第五组VEGFR刘有平陈桂英佟岩王钢教学

1、第五组：VEGFR刘有平 陈桂英佟岩 王钢背景介绍:VEGFR：血管内皮细胞生长因子受体(vascular endothelial growth factor receptor) 血管生成是人体肿瘤生长和转移的必要条件，抑制肿瘤细胞介导的血管生成已成为近 年来寻找新型抗肿瘤药物的一个主要研究方向。VEGF：血管内皮细胞生长因子，体内活性最强、专属性最高的促血管生成因子VEGFR：受体酪氨酸激酶，以VEGF受体为靶点的肿瘤血管生成抑制剂具有特异性高、 不易产生耐受性、毒性小等优点，成为近年来抗肿瘤药物研究与开发的热点。分类：VEGFR1VEGFR2：在血管生成中作用最重要VEGFR3检索策略分析

2、：检索目的：检索以VEGFR2为靶点的抗肿瘤药物研究进展检索入口 ： Drugs & BiologiesDrugs & Biologies、Targets & PathwaysIGenomicsBiomarkersDrug Name SearchQuick Access to PipeEne Infbnna:ioiiGatervavs to Devehpmenc StatusgoOrganic SynthesisExperimental PharmacologyPharmacokineticsAletabolisrnClinical StudiesDisease BriefngsCompani

3、es & Research InstitutionsLiteraturePatentsHighlightsToday*& NewsConditicnLookLpJOctober 17-212011Company News Roch亡 to expand HCV portfolio with acquisition of Anadvs Dermatological Disorders ULURU tc out-license European rights to Altrazwal Substance Abuse & Poisoning FDA grants accelerated approv

4、al to AcoPharmas Ferripg: Metabolic Disorders TTTS 北submits XDA for QnxaAnalgesia & Anesthesia Archimedes Pharma launches LazandaWHATS NEWIMPORTANTNOTICESNEW INTEGRITYLEARNING CENTERWeekly InsightsOneQick access to recem andrelevani infannaon found in IMegHly.updstedescii MondayThe Starting LineA se

5、lection of new molecularentities and fargets i旳dy to enter the R&D arena.Advanced SearchSession HistoryClear FormStartSelect ValueOptional ValueOptional Valu Lead Compounds Under Active DevelopmentIndex AND Index AND .6ndex AND ReferenceSelect ValueOptional ValueOptional Value卜Mdcx AND Index AND Ind

6、ex AND JTargets & PathwaysMamie (Target Name)z Index AND Condition (Condition)Index AND Optional Value-flndex AND PatentSelect Value1Optional Value1Optional Value15如 AND Index AND kidcx AND Make your selection directly from the list at right or enter a word or part of a word in the box below 日nd cli

7、ck Lookup- to display on the right a short list of search terms from which to make your selection. It is not necessary to use truncation in dicators.VEGFR Lookup 0-9ABCDEFGHIJKLMNOPCRMMSTUVWXYZClick the plus s-ign next to a term to display subclasses nnd make your selection Alteirnmtix/el” enter a w

8、ord or part of a word in the box below and click Lookup Then use the scroll bar in com bin ation with the First, Previous, Next and Last buttons to locate terms within the hierarchy.LookupClick the button below to chang亡 b-et/veenHierarchical and Alphabetical listsOrdei Al phafreticallySelect one or

9、 more terms from the list b-elow and click OK to copy the term(s) to the Search FormSoluble VEGFR1 (sFlt-1)Soluble VEGFR1 variant 2Soluble VEGFR1 variant 21VEGFR (nonspecified subtype) VEGFR-1VEGFR-1 (Flt-1)VEUFRT |VtUhK-2 (hLK-1 /KD R)VEGFR-3VEGFR-3 (FLT4) isoform 2VEGFR1VEGFR2VEGFR3Vegfr!Vegfr2Veg

