Did you know ? If you order before Friday 14h we deliver 90PCT of the the time next Tuesday, GENTAUR another in time delivery

Pubmed ID :20007378
Publication Date : //

Structural analysis of the catalytically inactive kinase domain of the human EGF receptor 3.


The kinase domain of human epidermal growth factor receptor (HER) 3/ErbB3, a member of the EGF receptor (EGFR) family, lacks several residues that are critical for catalysis. Because catalytic activity in EGFR family members is switched on by an allosteric interaction between kinase domains in an asymmetric kinase domain dimer, HER3 might be specialized to serve as an activator of other EGFR family members. We have determined the crystal structure of the HER3 kinase domain and show that it appears to be locked into an inactive conformation that resembles that of EGFR and HER4. Although the crystal structure shows that the HER3 kinase domain binds ATP, we confirm that it is catalytically inactive but can serve as an activator of the EGFR kinase domain. The HER3 kinase domain forms a dimer in the crystal, mediated by hydrophobic contacts between the N-terminal lobes of the kinase domains. This N-lobe dimer closely resembles a dimer formed by inactive HER4 kinase domains in crystal structures determined previously, and molecular dynamics simulations suggest that the HER3 and HER4 N-lobe dimers are stable. The kinase domains of HER3 and HER4 form similar chains in their respective crystal lattices, in which N-lobe dimers are linked together by reciprocal exchange of C-terminal tails. The conservation of this tiling pattern in HER3 and HER4, which is the closest evolutionary homolog of HER3, might represent a general mechanism by which this branch of the HER receptors restricts ligand-independent formation of active heterodimers with other members of the EGFR family.

Authors : Jura Natalia , Shan Yibing , Cao Xiaoxian , Shaw David E , Kuriyan John ,

Related products :

