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 :10633045
Publication Date : //

Binding mode of the 4-anilinoquinazoline class of protein kinase inhibitor: X-ray crystallographic studies of 4-anilinoquinazolines bound to cyclin-dependent kinase 2 and p38 kinase.


4-Anilinoquinazolines represent an important class of protein kinase inhibitor. Modes of binding for two members of this inhibitor class were determined by X-ray crystallographic analysis of one inhibitor (4-[3-hydroxyanilino]-6,7-dimethoxyquinazoline) in complex with cyclin-dependent kinase 2 (CDK2) and the other (4-[3-methylsulfanylanilino]-6,7-dimethoxyquinazoline) in complex with p38 kinase. In both inhibitor/kinase structures, the 4-anilinoquinazoline was bound in the ATP site with the quinazoline ring system oriented along the peptide strand that links the two domains of the protein and with the anilino substituent projecting into a hydrophobic pocket within the protein interior. In each case, the nitrogen at position-1 of the quinazoline accepted a hydrogen bond from a backbone NH (CDK2, Leu-83; p38, Met-109) of the domain connector strand, and aromatic hydrogen atoms at C2 and C8 interacted with backbone carbonyl oxygen atoms of the peptide strand. The anilino group of the CDK2-bound compound was essentially coplanar with the quinazoline ring system and occupied a pocket between Lys-33 and Phe-80. For the p38-bound inhibitor, the anilino group was angled out of plane and was positioned between Lys-53 and Thr-106 in a manner similar to that observed for the aryl substituent of the pyridinylimidazole class of inhibitor.

Authors : Shewchuk L , Hassell A , Wisely B , Rocque W , Holmes W , Veal J , Kuyper L F ,

Related products :

