Tyrosine kinase

From Proteopedia

(Difference between revisions)

Revision as of 09:48, 27 November 2016

Human Fyn tyrosine kinase kinase domain complex with inhibitor staurosporine (PDB code 2dq7).

Drag the structure with the mouse to rotate

1 Function
2 Relevance
3 Disease
4 Structural highlights
5 Traditional Chinese medicine as dual guardians against hypertension and cancer? ^[6]

Function

Tyrosine kinase (TK) transfers a phosphate group from ATP to tyrosine residues of proteins^[1]. TKs are classified as receptor-TK which are membrane-attached and cytoplasmic non-receptor TKs. Staurosporine inhibits TK and prevents ATP binding to it.
For Abelson tyrosine kinase see:

Bcr-Abl and Imatinib (STI571 or Gleevec)
Imatinib (Gleevec)
Dasatinib (Sprycel)
Nilotinib (Tasigna)

For Src tyrosine kinase^[2] see:

For Kit tyrosine kinase (or SCF or stem cell factor) see:

SCF-KIT

For Tyk tyrosine kinase see:

Student Project 5 for UMass Chemistry 423 Spring 2015

Relevance

Bcr-Abl inhibitors are used against chronic myelogenous leukemia (CLM)^[3].

Disease

Mutated TK can cause unregulated growth of the cell and their inhibitors can be effective cancer treatment^[4].

Structural highlights

TK contains, starting from the N-terminal, SH4 – a membrane attachment domain; SH3 and SH2 domains which are a sequence-specific phosphotyrosine binding domains with roles in protein-protein interactions and the SH1 catalytic kinase domain. The staurosporine inhibitor binds the kinase domain of Fyn TK which contains a phosphotyrosine, in the groove between the N- and C-lobes^[5].

Traditional Chinese medicine as dual guardians against hypertension and cancer? ^[6]

functions as a signal protein and is implicated in various diseases. The carboxyl terminal of Src kinase is important in regulating conformation and activity of Src. Src protein is locked as an inward folding conformation through binding between the phosphorylated Tyr527 and the SH2 domain under normal inactive conditions. Src is activated when dephosphorylation of Tyr527 and phosphorylation of Tyr419 occurs. From N-terminal to C-terminal, Src is composed of a (residues 270–340; colored in violet) which binds adenosine triphosphate (ATP) and a (residues 345–523; colored in green) which binds with substrates. The ATP binding site is also partially located in the larger lobe. By regulating the alpha-helix structure, the large lobe can move toward or away from the small lobe, opening or closing the cleft between the two lobes. The Src catalytic site is located within the cleft. An open conformation allows the entrance of ATP into the cleft and exit of adenosine diphosphate (ADP) from the cleft. Drugs that can either interact with the residues (404–432) on the activation loop or inhibit the activation loop from moving away and opening the cleft as a result of Tyr419 phosphorylation can effectively inhibit Src activity. In this in vivo study, and have multiple stable interactions with the two Src cleft loops while simultaneously interacting with Asp407, hindering the activation loop from activation. Considering the aforementioned interactions with Src and high afﬁnity with EGFR, HER2, and HSP90, we suggest that Angeliferulate and HMID which both originate from the TCM Angelica sinensis may have potential as multi-targeting drug leads.

3D structures of tyrosine kinase

Updated on 27-November-2016 {{#tree:id=OrganizedByTopic|openlevels=0|

NON-RECEPTOR TYROSINE KINASES - nRTK

Fyn tyrosine kinase (Domains: SH3 80-141; SH2 142-247; kinase 260-537)

- 1shf, 3ua6 – hTK Fyn SH3 domain – human
- 3h0f, 3h0h, 3h0i, 3cqt - hTK Fyn SH3 domain (mutant)
- 2l2p, 2lp5 - cTK Fyn SH3 domain (mutant)- chicken - NMR
- 3uf4 – mTK Fyn SH3-SH2 domain – mouse
- 1zbj - hTK Fyn SH3 domain – NMR
- 1g83 - hTK Fyn SH2+SH3 domains (mutant)

Fyn complex

- 1fyn, 4znx - hTK Fyn SH3 domain + peptide
- 1nyf, 1nyg - hTK Fyn SH3 domain + peptide – NMR
- 1efn, 1avz - hTK Fyn SH3 domain + HIV Nef protein
- 1m27 - hTK Fyn SH3 domain + SH2 domain protein 1A + SLAM peptide
- 4d8d - hTK Fyn SH3 domain (mutant) + HIV Nef protein
- 3ua7 – hTK Fyn SH3 domain + hepatitis virus peptide
- 4eik - hTK Fyn SH3 domain + VSL12 peptide
- 1aot, 1aou - hTK Fyn SH2 domain + phosphopeptide - NMR
- 2dq7 – hTK kinase domain + staurosporine