Catalog number Product name Quantity
orb80846 Human Phosphoinositide 3-kinase p110g inactive mutant protein The PI3KdD946A protein is catalytically inactive mutant of PI3Kd with D946A mutation in the ATP binding site. This recombinant catalytical 1
31-052 AKT1 is a general protein kinase capable of phosphorylating several known proteins.The serine-threonine protein kinase encoded by the AKT1 gene is catalytically inactive in serum-starved primary and i 0.05 mg
EIAAB31464 Homo sapiens,Human,Inactive phospholipase C-like protein 1,Phospholipase C-deleted in lung carcinoma,Phospholipase C-related but catalytically inactive protein,PLCL1,PLC-L1,PRIP
EIAAB31463 Inactive phospholipase C-like protein 1,p130,Phospholipase C-related but catalytically inactive protein,Plcl1,PLC-L1,PRIP1,Rat,Rattus norvegicus
EIAAB31465 Inactive phospholipase C-like protein 1,Mouse,Mus musculus,Phospholipase C-related but catalytically inactive protein,Plcl1,PLC-L1,PRIP
E0148h ELISA Fetal liver kinase 1,FLK1,FLK-1,Homo sapiens,Human,KDR,Kinase insert domain receptor,Protein-tyrosine kinase receptor flk-1,Vascular endothelial growth factor receptor 2,VEGFR-2 96T
E0148h ELISA kit Fetal liver kinase 1,FLK1,FLK-1,Homo sapiens,Human,KDR,Kinase insert domain receptor,Protein-tyrosine kinase receptor flk-1,Vascular endothelial growth factor receptor 2,VEGFR-2 96T
U0148h CLIA Fetal liver kinase 1,FLK1,FLK-1,Homo sapiens,Human,KDR,Kinase insert domain receptor,Protein-tyrosine kinase receptor flk-1,Vascular endothelial growth factor receptor 2,VEGFR-2 96T
EIAAB33008 CCK4,CCK-4,Colon carcinoma kinase 4,Homo sapiens,Human,Inactive tyrosine-protein kinase 7,Protein-tyrosine kinase 7,Pseudo tyrosine kinase receptor 7,PTK7,Tyrosine-protein kinase-like 7
EIAAB10738 CD167 antigen-like family member B,DDR2,Discoidin domain receptor 2,Discoidin domain-containing receptor 2,Discoidin domain-containing receptor tyrosine kinase 2,Homo sapiens,Human,Neurotrophic tyrosi
EIAAB31494 Homo sapiens,Human,Inactive choline phosphatase 5,Inactive phosphatidylcholine-hydrolyzing phospholipase D5,Inactive phospholipase D5,Inactive PLD 5,PLD5,PLDc
10-663-45537 ERK2_MAPK1 (p42 MAP Kinase) - Inactive Enzyme Human - EC 2.7.11.24; Extracellular signal-regulated kinase 2; ERK-2; Mitogen-activated protein kinase 2; MAP kinase 2; MAPK 2; p42-MAPK; ERT1 N_A 0.02 mg
10-663-45537 ERK2_MAPK1 (p42 MAP Kinase) - Inactive Enzyme Human - EC 2.7.11.24; Extracellular signal-regulated kinase 2; ERK-2; Mitogen-activated protein kinase 2; MAP kinase 2; MAPK 2; p42-MAPK; ERT1 N_A 0.003 mg
10-663-45537 ERK2_MAPK1 (p42 MAP Kinase) - Inactive Enzyme Human - EC 2.7.11.24; Extracellular signal-regulated kinase 2; ERK-2; Mitogen-activated protein kinase 2; MAP kinase 2; MAPK 2; p42-MAPK; ERT1 N_A 0.01 mg
EIAAB10735 Cak,CD167 antigen-like family member A,Cell adhesion kinase,Ddr1,Discoidin receptor tyrosine kinase,Eddr1,Epithelial discoidin domain receptor 1,Epithelial discoidin domain-containing receptor 1,Mouse
EIAAB10736 CAK,CD167 antigen-like family member A,Cell adhesion kinase,DDR1,Discoidin receptor tyrosine kinase,EDDR1,Epithelial discoidin domain receptor 1,Epithelial discoidin domain-containing receptor 1,HGK2,
EIAAB10737 CD167 antigen-like family member A,Cell adhesion kinase,Ddr1,Discoidin receptor tyrosine kinase,Eddr1,Epithelial discoidin domain receptor 1,Epithelial discoidin domain-containing receptor 1,Protein-t
15-288-21181 Vascular endothelial growth factor receptor 2 - EC 2.7.10.1; VEGFR-2; Kinase insert domain receptor; Protein-tyrosine kinase receptor Flk-1; CD309 antigen Polyclonal 0.1 mg
15-288-21181 Vascular endothelial growth factor receptor 2 - EC 2.7.10.1; VEGFR-2; Kinase insert domain receptor; Protein-tyrosine kinase receptor Flk-1; CD309 antigen Polyclonal 0.05 mg
EIAAB10739 CD167 antigen-like family member B,Ddr2,Discoidin domain receptor 2,Discoidin domain-containing receptor 2,Mouse,Mus musculus,Neurotrophic tyrosine kinase, receptor-related 3,Ntrkr3,Receptor protein-t
EIAAB31493 Inactive choline phosphatase 5,Inactive phosphatidylcholine-hydrolyzing phospholipase D5,Inactive phospholipase D5,Inactive PLD 5,Mouse,Mus musculus,Pld5
10-782-55028 Discoidin domain-containing receptor 2 - EC 2.7.10.1; Discoidin domain receptor 2; Receptor protein-tyrosine kinase TKT; Tyrosine-protein kinase TYRO 10; Neurotrophic tyrosine kinase. receptor-related 0.02 mg
10-782-55028 Discoidin domain-containing receptor 2 - EC 2.7.10.1; Discoidin domain receptor 2; Receptor protein-tyrosine kinase TKT; Tyrosine-protein kinase TYRO 10; Neurotrophic tyrosine kinase. receptor-related 0.01 mg
10-782-55028 Discoidin domain-containing receptor 2 - EC 2.7.10.1; Discoidin domain receptor 2; Receptor protein-tyrosine kinase TKT; Tyrosine-protein kinase TYRO 10; Neurotrophic tyrosine kinase. receptor-related 0.005 mg
10-782-55028 Discoidin domain-containing receptor 2 - EC 2.7.10.1; Discoidin domain receptor 2; Receptor protein-tyrosine kinase TKT; Tyrosine-protein kinase TYRO 10; Neurotrophic tyrosine kinase. receptor-related 0.001 mg


