCFLPGLG ?
CSF2RB P32927 Y882 KALKQQDYLSLPPWE ?
DAPP1 Q9UN19 Y139 KVEEPSIYESVRVHT
DOK2 O60496 Y271 LPRPDSPYSRPHDSL
DOK2 O60496 Y299 PRGQEGEYAVPFDAV
DOK2 O60496 Y345 PPRPDHIYDEPEGVA
EpoR P19235 Y489 DGPYSNPYENSLIPA ?
EpoR P19235 Y504 AEPLPPSYVACS___ ?
FcGR2A P12318 Y304 TDDDKNIYLTLPPND
FcGR2B P31994 Y292 GAENTITYSLLMHPD
FcGR2C P31995 Y310 TDDDKNIYLTLPPND
GCET2 Q8N6F7 Y107 GNSAEEYYENVPCKA
GCET2 Q8N6F7 Y128 LGGTETEYSLLHMPS
GluR2 P42262 Y876 YKEGYNVYGIESVKI
GRP58 P30101 Y445 ANDVPSPYEVRGFPT
GRP58 P30101 Y454 VRGFPTIYFSPANKK
GRP58 P30101 Y467 KKLNPKKYEGGRELS
HS1 (HCLS1) P14317 Y222 MEAPTTAYKKTTPIE +
LAB Q9GZY6 Y110 RHGSEEAYIDPIAME
LAB Q9GZY6 Y118 IDPIAMEYYNWGRFS
LAB Q9GZY6 Y119 DPIAMEYYNWGRFSK
LAB Q9GZY6 Y136 EDDDANSYENVLICK
LAB Q9GZY6 Y95 EDPASSRYQNFSKGS
LPXN O60711 Y72 NIQELNVYSEAQEPK
Lyn P07948 Y397 RVIEDNEYTAREGAK +
NIPP-1 Q12972 Y335 NEPKKKKYAKEAWPG
NMT1 P30419 Y117 EEASKRSYQFWDTQP
NMT1 P30419 Y180 YTLLNENYVEDDDNM +
p27Kip1 P46527 T187 NAGSVEQTPKKPGLR +
p27Kip1 P46527 Y88 KGSLPEFYYRPPRPP ?
PAG (PAG1) Q9NWQ8 Y381 GEEPEPDYEAIQTLN
PAG (PAG1) Q9NWQ8 Y387 SEEPEPDYEAIQTLN
PAG (PAG1) Q9NWQ8 Y417 LVPKENDYESISDLQ
PAG (PAG1) Q9NWQ8 Y431 LTVPESTYTSIQGDP
PKCd (PRKCD) Q05655 Y155 IKQAKIHYIKNHEFI -
PKCd (PRKCD) Q05655 Y313 SSEPVGIYQGFEKKT +
PKCd (PRKCD) Q05655 Y334 MQDNSGTYGKIWEGS ?
PKCd (PRKCD) Q05655 Y52 VQKKPTMYPEWKSTF -
PKCd (PRKCD) Q05655 Y567 IRVDTPHYPRWITKE -
PTEN P60484 Y240 RREDKFMYFEFPQPL +
PTPN6 (SHP1) P29350 Y564 SKHKEDVYENLHTKN +
RGS16 O15492 Y168 TLMEKDSYPRFLKSP
RGS16 O15492 Y177 RFLKSPAYRDLAAQA
SLAM/SLAMF1 Q13291 Y327 ETNSITVYASVTLPE
SLC4A1 P02730 Y21 ENLEQEEYEDPDIPE
SLC4A1 P02730 Y359 AKPDSSFYKGLDLNG
SLC4A1 P02730 Y8 MEELQDDYEDMMEEN
SLC4A1 P02730 Y904 EEEGRDEYDEVAMPV
SNCA P37840 Y125 VDPDNEAYEMPSEEG
STAT5A P42229 Y694 LAKAVDGYVKPQIKQ +
Syk P43405 Y323 STVSFNPYEPELAPW +
Syk P43405 Y348 LPMDTEVYESPYADP +
Syk P43405 Y352 TEVYESPYADPEEIR +
TIF1B Q13263 Y449 PMEVQEGYGFGSGDD +
TIF1B Q13263 Y458 FGSGDDPYSSAEPHV +
TIF1B Q13263 Y517 PGSTTEDYNLIVIER +
TRIM28 Q13263 Y458 FGSGDDPYSSAEPHV +
TRIM28 Q13263 Y517 PGSTTEDYNLIVIER +
TRPV4 Q9HBA0 Y253 IERRCKHYVELLVAQ
WASP P42768 Y291 AETSKLIYDFIEDQG +
 