Abelson tyrosine kinase

Abl1 SH2 domain residues 120-220

- 1ab2 - hTK SH2 domain – NMR
- 3uyo, 3t04, 3k2m, 5dc4, 5dc9 - hTK SH2 domain + monobody

Abl1 SH3 domain residues 60-121

- 1ju5 - hTK SH3 domain (mutant) + CRK SH2 domain + phosphopeptide - NMR
- 1awo - hTK SH3 domain + phosphopeptide – NMR
- 1bbz - hTK SH3 domain + peptide
- 2o88 - hTK SH3 domain (mutant} + peptide
- 1abo - mTK SH3 domain + peptide
- 1abq - mTK SH3 domain
- 4jjb, 4jjc, 4jjd - hTK abl SH3 domain
- 4j9b, 3egu, 3eg2, 3eg3, 3eg0, 3eg1 - hTK abl SH3 domain (mutant)
- 4j9c, 4j9e, 4j9i - hTK abl SH3 domain (mutant) + p17 peptide
- 4j9d, 4j9f - hTK abl SH3 domain (mutant) + p0 peptide
- 4j9g, 4j9h - hTK abl SH3 domain (mutant) + p7 peptide

Abl1 SH3-SH2 domain

- 2abl - hTK SH3-SH2 domain
- 2fo0 - hTK SH3-SH2 domain (mutant)

Abl1 kinase domain residues 229-512

- 2g2h - hTK kinase domain (mutant)
- 1opj, 1opk - mTK kinase domain
- 2g1t - hTK kinase domain + peptide
- 2g2i, 2g2f - hTK kinase domain (mutant) + peptide
- 3ue4, 3cs9, 2hzi, 2hz4, 2hz0, 2hyy, 2gqg, 4wa9 - hTK kinase domain + cancer drug
- 2f4j, 4twp - hTK kinase domain (mutant) + cancer drug
- 3qrk, 3qri, 3qrj, 2v7a, 2e2b, 2hiw, 4zog, 5hu9, 4yc8 - hTK kinase domain + inhibitor
- 1fpu, 1m52, 2qoh, 3kf4, 3kfa - mTK kinase domain + inhibitor
- 2z60, 3dk3, 3dk6, 3dk7 - mTK kinase domain (mutant) + inhibitor
- 1iep, 2hzn, 3k5v, 3ms9, 3mss, 3oxz - mTK kinase domain + cancer drug
- 3ik3, 3oy3 - mTK kinase domain (mutant) + cancer drug

Abl1 SH2-kinase domain residues 119-531

- 4xey - hTK SH2-kinase domain

Abl1 SH3-SH2-kinase domain residues 1-531

- 1opl - hTK SH3-SH2-kinase domain (mutant}

Abl1 F-actin binding domain residues 1007-1130

- 1zzp - hTK abl F-actin binding domain – NMR

Abl2 SH2 domain residues 165-273

- 4eih - hTK SH2 domain
- 2ecd - hTK SH2 domain – NMR

Abl2 kinase domain residues 279-546

- 3gvu - hTK kinase domain + Gleevec
- 3hmi - hTK kinase domain + inhibitor
- 2xyn - hTK kinase domain + cancer drug

Abl2 C-terminal residues 1058-1182

- 2kk1 – hTK C terminal – NMR

Anaplastic lymphoma kinase (Alk)

- 2xb7, 2xba, 3aox - hTK kinase domain + inhibitor
- 4dce, 4fob, 4foc, 4fod, 4fny, 4fnz, 4joa - hTK kinase domain (mutant) + inhibitor
- 2xp2 - hTK kinase domain + cancer drug
- 2yfx, 4anq, 4ans - hTK kinase domain (mutant) + cancer drug
- 3l9p, 3lcs, 3lct, 2yhv, 2yjr, 2yjs, 4fnw, 4fnx, 4anl - hTK kinase domain (mutant)

Csk tyrosine kinase

- 3eac - hTK SH2 domain
- 3eaz - hTK SH2 domain (mutant)
- 2rsy - hTK SH2 domain + CBP phosphopeptide - NMR
- 1csk - hTK SH3 domain
- 1jeg - hTK SH3 domain + tyrosine phosphatase peptide - NMR
- 1byg - hTK kinase domain + staurosporine
- 3d7t, 3d7u - hTK kinase domain (mutant) + C-Src
- 1k9a - TK C terminal - rat

Jak tyrosine kinase see Janus kinase

p55-blk tyrosine kinase

- 1blj, 1blk - mTK p55-blk SH2 domain – NMR

Src tyrosine kinase (Domains: SH3 85-140; SH2 140-251; kinase 253-535)