 

GENTAUR Belgium BVBA BE0473327336
Voortstraat 49, 1910 Kampenhout BELGIUM
Tel 0032 16 58 90 45

Fax 0032 16 50 90 45
info@gentaur.com | Gentaur





GENTAUR Ltd.
Howard Frank Turnberry House
1404-1410 High Road
Whetstone London N20 9BH
Tel 020 3393 8531 Fax 020 8445 9411
uk@gentaur.com | Gentaur

 

 




GENTAUR France SARL
9, rue Lagrange, 75005 Paris
Tel 01 43 25 01 50

Fax 01 43 25 01 60
RCS Paris B 484 237 888

SIRET 48423788800017

BNP PARIBAS PARIS PL MAUBERT BIC BNPAFRPPPRG

france@gentaur.com | Gentaur

GENTAUR GmbH
Marienbongard 20
52062 Aachen Deutschland
Support Karolina Elandt
Tel: 0035929830070
Fax: (+49) 241 56 00 47 88

Logistic :0241 40 08 90 86
Bankleitzahl 39050000
IBAN lautet DE8839050000107569353
Handelsregister Aachen HR B 16058
Umsatzsteuer-Identifikationsnummer *** DE 815175831
Steuernummer 201/5961/3925
de@gentaur.com | Gentaur

GENTAUR U.S.A
Genprice Inc, Logistics
547, Yurok Circle
San Jose, CA 95123
CA 95123
Tel (408) 780-0908,
Fax (408) 780-0908,
sales@genprice.com

Genprice Inc, Invoices and accounting
6017 Snell Ave, Ste 357
San Jose, CA 95123




GENTAUR Nederland BV
NL850396268B01 KVK nummer 52327027
Kuiper 1
5521 DG Eersel Nederland
Tel:  0208-080893  Fax: 0497-517897
nl@gentaur.com | Gentaur
IBAN: NL04 RABO 0156 9854 62   SWIFT RABONL2U






GENTAUR Spain
tel:0911876558
spain@gentaur.com | Gentaur






ГЕНТАУЪР БЪЛГАРИЯ
ID # 201 358 931 /BULSTAT
София 1000, ул. "Граф Игнатиев" 53 вх. В, ет. 2
Tel 0035924682280 Fax 0035924808322
e-mail: Sofia@gentaur.com | Gentaur
IBAN: BG11FINV91501014771636
BIC: FINVBGSF

GENTAUR Poland Sp. z o.o.


ul. Grunwaldzka 88/A m.2
81-771 Sopot, Poland
TEL Gdansk 058 710 33 44 FAX  058 710 33 48              

poland@gentaur.com | Gentaur

Other countries

Österreich +43720880899

Canada Montreal +15149077481

Ceská republika Praha +420246019719

Danmark +4569918806

Finland Helsset +358942419041

Magyarország Budapest +3619980547

Ireland Dublin+35316526556

Luxembourg+35220880274

Norge Oslo+4721031366

Sverige Stockholm+46852503438

Schweiz Züri+41435006251

US New York+17185132983

GENTAUR Italy
SRL IVA IT03841300167
Piazza Giacomo Matteotti, 6
24122 Bergamo Tel 02 36 00 65 93
Fax 02 36 00 65 94
italia@gentaur.com | Gentaur