RelatedCAS#:262438-43-7(freebase) Unknown(TFA)  

Synonym:ATN161;ATN161;ATN-161;AcPHSCNNH2

IUPAC/ChemicalName:(S)-2-((R)-2-((S)-2-((S)-2-((S)-1-acetylpyrrolidine-2-carboxamido)-3-(1H-imidazol-5-yl)propanamido)-3-hydroxypropanamido)-3-mercaptopropanamido)succinamide

InChiKey:MMHDBUJXLOFTLC-WOYTXXSLSA-N

InChiCode:InChI=1S/C23H35N9O8S/c1-11(34)32-4-2-3-17(32)23(40)29-14(5-12-7-26-10-27-12)20(37)30-15(8-33)21(38)31-16(9-41)22(39)28-13(19(25)36)6-18(24)35/h7,10,13-17,33,41H,2-6,8-9H2,1H3,(H2,24,35)(H2,25,36)(H,26,27)(H,28,39)(H,29,40)(H,30,37)(H,31,38)/t13-,14-,15-,16-,17-/m0/s1

SMILESCode:O=C(N)[C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@H]1N(C(C)=O)CCC1)=O)CC2=CN=CN2)=O)CO)=O)CS)=O)CC(N)=O

TechnicalData

AdditionalInformation

ATN-161inhibitedVEGF-inducedmigrationandcapillarytubeformationinhCECs,butdidnotinhibitproliferation.Invivo,injectionofATN-161afterlaserphotocoagulationinhibitedCNVleakageandneovascularizationtoanextentsimilartoAF564.FurThermore,SD-OCTandhistologicexaminationsindicatedthatATN-161significantlydecreasedthesizeoflaser-inducedlesions.CONCLUSIONS:Integrinα5β1inhibitionbyATN-161maybeapromisingalternativetherapyforCNV-relatedangiogenesis.Inaddition,SD-OCTtechnologyallowsexcellentvisualizationofexperimentallyinducedCNVinvivo.(source:InvestOphthalmolVisSci.2011Sep14;52(10):7213-20).
  
 

References

1:DaiW,YangT,WangX,WangJ,ZhangX,ZhangQ.PHSCNK-Modifiedanddoxorubicin-loadedliposomesasadualtargetingsystemtointegrin-overexpressingtumorneovasculatureandtumorcells.JDrugTarget.2010May;18(4):254-63.PubMedPMID:19824864.

2:DoñateF,ParryGC,ShakedY,HensleyH,GuanX,BeckI,Tel-TsurZ,PlunkettML,ManuiaM,ShawDE,KerbelRS,MazarAP.PharmacologyofthenovelantiangiogenicpeptideATN-161(Ac-PHSCN-NH2):observationofaU-shapeddose-responsecurveinseveralpreclinicalmodelsofangiogenesisandtumorgrowth.ClinCancerRes.2008Apr1;14(7):2137-44.PubMedPMID:18381955.

3:DaneseS,SansM,SpencerDM,BeckI,DoñateF,PlunkettML,delaMotteC,RedlineR,ShawDE,LevineAD,MazarAP,FiocchiC.Angiogenesisblockadeasanewtherapeuticapproachtoexperimentalcolitis.Gut.2007Jun;56(6):855-62.Epub2006Dec14.PubMedPMID:17170016.

4:ChidlowJHJr,LangstonW,GreerJJ,OstaninD,ABDelbaqiM,HoughtonJ,SenthilkumarA,ShuklaD,MazarAP,GrishamMB,KevilCG.Differentialangiogenicregulationofexperimentalcolitis.AmJPathol.2006Dec;169(6):2014-30.PubMedPMID:17148665;PubMedCentralPMCID:PMC1762465.

5:KhaliliP,ArakelianA,ChenG,PlunkettML,BeckI,ParryGC,DoñateF,ShawDE,MazarAP,RabbaniSA.Anon-RGD-basedintegrinbindingpeptide(ATN-161)blocksbreastcancergrowthandmetastasisinvivo.MolCancerTher.2006Sep;5(9):2271-80.PubMedPMID:16985061.

6:CianfroccaME,KimmelKA,GalloJ,CardosoT,BrownMM,HudesG,LewisN,WeinerL,LamGN,BrownSC,ShawDE,MazarAP,CohenRB.Phase1trialoftheantiangiogenicpeptideATN-161(Ac-PHSCN-NH(2)),abetaintegrinantagonist,inpatientswithsolidtumours.BrJCancer.2006Jun5;94(11):1621-6.PubMedPMID:16705310;PubMedCentralPMCID:PMC2361324.

7:StoeltzingO,LiuW,ReinmuthN,FanF,ParryGC,ParikhAA,McCartyMF,BucanaCD,MazarAP,EllisLM.Inhibitionofintegrinalpha5beta1functionwithasmallpeptide(ATN-161)pluscontinuous5-FUinfusionreducescolorectallivermetastasesandimprovessurvivalinmice.IntJCancer.2003Apr20;104(4):496-503.PubMedPMID:12584749.