Src tyrosine kinase SH2 domain

- 3eac - hTK
- 4f59, 3eaz - hTK (mutant)
- 1f2f - cTK (mutant)
- 1spr - RsvTK + phosphate – Rous sarcoma virus
- 2jyq – RsvTK – NMR
- 1kc2, 1sps, 1is0, 1nzl, 1nzv - RsvTK + peptide
- 1sha, 1shb - RsvTK + phosphopeptide
- 1shd - cTK + TRKA receptor
- 4f5b - hTK (mutant) + phosphotyrosine
- 4f5a - hTK (mutant) + phosphate
- 1o4c - hTK + phosphate
- 1o41, 1o42, 1o43, 1o44, 1o45, 1o46, 1o47, 1o48, 1o49, 1o4a, 1o4b, 1o4d, 1o4e, 1o4f, 1o4g, 1o4h, 1o4i, 1o4j, 1o4k, 1o4l, 1o4m, 1o4n, 1o4o, 1o4p, 1o4q, 1o4r - hTK + inhibitor
- 1hcs, 1hct - hTK + peptide - NMR
- 1a07, 1a08, 1a09, 1a1a, 1a1b, 1a1c, 1a1e - hTK + peptide
- 1f1w - cTK (mutant) + peptide
- 1p13 - cTK + peptide
- 1qwe, 1qwf - RsvTK + peptide

Src tyrosine kinase SH3 domain

- 1srl, 1srm - cTK – NMR
- 3fj5, 4jz3, 4jz4 - cTK
- 4le9, 4oml, 4omm, 4omn, 4omo, 4omp, 4omq, 5i11, 4rtu, 4rtx - cTK (mutant)
- 4y92 - TK (mutant) Avian sarcoma virus
- 4hxj, 1prl, 4qt7, 4rty, 4rtz - cTK + peptide
- 1prm, 1rlp, 1rlq, 1nlo, 1nlp - cTK + peptide - NMR
- 4hvu, 4hvv, 4hvw, 4rtv, 4rtw - cTK (mutant) + peptide
- 1jeg – TK + protein-tyrosine phosphatase peptide – mouse

Src tyrosine kinase kinase domain residues 253-535

- 3of0, 2qi8 - cTK (mutant)
- 1yo6 - hTK
- 1yoj - hTK (mutant)
- 3tz7, 3tz8, 3tz9, 4dgg – cTK (mutant) + pyrazolin derivative
- 4fic, 3uqg, 3uqf, 3u51, 3u4w, 4agw, 3qlg, 3qlf, 3g6g, 3el8, 3f6x, 2hwo, 2hwp, 2oiq, 3en4, 3en5, 3en6, 3en7, 3el7, 5bmm, 5j5s, 4ybj, 4ybk – cTK + inhibitor
- 4lgg, 4lgh, 3svv, 3oez, 3lok, 3g5d, 3f3w, 3f3v, 3geq, 3g6h, 3f3t, 3f3u, 2qlq, 2qq7, 4lgg, 4lgh, 4mcv, 4o2p – cTK (mutant) + inhibitor
- 4u5j – cTK (mutant) + cancer drug
- 1yol, 1yom – hTK (mutant) + inhibitor
- 2bdf, 2bdj – hTK + inhibitor
- 1byg – hTK + staurosporine
- 4mxo – hTK + cancer drug
- 4mxx, 4mxy, 4mxz – hTK (mutant) + cancer drug
- 3d7t, 3d7u – cTK + Csk
- 3dqw, 3dqx - cTK (mutant) + ATP

Src tyrosine kinase C terminal domain

- 1k9a – rTK – rat

Src tyrosine kinase SH2+SH3+kinase domains residues 85-535

- 1ksw – hTK (mutant)+ ADP derivative
- 1y57 – hTK + inhibitor
- 4k11 – hTK (mutant) + inhibitor

Src tyrosine kinase SH2+SH3+kinase+C terminal domains

- 1fmk – hTK
- 2ptk – cTK
- 2src – hTK + AMPPNP

Src tyrosine kinase N terminal+SH2+SH3+kinase domains

- 2h8h – hTK + inhibitor

Lymphocyte-specific tyrosine kinase Lck (Domains: SH3 58-118; SH2 122-225; kinase 230-500)

- 1kik, 1h92 - hTK Lck SH3 domain – NMR
- 2iim - hTK Lck SH3 domain
- 4d8k, 1x27 - hTK Lck SH3-SH2 domain
- 3lck - hTK Lck kinase domain

Lck complex

- 1lcj, 1lkk, 1lkl - hTK Lck SH2 domain (mutant) + phosphopeptide
- 1cwd, 1cwe, 1ijr - hTK Lck SH2 domain + phosphopeptide
- 1bhf - hTK Lck SH2 domain + peptide inhibitor
- 1fbz - hTK Lck SH2 domain + inhibitor
- 1bhh - hTK Lck SH2 domain + T-lymphocyte-specific TK
- 1lck - hTK Lck SH3-SH2 domain (mutant) + phosphopeptide
- 1x27 - hTK Lck SH3-SH2 domain + peptide
- 1qpj - hTK Lck kinase domain + staurosporin
- 2of2, 2of4, 2ofu, 2ofv, 2og8, 3b2w, 3bym, 3bys, 3byu, 2zm1, 2zm4, 3byo, 2zyb, 3ac1, 3ac2, 3ac3, 3ac4, 3ac5, 3ac8, 3acj, 3ack, 3kmm, 3ad4, 3ad5, 3ad6, 1qpc, 1qpd, 1qpe - hTK Lck kinase domain + inhibitor
- 3mpm - hTK Lck kinase domain (mutant) + inhibitor
- 4c3f - hTK Lck kinase domain (mutant) + chemotype
- 2pl0 - hTK Lck kinase domain + imatinib
- 3kxz - hTK Lck kinase domain + probe molecule
- 1q68 - hTK Lck residues 6-34 (mutant) + CD4 peptide – NMR
- 1q69 - hTK Lck residues 6-34 (mutant) + CD8 – NMR