Protein Kinase Specificity

Matrix of observed frequency (%) of amino acids in aligned protein substrate phosphosites

Kinections GIF
Matrix Type:
Experimentally derived from alignment of 106 known protein substrate phosphosites and 110 peptides phosphorylated by recombinant Lyn in vitro tested in-house by Kinexus.
Domain #:
1
 

Inhibitors

For further details on these inhibitors click on the Compound Name and enter it into DrugKiNET or click on the ID's
Based on in vitro and/or in vivo phosphorylation data
Compound Name KD, Ki or IC50 (nM) PubChem ID ChEMBL ID PubMed ID
Dasatinib Ki = 130 pM 11153014 1421 15546730
CHEMBL1784637 IC50 < 150 pM 46864270 1784637 21561767
Ponatinib IC50 = 240 pM 24826799 20513156
Staurosporine IC50 = 490 pM 5279 19397322
PD173955 Kd = 2.2 nM 447077 386051 22037378
CHEMBL249097 IC50 = 3 nM 25138012 249097 17600705
CHEMBL364623 IC50 = 4 nM 11153014 364623 17154512
Bosutinib Kd = 4.2 nM 5328940 288441 22037378
Foretinib Kd = 9.1 nM 42642645 1230609 22037378
AST-487 Kd = 14 nM 11409972 574738 18183025
Bafetinib IC50 = 19 nM 24853523 16105974
CHEMBL436137 IC50 = 21 nM 11719421 436137 16931012
Lck Inhibitor IC50 < 25 nM 6603792 22037377
CHEMBL230686 Ki = 25.9 nM 11562302 230686 17113292
Kinome_714 IC50 = 26 nM 46886323 20346655
CHEMBL1092754 IC50 = 27.7 nM 44541014 1092754 20188552
SureCN5520662 IC50 = 28 nM 24766030 477817 18606543
DCC2036 IC50 = 29 nM 25066467
BML-275 IC50 > 50 nM 11524144 478629 22037377
GSK-3 Inhibitor IX IC50 > 50 nM 5287844 409450 22037377
PP121 IC50 < 50 nM 24905142 18849971
SU11652 IC50 > 50 nM 24906267 13485 22037377
TWS119 IC50 > 50 nM 9549289 405759 22037377
Masitinib Kd = 61 nM 10074640 22037378
AT9283 IC50 > 100 nM 24905142 19143567
BMS-690514 Kd < 100 nM 11349170 21531814
Nilotinib Kd = 100 nM 644241 255863 22037378
Vandetanib Kd = 110 nM 3081361 24828 18183025
Aloisine A IC50 > 150 nM 5326843 75680 22037377
Alsterpaullone; 2-Cyanoethyl IC50 > 150 nM 16760286 260138 22037377
Cdk1/2 Inhibitor III IC50 > 150 nM 5330812 261720 22037377
GSK-3 Inhibitor X IC50 > 150 nM 6538818 430226 22037377
Hesperadin Kd < 150 nM 10142586 514409 19035792
IDR E804 IC50 > 150 nM 6419764 1802727 22037377
K-252a; Nocardiopsis sp. IC50 > 150 nM 3813 281948 22037377
Ki11502 IC50 > 150 nM 22037377
N-Benzoylstaurosporine IC50 > 150 nM 56603681 608533 22037377
Src Kinase Inhibitor I IC50 > 150 nM 1474853 97771 22037377
SU6656 IC50 > 150 nM 5353978 605003 22037377
SureCN7018367 Kd < 150 nM 18792927 450519 19035792
Motesanib Kd = 160 nM 11667893 572881 18183025
Lestaurtinib Kd = 190 nM 126565 22037378
Nintedanib IC50 = 195 nM 9809715 502835 18559524
Ibrutinib IC50 = 200 nM 24821094 1873475 21958547
Imatinib IC50 = 220 nM 123596 941 17376680
AG1478 IC50 > 250 nM 2051 7917 22037377
Alsterpaullone IC50 > 250 nM 5005498 50894 22037377
Compound 56 IC50 > 250 nM 2857 29197 22037377
Flt-3 Inhibitor II IC50 > 250 nM 11601743 377193 22037377
JAK3 Inhibitor VI IC50 > 250 nM 16760524 22037377
SB218078 IC50 > 250 nM 447446 289422 22037377
SU11274 IC50 > 250 nM 9549297 261641 22037377
Syk Inhibitor IC50 > 250 nM 6419747 104279 22037377
WHI-P154 IC50 > 250 nM 3795 473773 22037377
Cediranib Kd = 270 nM 9933475 491473 22037378
Sunitinib Kd = 270 nM 5329102 535 18183025
NVP-TAE684 Kd = 280 nM 16038120 509032 22037378
SureCN2934634 IC50 = 290 nM 45375865 1080994 19854645
BGJ398 IC50 = 300 nM 53235510 21936542
CHEMBL307152 IC50 < 300 nM 11655119 307152 12824014
TG101209 IC50 < 300 nM 16722832 17541402
Dovitinib Kd = 370 nM 57336746 18183025
RAF265 Kd = 370 nM 11656518 558752 18183025
Alisertib IC50 < 500 nM 24771867 22016509