10、fr3Select a Value:SAIDS田 Anesth 背 iaI ElCmncer ISCardiovascular DisordersECongenital defectsECritical care medicine0Dermatological DisordersDiag no stiesEDisorders of Sexual Function and ReproductionSEar Disorders田Endocrine DisordersEEye Disorders田Gastrointestinal Disorders田Genetic DisordersSGenitou

11、rinarv DisordersEHematologic Diseases田Immunological Disorders田 Infections Advanced SearchSession HistoryClear Po-rmiStart Lead Compounds Under Active DevelopmentSelect ValueIndex AND rOptional ValuefIndex AND Optional ValueIndex AND Jindex AND Index AND Index AND ReferenceTargets & PathwaysMame (Tar

12、get Hame)VEGFWIndex AND Condition (Condition)MCancerM莎两AND Optional Valueindex AND Select ValueOptionalValueOptional ValuePatentSelect ValueOptional ValueOptional ValueIndex AND index AND r fadex AND 结果:1370个卜、THOMSON RFUTERSIntegrityQuick SearchDrugs & Biologies Name = PEGFRZ AND Condition = Cancer

13、Entrv NumberHighest PhaseCode NameGeneric NameBrand NameProduct Category 117760Precli nical5GGPGGPentagalloyl glucoseTherapeutic GroupMechanism of ActionOrganizationAlzheimers DementiafAldose ReductaseEwha WomansTreatment ofInhibitorsUniversityAnti-Hepatitis C VirusAn giogenesisKanawon NationalDrugs

14、InhibitorsUniversityAn tiallergy/AntiasthmaticAntiamyloidogenicKvuna HeeDrugsAgentsUn iversitvAn ticoagula ntsAn tioxida ntsSeoul NationalAntiviral DrugsHCV NS3Un iversitvOncolytic DrugsProteaseUniversity ofStroke, Treatment of Symptomatic AntidiabeticInhibitorsTokushimaHMOX1Universitv ofAgentsExpre

15、ssi onTovamaVasodilatorsEnhencers Mediator Release Inhibitors Phagocytosis InducersWonkwang UniversityProlyl Endopeptidase (prolyl oligopeptidase; POP) Inhibitors VEGFR-1 (Flt-1) InhibitorsJibP Development Status Organization Major Therapeutic GroupsP Therapeutic Groupt Major Condition Groupsb Condi

16、tion Mechanistic ScopeMolecular Mechanisms Cellular Mechanisms Major Product Categories Product CategoryP Launch Yeart Therapeutic Impact andOrganization (3D chart)P Targett Under Active Development / No Development Reported Condition and Phase(3D chart)Rlter by StatisticsNot Deter minedDisc on tinu

17、edBiological TestingPreclinicalIND FiledClinicalPhase I1 Display OptionsIIIHorizontalVerticalPie ChartDisplayDisplayDisplayView Subset(s)Print ChartPhase I/IIPre- RegisteredLaunchwdNot ApplicableG Check AllnoooooCMXTVOcoOOOHoowrl00004 ocoiH Help索拉非尼，凡德他尼，舒尼替尼，帕卩坐帕尼等Records Retrieved6 in Drugs 8 Biol

18、ogies Search ResultsOptionsDrugs & Biologies Search ResultsEntryHighestCode NameGenericBrandNumberPhase ；NameName 283701Product CategoryTherapeutic GroupMechanism of ActionOrganizationFilter by StatisticsLaunched-2007Actinic Keratoses, AgentsAGE InhibitorsAbbottfor(MaillardsBradlevBladder C 汕 cer Th

19、erapyReactionPharmaceuticalsChemopreventive AgentsInhibitors)Dermatologic DrugsAP-1 IrhibitorsEpitomeGenital Wartsr TreatmentATM KinaseExpa nscierceforIrflammatory BowelInhibitorsATQ KinaseGC-RiseJSBia PharmJusteDisease, Agents forInhibitorsAdenosine AlAntagonistsMediGeneAdenosine A2AMitsui NornAn t