Syk - spleen tyrosine kinase

- 1xba, 4xg2 – Syk kinase domain

Syk complex

- 1xbb - Syk kinase domain + Gleevec
- 1xbc - Syk kinase domain + staurosporine
- 3emg, 3fqe, 3fqh, 3fqs, 3srv, 4dfl, 4dfn, 3vf8, 3vf9, 3tub, 3tuc, 3tud, 4f4p, 4fyn, 4fyo, 4fz6, 4fz7, 4gfg, 4i0r, 4i0s, 4i0t, 4puz, 4pv0, 4rx7, 4rx8, 4rx9, 5lma, 5lmb, 5ghv, 4wnm, 4xg3, 4xg4, 4xg6, 4xg7, 4xg8, 4xg9, 4rss, 4yjv, 5c26, 5c27, 4yjo, 4yjp, 4yjq, 4yjr, 4yjs, 4yjt, 4yju - Syk kinase domain + inhibitor
- 4px6 - Syk kinase domain (mutant) + inhibitor
- 1csy, 1csz - Syk SH2 domain + phosphopeptide – NMR
- 4fl1, 4fl2 - Syk kinase domain + ANP
- 4fl3 - Syk kinase domain (mutant) + ANP
- 1a81 – Syk tandem SH2 domain + T-cell surface peptide

Itk/Tsk tyrosine kinase

- 1lui, 1luk, 1lum, 1lun – mTK Itk SH2 domain – NMR
- 3s9k – mTK Itk SH2 domain
- 2etz, 2eu0 – hTK Itk SH2 domain + phosphopeptide – NMR
- 1awj, 2rn8, 2rna – mTK Itk SH3 domain – NMR
- 2yuq, 2lmj – hTK Itk SH3 domain – NMR
- 2k79, 2k7a – mTK Itk SH2+SH3 domains – NMR
- 1sm2, 1snu, 1snx – hTK Itk kinase domain
- 3miy – hTK Itk kinase domain + cancer drug
- 3v5j, 3v5l, 3v8t, 3v8w – hTK Itk kinase domain + inhibitor
- 3mj1, 3mj2, 3qgw, 3qgy, 4hct, 4hcu, 4hcv, 4kio – hTK Itk kinase domain (mutant) + inhibitor
- 3t9t – hTK Itk kinase domain (mutant) + arthritis drug
- 2e6i – hTK Itk BTK motif – NMR
- 4l7s, 4m0y, 4m0z, 4m12, 4m13, 4m14, 4m15, 4mf0, 4mf1 - hTK Itk kinase domain + inhibitor
- 4pp9, 4ppa, 4ppb, 4ppc, 4pqn, 4qd6, 4rfm - hTK Itk kinase domain (mutant) + inhibitor

Zap tyrosine kinase

- 4k2r – hTK Zap
- 2ozo - hTK Zap (mutant)
- 1m61 - hTK Zap SH2 domain

Zap complex

- 2oq1 - hTK Zap SH2 domain + peptide
- 1u59 - hTK Zap kinase domain + staurosporine

Pyk2 tyrosine kinase or or protein-tyrosine kinase 2-β

- 3cc6, 3fzo - hTK Pyk2 kinase domain
- 3gm2 - hTK Pyk2 FAT domain
- 3gm3 - hTK Pyk2 FAT domain (mutant)
- 4eku – hTK Pyk2 FERM domain
- 2lk4 - hTK Pyk2 FAT domain – NMR

Pyk2 complex

- 3fzp - hTK Pyk2 kinase domain + ATPγS
- 3fzr, 3fzs, 3fzt, 3h3c, 3et7 - hTK Pyk2 kinase domain + inhibitor
- 3gm1, 4r32 - hTK Pyk2 FAT domain + paxillin peptide
- 4xek, 4xev, 4xef - hTK Pyk2 FAT domain + leupaxin peptide
- 4h1j - hFAK2 kinase domain + pyrazole inhibitor
- 4h1m - hFAK2 kinase domain + indole inhibitor
- 3u3c, 3u3f – hFAK2 FAT domain (mutant) + paxillin LD2 motif