BPIQ-I IC50 = 500 nM 2427 22037377
Pazopanib IC50 = 500 nM 10113978 477772 22037377
PP1 Analog II; 1NM-PP1 IC50 = 500 nM 5154691 573578 22037377
TG101348 Kd = 500 nM 16722836 1287853 22037378
Tozasertib IC50 = 500 nM 5494449 572878 22037377
AMG458 IC50 = 506 nM 16086104 386661 18553959
Erlotinib Kd = 530 nM 176870 553 18183025
Ki-20227 Kd = 710 nM 9869779 1908396 22037378
Pelitinib Kd = 720 nM 6445562 607707 18183025
Canertinib Kd = 780 nM 156414 31965 15711537
SU14813 Kd = 810 nM 10138259 1721885 18183025
Neratinib Kd = 820 nM 9915743 180022 22037378
CUDC-101 IC50 = 840 nM 24756910 598797 20143778
Crizotinib Kd = 940 nM 11626560 601719 22037378
Doramapimod IC50 = 960 nM 156422 103667 22014550
Gefitinib Kd = 990 nM 123631 939 18183025
CGP74514A IC50 > 1 µM 2794188 367625 22037377
CHEMBL566515 Kd < 1 µM 44478401 566515 19788238
Flt-3 Inhibitor III IC50 > 1 µM 11772958 22037377
Indirubin-3′-monoxime IC50 > 1 µM 5326739 22037377
JNJ-10198409 IC50 > 1 µM 9797370 120077 22037377
Kenpaullone IC50 > 1 µM 3820 296586 22037377
MK5108 IC50 > 1 µM 24748204 20053775
PD158780 IC50 > 1 µM 4707 53753 22037377
Purvalanol A IC50 > 1 µM 456214 23327 22037377
Silmitasertib IC50 > 1 µM 24748573 21174434
SNS314 IC50 > 1 µM 16047143 514582 18678489
SureCN10063060 Ki > 1 µM 52936621 21391610
WZ3146 Kd > 1 µM 44607360 20033049
WZ4002 Kd > 1 µM 44607530 20033049
PLX4720 Kd = 1.1 µM 24180719 1230020 22037378
SureCN5632345 Kd < 1.25 µM 44593646 515466 19035792
MLN8054 Kd = 1.4 µM 11712649 259084 18183025
Barasertib Kd = 1.6 µM 16007391 215152 18183025
Kinome_2553 Ki > 1.6 µM 16007116 377383 16854050
CHEMBL248757 Ki > 1.667 µM 44444843 248757 17935989
CHEMBL1240703 Kd = 1.7 µM 52945601 1240703 19654408
JNK Inhibitor VIII Ki > 1.7 µM 11624601 210618 16759099
Kinome_3027 Ki > 1.7 µM 11640926 378627 16759099
Kinome_3028 Ki > 1.7 µM 11590363 210928 16759099
VX745 Kd = 1.7 µM 3038525 119385 18183025
Momelotinib IC50 > 2 µM 25062766 19295546
CHEMBL451523 IC50 = 2.4 µM 9917045 451523 19356929
Sorafenib Kd = 3 µM 216239 1336 18183025
KW2449 Kd = 3.1 µM 11427553 1908397 22037378
SureCN4875304 IC50 > 3.5 µM 46871765 20472445
JNJ-28871063 IC50 > 4 µM 17747413 17975007
Ponatinib IC50 = 160 pM 24826799 20513156
Staurosporine IC50 = 490 pM 5279 19397322
Dasatinib IC50 < 25 nM 11153014 1421 22037377
PP121 IC50 < 25 nM 24905142 18849971
Bosutinib IC50 > 50 nM 5328940 288441 22037377
Dovitinib IC50 > 50 nM 57336746 22037377
Lck Inhibitor IC50 > 50 nM 6603792 22037377
SU6656 IC50 = 130 nM 5353978 605003 18077363
GSK-3 Inhibitor IX IC50 > 150 nM 5287844 409450 22037377
Masitinib IC50 > 150 nM 10074640 22037377
SU11652 IC50 > 150 nM 24906267 13485 22037377
TWS119 IC50 > 150 nM 9549289 405759 22037377
K-252a; Nocardiopsis sp. IC50 > 250 nM 3813 281948 22037377
Ki11502 IC50 > 250 nM 22037377
PDK1/Akt/Flt Dual Pathway Inhibitor IC50 > 250 nM 5113385 599894 22037377
Src Kinase Inhibitor I IC50 > 250 nM 1474853 97771 22037377
Compound 56 IC50 = 500 nM 2857 29197 22037377
GSK-3 Inhibitor X IC50 = 500 nM 6538818 430226 22037377
IDR E804 IC50 = 500 nM 6419764 1802727 22037377
JAK3 Inhibitor VI IC50 = 500 nM 16760524 22037377
Nilotinib IC50 = 500 nM 644241 255863 22037377
SU11274 IC50 = 500 nM 9549297 261641 22037377
Vemurafenib IC50 = 599 nM 42611257 1229517 20823850
BML-275 IC50 > 1 µM 11524144 478629 22037377
Cdk1/2 Inhibitor III IC50 > 1 µM 5330812 261720 22037377
Flt-3 Inhibitor II IC50 > 1 µM 11601743 377193 22037377
Gefitinib IC50 > 1 µM 123631 939 22037377
Pazopanib IC50 > 1 µM 10113978 477772 22037377
WHI-P154 IC50 > 1 µM 3795 473773 22037377
 