20、agonists(Originator)Adenosine A2BNational CancerAntagonistsInsti:u:eAldose ReductaseNatl Inst DabetesInhibitorsDigest Kidney DisAngiogenesisNvccmedInhibitorsPharmaNovaAntioxidantsPolyphenon PharmaApoptosis InducerslOrignator) TevaAromataseInhibitorTriton 3harmaBacterial EffluxPump InhibitorsUniversi

21、ty ofCalifornia, SanKunecatechins Polyphenon Herbals Sinecatechins EVeregen4 Development Status卜 Organization卜 Major Therapeutic Groups Therapeutic Group Major Condition Groups ConditionP Mechanistic ScopeMolecular MeehsnismsCellular Mechanisms Major Product CategoriesP Product Category Launch Year卜

22、 Therapeutic Impact andOrganization(3D chart) TargetP Under Active DevelopmentI No DevelopmentReported Condition and Phase(3D chart) Filter Only Lead CompoundsRecords Retrieved1 in Drugs & BiologiesDrugs & Biologies Search Results Entry Humber304792UPDATESChemical StructureCAS Registry No.Molecular

23、Formula338992-00-0338992-48-6 (HCI)338992-53-3(mono trifluoroacetate)C22H24BrFN4O2Molecular Weight475.354Highest PhaseLaunched - 2011Under ActiveDevelopment0VandetanibChemical Nam引DescriptionN-(4-Bromo-2-fluorophenyl)-6-methoxy-7-(l-methylpiperidin-4-ylmethoxy)quinazolin-4-amineOptionsIKeep Me Poste

24、dExport Center韵 Integrity Reports0Product List with StructuresNJ4卜fDisplay Milestones=Gateways to Product Development StatussReferencesAll Related Information via Quick Search(SPrinter Friendly FormatFilter by StatisticsStandard InChi1S/C22H24BFN4O2/c12&7知 4(&28”230211仏14儆诃20(21)292)22(26仔2519)271&4

25、15(23)弘17(18)24/1)34311,仔14比512112,125.26,27)Standard InChlKeyUHTHHESEBZOYNR-UHFFFAOYSA-Nb Development StatusA OrganizationP Major Therapeutic Groupst Therapeutic GroupP Major Condition Groupsb Condition Mechanistic Scope Molecular Mechanisms Cellular Mechanismst Major Product CategoriesP Product Ca

26、tegoryb Launch YearP Therapeutic Impact and Organization (3D chart)卜 Targett Under Active Development / No Development ReportedRELATED10如I 5!RECORDSRELATED145INFO IRECORDSRELATED IMFOTargets & Pathways GenomicsPatentsExperimental PhamacologyClinical StudiesDisease Briefings设置邮件提醒Launuhed2011AZD-6474

27、CH-331ZD-6474Umn detanibCaprels-a ZactimaRecords Retrieved6 in Drugs & Biologies Search ResultsDrugs & Biologies Search ResultsAbl Kinase Inhibitors Angiogenesis Inhibitors-EGFR (HER1； erbBl) Inhibitors Flt3 (FLK2/STK1) Inhibitors KIT (C-KIT) Inhibitors RET Inhibitors VEGFR-L (Flt-1) Inhibitors VEGF

28、R-2 (FLK- 1/KDR) Inhibitors VEGFR-3(FLT4) InhibitorsAstra Ze 门 eta (Oridinnto 门D吕naFarbw厂 Umncer I门EtituteNLD- Andersen dancer UenterNaticnad Came已厂Stanfa 厂dUnivsfsityTyrphostins. Brain Cancer Therap-y Breast Cancer Therapy Cancer Associated Dis-orders, Treatment of Cancer of Un specified Body Locat

29、ion/System Colorectal Cancer Therapy Di gestive/Gastrointestinal Cancer Therapy Endocrine cer Therapy Female Reproductive System Cancer Therapy Genitourinary Cencer Therapy Glioblastoma M u 11 if o r nn eTh e ra py Head and Neck Oancer Therapy Liver Cancer Therapy NAiirnlngirAl CJpnpfic Disorders, Treatment of Non-Small Cell Lung Cancer Therapy Pancreatic Cancer Therapy Prostate Cancer Therapy Rznial C