CapAB tyrosine kinase

- 3bfv - SaTK CapA1/CapB2 – Staphylococcus aureus
- 2ved - SaTK CapA1/CapB2 + Mg + ADP

Fer tyrosine kinase

- 2kk6 - hTK Fer SH2 domain – NMR

Ptk6 tyrosine kinase

- 1rja - hTK Ptk6 SH2 domain – NMR
- 2kgt - hTK Ptk6 SH3 domain – NMR

Lyn tyrosine kinase (Domains: SH3 39-101; SH2 115-229; kinase 239-512)

- 4tzi - hTK Lyn SH2 domain
- 1w1f - hTK Lyn SH3 domain – NMR
- 1wa7 - hTK Lyn SH3 domain + peptide – NMR
- 3a4o - hTK Lyn residues 233-512 + staurosporine
- 2zv7 - mTK Lyn kinase domain
- 2zv8 - mTK Lyn kinase domain + AMPPNP
- 2zv9 - mTK Lyn kinase domain + PP2
- 2zva - mTK Lyn kinase domain + cancer drug

Txk tyrosine kinase

- 2dm0 - hTK Txk SH2 domain – NMR

Yes tyrosine kinase

- 2hda - hTK Yes SH3 domain

Tec tyrosine kinase

- 2lul - hTK Tec PH domain - NMR

Fes/Fps tyrosine kinase

- 1wqu, 2dcr - hTK Fes SH2 domain - NMR
- 3bkb - hTK Fes SH2+kinase domain - NMR
- 4dyl - hTK Fes F-Bar domain
- 3cbl - hTK Fes SH2+kinase domain + peptide
- 3cd3 - hTK Fes SH2+kinase domain + peptide + staurosporine
- 4e93 - hTK TFes + inhibitor

Etk tyrosine kinase

- 3cio - EcTK Etk kinase domain – Escherichia coli

Wzc tyrosine kinase

- 3la6 - EcTK Wzc kinase domain

Ros tyrosine kinase

- 3zbf - hTK Ros kinase domain + cancer drug
- 4uxl - hTK Ros kinase domain + inhibitor

Tyk tyrosine kinase (Domains: SH2+FERM 23-540; pseudokinase 541-880; kinase 880-1170)

- 3lxn, 3lxp, 3nyx, 3nz0, 4e1z, 4e20, 4gfo, 4gih, 4gii, 4gj2, 4gj3, 4py1 - hTK Tyk2 kinase domain (mutant) + inhibitor
- 4gvj - hTK Tyk2 kinase domain (mutant) + ADP
- 4oli - hTK Tyk2 pseudokinase + kinase domains
- 3zon - hTK Tyk2 pseudokinase domain
- 4wov - hTK Tyk2 pseudokinase domain + inhibitor
- 4po6 - hTK Tyk2 SH2+FERM domains + IFNAR1 peptide

Kit tyrosine kinase

- 2ec8 - hNTPK Kit extracellular domain
- 3g0e, 3g0f - hNTPK Kit kinase domain (mutant) + cancer drug
- 2e9w, 2o26 - hNTPK Kit extracellular domain + stem cell factor

Hck tyrosine kinase

- 3hck - hTK SH2 domain - NMR
- 1bu1 - hTK SH3 domain
- 4hck, 5hck - hTK SH3 domain - NMR
- 2oj2, 2oi3 - hTK SH3 domain + peptide - NMR
- 3rbb, 3rea, 3reb - hTK SH3 domain (mutant) + HIV NEF
- 3nhn - hTK SH3-SH2-linker domain
- 4u5w - hTK Hck SH3-SH2 domains + NEF
- 2c0i, 2c0o, 2c0t - hTK SH3-SH2-SH1 domain + inhibitor
- 2hk5 - hTK kinase domain + inhibitor
- 1qcf, 3vry, 3vrz, 3vs0, 3vs1, 3vs2, 3vs3, 3vs4, 3vs5, 3vs6, 3vs7 - hTK SH3-SH2-kinase-tail domain + inhibitor
- 1ad5 - hTK SH3-SH2-kinase-tail domain + AMPPNP
- 2hck - hTK SH3-SH2-kinase-tail domain + quercetin
- 4lud, 4lue - hTK Hck SH2+SH3+kinase domain (mutant) + fluorescent compound
- 4orz - hTK Hck SH3 domain (mutant) + NEF + single domain antibody

RECEPTOR TYROSINE KINASES - RTK

Bruton’s tyrosine kinase (Domains: PH 1-170; SH3 216-273; SH2 273-378; kinase 378-659)

- 2z0p - hTK Btk PH domain
- 1btk – hTK Btk PH domain (mutant)
- 3p08, 1k2p - hTK Btk kinase domain
- 1aww, 1awx, 1qly - hTK Btk SH3 domain – NMR
- 2ge9 - hTK Btk SH2 domain – NMR
- 4xi2 - hTK Btk SH3-SH2-kinase domain

