| Target
Information |
| Name | Angiopoietin 1 receptor |
| Type of target | Discontinued target |
| Synonyms | CD202b antigen |
| Endothelial Cell-Specific Receptor TIE-2 |
| P140 TEK |
| Tunica interna endothelial cell kinase |
| Tyrosine-protein kinase receptor TEK |
| Tyrosine-protein kinase receptor TIE-2 |
| Disease | Tumors
[ICD9: 140-199, 210-229 ICD10: C00-C75, C7A, C7B, D10-D36, D3A] | [1] |
| Drug(s) | CEP-7055 |  | Discontinued in Phase I | Pancreastic cancer, prostate cancer & solid tumours | [2] |
| BioChemical Class | Transferases transferring phosphorus-containing groups |
| EC Number | EC 2.7.1.112 |
| UniProt ID | Q02763 |
| PDB Structure | 1FVR; 2GY5; 2GY7; 2OO8; 2OSC; 2P4I; 2WQB; 3BEA; 3L8P; 4K0V. |
| Function | This protein is a protein tyrosine-kinase transmembrane receptor for angiopoietin 1. It may constitute the earliest mammalian endothelial cell lineage marker. Probably regulates endothelial cell proliferation, differentiation and guides the proper pattern. |
| Sequence | MDSLASLVLCGVSLLLSGTVEGAMDLILINSLPLVSDAETSLTCIASGWRPHEPITIGRD
FEALMNQHQDPLEVTQDVTREWAKKVVWKREKASKINGAYFCEGRVRGEAIRIRTMKMRQ
QASFLPATLTMTVDKGDNVNISFKKVLIKEEDAVIYKNGSFIHSVPRHEVPDILEVHLPH
AQPQDAGVYSARYIGGNLFTSAFTRLIVRRCEAQKWGPECNHLCTACMNNGVCHEDTGEC
ICPPGFMGRTCEKACELHTFGRTCKERCSGQEGCKSYVFCLPDPYGCSCATGWKGLQCNE
ACHPGFYGPDCKLRCSCNNGEMCDRFQGCLCSPGWQGLQCEREGIQRMTPKIVDLPDHIE
VNSGKFNPICKASGWPLPTNEEMTLVKPDGTVLHPKDFNHTDHFSVAIFTIHRILPPDSG
VWVCSVNTVAGMVEKPFNISVKVLPKPLNAPNVIDTGHNFAVINISSEPYFGDGPIKSKK
LLYKPVNHYEAWQHIQVTNEIVTLNYLEPRTEYELCVQLVRRGEGGEGHPGPVRRFTTAS
IGLPPPRGLNLLPKSQTTLNLTWQPIFPSSEDDFYVEVERRSVQKSDQQNIKVPGNLTSV
LLNNLHPREQYVVRARVNTKAQGEWSEDLTAWTLSDILPPQPENIKISNITHSSAVISWT
ILDGYSISSITIRYKVQGKNEDQHVDVKIKNATITQYQLKGLEPETAYQVDIFAENNIGS
SNPAFSHELVTLPESQAPADLGGGKMLLIAILGSAGMTCLTVLLAFLIILQLKRANVQRR
MAQAFQNVREEPAVQFNSGTLALNRKVKNNPDPTIYPVLDWNDIKFQDVIGEGNFGQVLK
ARIKKDGLRMDAAIKRMKEYASKDDHRDFAGELEVLCKLGHHPNIINLLGACEHRGYLYL
AIEYAPHGNLLDFLRKSRVLETDPAFAIANSTASTLSSQQLLHFAADVARGMDYLSQKQF
IHRDLAARNILVGENYVAKIADFGLSRGQEVYVKKTMGRLPVRWMAIESLNYSVYTTNSD
VWSYGVLLWEIVSLGGTPYCGMTCAELYEKLPQGYRLEKPLNCDDEVYDLMRQCWREKPY
ERPSFAQILVSLNRMLEERKTYVNTTLYEKFTYAGIDCSAEEAA
|
| Related US Patent | 6,413,932 |
| 6,521,424 |
| Target Validation | Click to Find Target Validation Information. |
| Inhibitor | (4-Phenoxy-phenyl)-quinazolin-4-yl-amine | | [3] |
| 3,4-di- (4-methoxyphenyl)-1H-pyrrole-2,5-dione | | [4] |
| 3,4-diphenyl-1H-pyrrole-2,5-dione | | [4] |
| 3- (4-methoxyphenyl)-4-phenyl-1H-pyrrole-2,5-dione | | [4] |
| 3- (indole-3-yl)-4-phenyl-1H-pyrrole-2,5-dione | | [4] |
| A-420983 | | [5] |
| CEP-7055 | | [2] |
| Multitarget | CEP-7055 | | [2] |
| Cross References |
3D Structure
Related Literature
On-Line
Medical Dictionary |
| Ref 1 | Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. To Reference |
| Ref 2 | A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22. To Reference |
| Ref 3 | Bioorg Med Chem Lett. 2000 Oct 2;10(19):2167-70.Pyrrolo[2,3-d]pyrimidines containing an extended 5-substituent as potent and selective inhibitors of lck I. To Reference |
| Ref 4 | J Med Chem. 2006 Feb 23;49(4):1271-81.Design, synthesis, and biological evaluation of 3,4-diarylmaleimides as angiogenesis inhibitors. To Reference |
| Ref 5 | Bioorg Med Chem Lett. 2004 May 17;14(10):2613-6.A-420983: a potent, orally active inhibitor of lck with efficacy in a model of transplant rejection. To Reference |