Disease Linkage

General Disease Association:

Cancer, neurological disorders
Specific Diseases (Non-cancerous):

Chorea-Acanthocytosis; Acanthocytosis
Specific Cancer Types:
Sarcomas
Comments:
LYN appears to be an oncoprotein (OP). Lyn is constitutively phosphorylated and activated in cells of chronic myelogenous leukemia (CML) and acute myeloid leukemia (AML) patients. Abnormally enhanced expression levels of activation of Lyn signalling can be critical in survival and proliferation of some types of cancers.
 
Gene Expression in Cancers:

TranscriptoNET (www.transcriptonet.ca) analysis with mRNA expression data retrieved from the National Center for Biotechnology Information's Gene Expression Omnibus (GEO) database, which was normalized against 60 abundantly and commonly found proteins, indicated altered expression for this protein kinase as shown here as the percent change from normal tissue controls (%CFC) as supported with the Student T-test in the following types of human cancers: Barrett's esophagus epithelial metaplasia (%CFC= +309, p<0.0001); Bladder carcinomas (%CFC= +85, p<0.002); Brain glioblastomas (%CFC= -98, p<0.002); Brain oligodendrogliomas (%CFC= -54, p<0.088); Cervical cancer (%CFC= -71, p<0.0001); Clear cell renal cell carcinomas (cRCC) (%CFC= +90, p<0.0009); Colon mucosal cell adenomas (%CFC= +47, p<0.0001); Large B-cell lymphomas (%CFC= +90, p<0.019); Oral squamous cell carcinomas (OSCC) (%CFC= +604, p<0.0001); Papillary thyroid carcinomas (PTC) (%CFC= +81, p<0.096); Pituitary adenomas (ACTH-secreting) (%CFC= -53, p<0.053); Prostate cancer - metastatic (%CFC= +46, p<0.0001); and Skin squamous cell carcinomas (%CFC= +102, p<0.0009). The COSMIC website notes an up-regulated expression score for LYN in diverse human cancers of 404, which is 0.9-fold of the average score of 462 for the human protein kinases. The down-regulated expression score of 19 for this protein kinase in human cancers was 0.3-fold of the average score of 60 for the human protein kinases.
Mutagenesis Experiments:

Insertional mutagenesis studies in mice have not yet revealed a role for this protein kinase in mouse cancer oncogenesis.
Mutation Rate in All Cancers:

Percent mutation rates per 100 amino acids length in human cancers: 0.08 % in 25188 diverse cancer specimens. This rate is only 12 % higher than the average rate of 0.075 % calculated for human protein kinases in general.
Mutation Rate in Specific Cancers:

Highest percent mutation rates per 100 amino acids length in human cancers: 0.49 % in 805 skin cancers tested; 0.43 % in 1093 large intestine cancers tested; 0.32 % in 602 endometrium cancers tested.
Frequency of Mutated Sites:

None > 3 in 20,440 cancer specimens
Comments:
Only 3 deletions, and no insertions or complex mutations are noted on the COSMIC website.
 
COSMIC Entry:
LYN
OMIM Entry:
165120
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