Btk complex

- 1b55 - hTK Btk PH domain + inositol-tetrakisphosphate
- 1bwn - hTK Btk PH domain (mutant) + inositol-tetrakisphosphate
- 3gen, 3ocs, 3pix, 3piy, 3piz, 3pj1, 3pj2, 3pj3, 4nwm, 4yhf, 5jrs, 5fbo, 5fbn, 4rx5, 5bpy, 5bqo - hTK Btk kinase domain + inhibitor
- 3k54, 3t9t, 4ot5, 4ot6, 4otq, 4otr, 4otf, 4rfy, 4rfz, 4rg0 - hTK Btk kinase domain (mutant) + inhibitor
- 3oct - hTK Btk kinase domain (mutant) + cancer drug
- 5kup - hTK Btk residues 427-691 + inhibitor

Fms tyrosine kinase

- 2i0v - hTK Fms kinase domain

Fms complex

- 2i0y, 2i1m - hTK Fms kinase domain + inhibitor
- 3dpk - hTK Fms kinase domain (mutant) + inhibitor
- 1flt – hTK Fms Igg-like domain + VEGF
- 1qty - hTK Fms domain 2 + VEGF

Mer tyrosine kinase

- 2dbj - hTK Mer FN2 domain – NMR
- 2p0c - hTK Mer kinase domain

Mer complex

- 3brb - hTK Mer kinase domain + ADP
- 3bpr, 3tcp, 4m3q, 4mh7, 4mha - hTK Mer kinase domain + inhibitor

Bone marrow tyrosine kinase

- 2ekx - hTK Bmx SH2 domain – NMR
- 2ys2 - hTK Bmx Btk motif – NMR

Bone marrow tyrosine kinase complex

- 3sxr - hTK Bmx kinase domain (mutant) + dasatinib
- 3sxs - hTK Bmx kinase domain (mutant) + inhibitor

ErbB tyrosine kinase see Epidermal Growth Factor Receptor

Musk tyrosine kinase

- 3hkl - rTK Musk Fz-Crd domain
- 1luf, 2iep - rTK Musk cytoplasmic domain

Brk tyrosine kinase or protein-tyrosine kinase 6

- [[5da7v] - hTK Brk kinase domain
- 5da3 - hTK Brk kinase domain + inhibitor

}}

↑ Hubbard SR, Till JH. Protein tyrosine kinase structure and function. Annu Rev Biochem. 2000;69:373-98. PMID:10966463 doi:http://dx.doi.org/10.1146/annurev.biochem.69.1.373
↑ Roskoski R Jr. Src protein-tyrosine kinase structure and regulation. Biochem Biophys Res Commun. 2004 Nov 26;324(4):1155-64. PMID:15504335 doi:http://dx.doi.org/10.1016/j.bbrc.2004.09.171
↑ Tolomeo M, Dieli F, Gebbia N, Simoni D. Tyrosine kinase inhibitors for the treatment of chronic myeloid leukemia. Anticancer Agents Med Chem. 2009 Oct;9(8):853-63. PMID:19538165
↑ Lengyel E, Sawada K, Salgia R. Tyrosine kinase mutations in human cancer. Curr Mol Med. 2007 Feb;7(1):77-84. PMID:17311534
↑ Kinoshita T, Matsubara M, Ishiguro H, Okita K, Tada T. Structure of human Fyn kinase domain complexed with staurosporine. Biochem Biophys Res Commun. 2006 Aug 4;346(3):840-4. Epub 2006 Jun 13. PMID:16782058 doi:10.1016/j.bbrc.2006.05.212
↑ Tou WI, Chen CY. Traditional Chinese medicine as dual guardians against hypertension and cancer? J Biomol Struct Dyn. 2012 Jul;30(3):299-317. Epub 2012 Jun 12. PMID:22694277 doi:10.1080/07391102.2012.680030

Proteopedia Page Contributors and Editors (what is this?)

Michal Harel, Alexander Berchansky, Joel L. Sussman

Retrieved from "http://52.214.119.220/wiki/index.php/Tyrosine_kinase"