Catalog number Product name Quantity
EIAAB06559 CDI1,CDK2-associated dual-specificity phosphatase,CDKN3,CIP2,Cyclin-dependent kinase inhibitor 3,Cyclin-dependent kinase interactor 1,Cyclin-dependent kinase-interacting protein 2,Homo sapiens,Human,K
EIAAB06524 CAK-kinase p42,CCRK,CDCH,CDK20,CDK-activating kinase p42,Cell cycle-related kinase,Cell division protein kinase 20,Cyclin-dependent kinase 20,Cyclin-dependent protein kinase H,Cyclin-kinase-activating
EIAAB06523 CAK-kinase p42,Ccrk,Cdch,Cdk20,CDK-activating kinase p42,CDK-related protein kinase PNQLARE,Cell cycle-related kinase,Cell division protein kinase 20,Cyclin-dependent kinase 20,Cyclin-dependent protei
EIAAB06522 CDC2L6,CDC2-related protein kinase 6,CDK11,CDK19,Cell division cycle 2-like protein kinase 6,Cell division protein kinase 19,Cyclin-dependent kinase 11,Cyclin-dependent kinase 19,Death-preventing kina
15-288-21185 Cyclin-dependent kinase inhibitor 2A. isoforms 1_2_3 - Cyclin-dependent kinase 4 inhibitor A; CDK4I; p16-INK4; p16-INK4a; Multiple tumor suppressor 1; MTS1 Polyclonal 0.05 mg
15-288-21185 Cyclin-dependent kinase inhibitor 2A. isoforms 1_2_3 - Cyclin-dependent kinase 4 inhibitor A; CDK4I; p16-INK4; p16-INK4a; Multiple tumor suppressor 1; MTS1 Polyclonal 0.1 mg
E0794r ELISA CDK4I,Cdkn2a,Cyclin-dependent kinase 4 inhibitor A,Cyclin-dependent kinase inhibitor 2A, isoform 1,p16,p16-INK4,P16ink4a,p16-INK4a,Rat,Rattus norvegicus 96T
U0794r CLIA CDK4I,Cdkn2a,Cyclin-dependent kinase 4 inhibitor A,Cyclin-dependent kinase inhibitor 2A, isoform 1,p16,p16-INK4,P16ink4a,p16-INK4a,Rat,Rattus norvegicus 96T
E0794r ELISA kit CDK4I,Cdkn2a,Cyclin-dependent kinase 4 inhibitor A,Cyclin-dependent kinase inhibitor 2A, isoform 1,p16,p16-INK4,P16ink4a,p16-INK4a,Rat,Rattus norvegicus 96T
E0794m ELISA kit CDK4I,Cdkn2a,Cyclin-dependent kinase 4 inhibitor A,Cyclin-dependent kinase inhibitor 2A, isoforms 1_2,Mouse,Mus musculus,p16-INK4,P16ink4a,p16-INK4a 96T
E0794m ELISA CDK4I,Cdkn2a,Cyclin-dependent kinase 4 inhibitor A,Cyclin-dependent kinase inhibitor 2A, isoforms 1_2,Mouse,Mus musculus,p16-INK4,P16ink4a,p16-INK4a 96T
U0794m CLIA CDK4I,Cdkn2a,Cyclin-dependent kinase 4 inhibitor A,Cyclin-dependent kinase inhibitor 2A, isoforms 1_2,Mouse,Mus musculus,p16-INK4,P16ink4a,p16-INK4a 96T
U1943h CLIA CDKN2C,CDKN6,Cyclin-dependent kinase 4 inhibitor C,Cyclin-dependent kinase 6 inhibitor,Homo sapiens,Human,p18-INK4c,p18-INK6 96T
U1943h CLIA kit CDKN2C,CDKN6,Cyclin-dependent kinase 4 inhibitor C,Cyclin-dependent kinase 6 inhibitor,Homo sapiens,Human,p18-INK4c,p18-INK6 96T
E1943h ELISA CDKN2C,CDKN6,Cyclin-dependent kinase 4 inhibitor C,Cyclin-dependent kinase 6 inhibitor,Homo sapiens,Human,p18-INK4c,p18-INK6 96T
E1943h ELISA kit CDKN2C,CDKN6,Cyclin-dependent kinase 4 inhibitor C,Cyclin-dependent kinase 6 inhibitor,Homo sapiens,Human,p18-INK4c,p18-INK6 96T
E0794h ELISA kit CDK4I,CDKN2,CDKN2A,Cyclin-dependent kinase 4 inhibitor A,Cyclin-dependent kinase inhibitor 2A, isoforms 1_2_3,Homo sapiens,Human,MTS1,MTS-1,Multiple tumor suppressor 1,p16-INK4,p16INK4A,p16 96T
U0794h CLIA CDK4I,CDKN2,CDKN2A,Cyclin-dependent kinase 4 inhibitor A,Cyclin-dependent kinase inhibitor 2A, isoforms 1_2_3,Homo sapiens,Human,MTS1,MTS-1,Multiple tumor suppressor 1,p16-INK4,p16INK4A,p16-INK4a 96T
E1943m ELISA Cdkn2c,Cyclin-dependent kinase 4 inhibitor C,Cyclin-dependent kinase 6 inhibitor,Mouse,Mus musculus,p18-INK4c,p18-INK6 96T
U1943m CLIA kit Cdkn2c,Cyclin-dependent kinase 4 inhibitor C,Cyclin-dependent kinase 6 inhibitor,Mouse,Mus musculus,p18-INK4c,p18-INK6 96T
E1943m ELISA kit Cdkn2c,Cyclin-dependent kinase 4 inhibitor C,Cyclin-dependent kinase 6 inhibitor,Mouse,Mus musculus,p18-INK4c,p18-INK6 96T
U1943m CLIA Cdkn2c,Cyclin-dependent kinase 4 inhibitor C,Cyclin-dependent kinase 6 inhibitor,Mouse,Mus musculus,p18-INK4c,p18-INK6 96T
EIAAB06568 CDKN1C,Cyclin-dependent kinase inhibitor 1C,Cyclin-dependent kinase inhibitor p57,Homo sapiens,Human,KIP2,p57Kip2
EIAAB06565 CDKN1B,Cyclin-dependent kinase inhibitor 1B,Cyclin-dependent kinase inhibitor p27,Homo sapiens,Human,KIP1,p27Kip1
EIAAB06567 Cdkn1c,Cyclin-dependent kinase inhibitor 1C,Cyclin-dependent kinase inhibitor p57,Kip2,Mouse,Mus musculus,p57Kip2


 

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





GENTAUR Ltd.
Unicorn House, Station Cl
Hertfordshire, Potters Bar EN6 1TL
Whetstone London N20 9BH
Tel 020 3393 8531 Fax 020 8445 9411
uk@gentaur.com | Gentaur | 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
RIB 30004 00187 00010092253 10
BNP PARIBAS PARIS PL MAUBERT BIC BNPAFRPPPRG
IBAN FR76 3000 4001 8700 0100 9225 310
france@gentaur.com | Gentaur | Gentaur

GENTAUR GmbH
Marienbongard 20
52062 Aachen Deutschland
Support Karolina Elandt
Tel: +49 0241 40 08 90 86, +49 0241 95 78 94 78, +49 0241 40 08 90 86
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

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 | Gentaur
IBAN: NL04 RABO 0156 9854 62   SWIFT RABONL2U






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