1T46: PDB entry 1T46

Structural basis for the autoinhibition and sti-571 inhibition of C-kit tyrosine kinase. Determined by X-ray diffraction at 1.6 Å resolution. Released 15 Jun 2004.

Method: X-ray diffraction
Resolution: 1.6 Å
Organism: Homo sapiens
Chains: 1
Atoms: 2,696
Mol. weight: 36.07 kDa
Ligands: PO4, STI
Released: 15 Jun 2004

Explore 1T46 in 3D Show helices and sheets RCSB PDB PDBe

Secondary structure: helices and β-sheets

1T46 contains 19 α-helices and 12 β-strands across 1 chain. Residue ranges use author residue numbering, as in the PDB file, from PDBe. To see them in 3D, choose the Cartoon representation with Secondary structure coloring: helices, sheets and coils get different colors.

Chain A: 19 helices, 12 β-strands

Element	Residues	Length	Sheet
α-helix	577-578	2
α-helix	580-582	3
β-strand	583	1	1
α-helix	586-588	3
β-strand	589-597	9	1
β-strand	601-609	9	1
β-strand	617-625	9	1
α-helix	631-647	17
β-strand	653	1	2
α-helix	654-655	2
β-strand	656-660	5	1
β-strand	667-671	5	1
β-strand	676-677	2	2
α-helix	678-684	7
α-helix	766-785	20
α-helix	795-797	3
β-strand	798-801	4	2
β-strand	805-808	4	2
α-helix	812-814	3
β-strand	824-825	2	3
β-strand	830-831	2	3
α-helix	833-835	3
α-helix	838-843	6
α-helix	848-863	16
α-helix	867-868	2
α-helix	877-885	9
α-helix	889-892	4
α-helix	897-906	10
α-helix	911-913	3
α-helix	915-916	2
α-helix	917-930	14

Molecules and chains

Molecule	Chains	Type	Length	Organism	UniProt
Homo sapiens v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog	A	protein	313	Homo sapiens	P10721 (AlphaFold model)

Sequence of entity 1 (A), FASTA

>1T46_1 Homo sapiens v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog (chains A)
GNNYVYIDPTQLPYDHKWEFPRNRLSFGKTLGAGAFGKVVEATAYGLIKSDAAMTVAVKM
LKPSAHLTEREALMSELKVLSYLGNHMNIVNLLGACTIGGPTLVITEYCCYGDLLNFLRR
KRDSFICSKTSPAIMEDDELALDLEDLLSFSYQVAKGMAFLASKNCIHRDLAARNILLTH
GRITKICDFGLARDIKNDSNYVVKGNARLPVKWMAPESIFNCVYTFESDVWSYGIFLWEL
FSLGSSPYPGMPVDSKFYKMIKEGFRMLSPEHAPAEMYDIMKTCWDADPLKRPTFKQIVQ
LIEKQISESTNHI

Ligands and cofactors

ID	Name	Formula	Copies
PO4	Phosphate ion	O4 P	2
STI	4-(4-methyl-piperazin-1-ylmethyl)-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-yla…	C29 H31 N7 O	1

Primary citation

Structural basis for the autoinhibition and STI-571 inhibition of c-Kit tyrosine kinase. Mol, C.D., Dougan, D.R., Schneider, T.R. et al. J Biol Chem (2004) 279:31655-31663. DOI 10.1074/jbc.M403319200 · PubMed

Other PDB entries of the same protein (UniProt P10721 (AlphaFold model), which also has an AlphaFold model), best resolution first:

2VIF 1.45 Å, Crystal structure of SOCS6 SH2 domain in complex with a c-KIT phosphopeptide
8PQD 1.5 Å, c-KIT kinase domain in complex with avapritinib derivative 10
8S14 1.5 Å, c-KIT kinase domain in complex with sunitinib
3G0E 1.6 Å, KIT kinase domain in complex with sunitinib
8PQA 1.65 Å, c-KIT kinase domain in complex with avapritinib derivative 4
9TFD 1.65 Å, KIT kinase domain in complex with a pyrrolotriazine-based compound (11)
8PQ9 1.7 Å, c-KIT kinase domain in complex with avapritinib
9TFE 1.7 Å, KIT kinase domain in complex with an aminopyrimidine-based compound (15)
9TFG 1.7 Å, KIT kinase domain in complex with a 6-,7-dimethoxyquinoline-based compound (19)
9TFH 1.7 Å, KIT kinase domain in complex with a 7-methylquinazoline-based compound (25)
9TFK 1.7 Å, KIT kinase domain in complex with a quinoline-3-carbonitrile-based compound (38)
9TFJ 1.75 Å, KIT kinase domain in complex with a 6,7-dimethoxyquinazoline-based compound (34)

Browse more

1T46 is part of these collections:

Kinases and cancer drug targets

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