Category: Topic Page

@@ Line 57: / Line 57: @@
 *Fyn complex
-**[[1fyn]] - hTK Fyn SH3 domain + peptide<br />
+**[[1fyn]], [[4znx]] - hTK Fyn SH3 domain + peptide<br />
 **[[1nyf]], [[1nyg]] - hTK Fyn SH3 domain + peptide – NMR<br />
 **[[1efn]], [[1avz]] - hTK Fyn SH3 domain + HIV Nef protein<br />
@@ Line 72: / Line 72: @@
 **[[1ab2]] - hTK SH2 domain – NMR<BR />
-**[[3uyo]], [[3t04]], [[3k2m]] - hTK SH2 domain + monobody <br />
+**[[3uyo]], [[3t04]], [[3k2m]], [[5dc4]], [[5dc9]] - hTK SH2 domain + monobody <br />
 *Abl1 SH3 domain residues 60-121
@@ Line 101: / Line 101: @@
 **[[3ue4]], [[3cs9]], [[2hzi]], [[2hz4]], [[2hz0]], [[2hyy]], [[2gqg]], [[4wa9]] - hTK kinase domain + cancer drug<br />
 **[[2f4j]], [[4twp]] - hTK kinase domain (mutant) + cancer drug<br />
-**[[3qrk]], [[3qri]], [[3qrj]], [[2v7a]], [[2e2b]], [[2hiw]] - hTK kinase domain + inhibitor<br />
+**[[3qrk]], [[3qri]], [[3qrj]], [[2v7a]], [[2e2b]], [[2hiw]], [[4zog]], [[5hu9]], [[4yc8]] - hTK kinase domain + inhibitor<br />
 **[[1fpu]], [[1m52]], [[2qoh]], [[3kf4]], [[3kfa]] - mTK kinase domain + inhibitor<br />
 **[[2z60]], [[3dk3]], [[3dk6]], [[3dk7]] - mTK kinase domain (mutant) + inhibitor<br />
@@ Line 185: / Line 185: @@
 **[[1srl]], [[1srm]] - cTK – NMR<br />
 **[[3fj5]], [[4jz3]], [[4jz4]] - cTK<br />
-**[[4le9]], [[4oml]], [[4omm]], [[4omn]], [[4omo]], [[4omp]], [[4omq]] - cTK (mutant) <br />
+**[[4le9]], [[4oml]], [[4omm]], [[4omn]], [[4omo]], [[4omp]], [[4omq]], [[5i11]], [[4rtu]], [[4rtx]] - cTK (mutant) <br />
-**[[4hxj]], [[1prl]], [[4qt7]] - cTK + peptide<br />
+**[[4y92]] - TK (mutant) Avian sarcoma virus<br />
+**[[4hxj]], [[1prl]], [[4qt7]], [[4rty]], [[4rtz]] - cTK + peptide<br />
 **[[1prm]], [[1rlp]], [[1rlq]], [[1nlo]], [[1nlp]] - cTK + peptide - NMR<br />
-**[[4hvu]], [[4hvv]], [[4hvw]] - cTK (mutant) + peptide<br />
+**[[4hvu]], [[4hvv]], [[4hvw]], [[4rtv]], [[4rtw]] - cTK (mutant) + peptide<br />
 **[[1jeg]] – TK + protein-tyrosine phosphatase peptide – mouse<br />
@@ Line 197: / Line 198: @@
 **[[1yoj]] - hTK (mutant) <br />
 **[[3tz7]], [[3tz8]], [[3tz9]], [[4dgg]] – cTK (mutant) + pyrazolin derivative<br />
-**[[4fic]], [[3uqg]], [[3uqf]], [[3u51]], [[3u4w]], [[4agw]], [[3qlg]], [[3qlf]], [[3g6g]], [[3el8]], [[3f6x]], [[2hwo]], [[2hwp]], [[2oiq]], [[3en4]], [[3en5]], [[3en6]], [[3en7]], [[3el7]] – cTK + inhibitor<br />
+**[[4fic]], [[3uqg]], [[3uqf]], [[3u51]], [[3u4w]], [[4agw]], [[3qlg]], [[3qlf]], [[3g6g]], [[3el8]], [[3f6x]], [[2hwo]], [[2hwp]], [[2oiq]], [[3en4]], [[3en5]], [[3en6]], [[3en7]], [[3el7]], [[5bmm]], [[5j5s]], [[4ybj]], [[4ybk]] – cTK + inhibitor<br />
 **[[4lgg]], [[4lgh]], [[3svv]], [[3oez]], [[3lok]], [[3g5d]], [[3f3w]], [[3f3v]], [[3geq]], [[3g6h]], [[3f3t]], [[3f3u]], [[2qlq]], [[2qq7]], [[4lgg]], [[4lgh]], [[4mcv]], [[4o2p]] – cTK (mutant) + inhibitor<br />
 **[[4u5j]] – cTK (mutant) + cancer drug<br />
@@ Line 255: / Line 256: @@
 *'''Syk - spleen tyrosine kinase'''
-**[[1xba]] – Syk kinase domain
+**[[1xba]], [[4xg2]] – Syk kinase domain
 *Syk complex
@@ Line 261: / Line 262: @@
 **[[1xbb]] - Syk kinase domain + Gleevec<br />
 **[[1xbc]] - Syk kinase domain + staurosporine<br />
-**[[3emg]], [[3fqe]], [[3fqh]], [[3fqs]], [[3srv]], [[4dfl]], [[4dfn]], [[3vf8]], [[3vf9]], [[3tub]], [[3tuc]], [[3tud]], [[4f4p]], [[4fyn]], [[4fyo]], [[4fz6]], [[4fz7]], [[4gfg]], [[4i0r]], [[4i0s]], [[4i0t]], [[4puz]], [[4pv0]], [[4rx7]], [[4rx8]], [[4rx9]] - Syk kinase domain + inhibitor<br />
+**[[3emg]], [[3fqe]], [[3fqh]], [[3fqs]], [[3srv]], [[4dfl]], [[4dfn]], [[3vf8]], [[3vf9]], [[3tub]], [[3tuc]], [[3tud]], [[4f4p]], [[4fyn]], [[4fyo]], [[4fz6]], [[4fz7]], [[4gfg]], [[4i0r]], [[4i0s]], [[4i0t]], [[4puz]], [[4pv0]], [[4rx7]], [[4rx8]], [[4rx9]], [[5lma]], [[5lmb]], [[5ghv]], [[4wnm]], [[4xg3]], [[4xg4]], [[4xg6]], [[4xg7]], [[4xg8]], [[4xg9]], [[4rss]], [[4yjv]], [[5c26]], [[5c27]], [[4yjo]], [[4yjp]], [[4yjq]], [[4yjr]], [[4yjs]], [[4yjt]], [[4yju]] - Syk kinase domain + inhibitor<br />
 **[[4px6]] - Syk kinase domain (mutant) + inhibitor<br />
 **[[1csy]], [[1csz]] - Syk SH2 domain + phosphopeptide – NMR<BR />
@@ Line 296: / Line 297: @@
 **[[1u59]] - hTK Zap kinase domain + staurosporine
-*'''Pyk2 tyrosine kinase'''
+*'''Pyk2 tyrosine kinase or or protein-tyrosine kinase 2-β'''
 **[[3cc6]], [[3fzo]] - hTK Pyk2 kinase domain <br />
@@ Line 308: / Line 309: @@
 **[[3fzp]] - hTK Pyk2 kinase domain + ATPγS<br />
 **[[3fzr]], [[3fzs]], [[3fzt]], [[3h3c]], [[3et7]] - hTK Pyk2 kinase domain + inhibitor<br />
-**[[3gm1]] - hTK Pyk2 FAT domain + paxillin peptide<br />
+**[[3gm1]], [[4r32]] - hTK Pyk2 FAT domain + paxillin peptide<br />
+**[[4xek]], [[4xev]], [[4xef]] - hTK Pyk2 FAT domain + leupaxin peptide<br />
 **[[4h1j]] - hFAK2 kinase domain + pyrazole inhibitor<br />
 **[[4h1m]] - hFAK2 kinase domain + indole inhibitor<br />
@@ Line 419: / Line 421: @@
 **[[1b55]] - hTK Btk PH domain + inositol-tetrakisphosphate<br />
 **[[1bwn]] - hTK Btk PH domain (mutant) + inositol-tetrakisphosphate<br />
-**[[3gen]], [[3ocs]], [[3pix]], [[3piy]], [[3piz]], [[3pj1]], [[3pj2]], [[3pj3]], [[4nwm]], [[4yhf]] - hTK Btk kinase domain + inhibitor<br />
+**[[3gen]], [[3ocs]], [[3pix]], [[3piy]], [[3piz]], [[3pj1]], [[3pj2]], [[3pj3]], [[4nwm]], [[4yhf]], [[5jrs]], [[5fbo]], [[5fbn]], [[4rx5]], [[5bpy]], [[5bqo]]  - hTK Btk kinase domain + inhibitor<br />
 **[[3k54]], [[3t9t]], [[4ot5]], [[4ot6]], [[4otq]], [[4otr]], [[4otf]], [[4rfy]], [[4rfz]], [[4rg0]] - hTK Btk kinase domain (mutant) + inhibitor<br />
 **[[3oct]] - hTK Btk kinase domain (mutant) + cancer drug<br />
+**[[5kup]] - hTK Btk residues 427-691 + inhibitor<br />
 *'''Fms tyrosine kinase'''
@@ Line 460: / Line 463: @@
 **[[3hkl]] - rTK Musk Fz-Crd domain <br />
 **[[1luf]], [[2iep]] - rTK Musk cytoplasmic domain <br />
+*Brk tyrosine kinase or protein-tyrosine kinase 6
+**[[5da7v] - hTK Brk kinase domain <br />
+**[[5da3]] - hTK Brk kinase domain + inhibitor<br />
 }}
 <references/>
 [[Category:Topic Page]]

Tyrosine kinase

From Proteopedia

Revision as of 09:48, 27 November 2016

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Traditional Chinese medicine as dual guardians against hypertension and cancer? ^[6]

3D structures of tyrosine kinase

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Tyrosine kinase

From Proteopedia

Revision as of 09:48, 27 November 2016

Contents

Function

Relevance

Disease

Structural highlights

Traditional Chinese medicine as dual guardians against hypertension and cancer? [6]

3D structures of tyrosine kinase

Proteopedia Page Contributors and Editors (what is this?)

Views

Personal tools

Navigation

Search

Toolbox

Traditional Chinese medicine as dual guardians against hypertension and cancer? ^[6]