Influence of Linker Molecules in Hexavalent RGD Peptides on Their Multivalent Interactions with Integrin alpha(v)3(beta)

'multivalent r)Deptideshavebeenusedasanexcellenttargetingvect tinteg11n(i33-Pcs1t1vetumors. Hu weve little attention has beenFa d to the influenceof linker muiecuiesinmlitivaentRGDPe:tides ntlelrdiss cat1 n(1nfr fromtumor thedissociatiun kinetics uL99 ic_iaheied hexava etRG1PePtideswhichhave(:H...

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Veröffentlicht in:Journal of medicinal chemistry 2021-11, Vol.64 (21), p.16008-16019
Hauptverfasser: Mizuno, Yuki, Kimura, Kohta, Onoe, Satoru, Shukuri, Miho, Kuge, Yuji, Akizawa, Hiromichi
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Sprache:eng
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Zusammenfassung:'multivalent r)Deptideshavebeenusedasanexcellenttargetingvect tinteg11n(i33-Pcs1t1vetumors. Hu weve little attention has beenFa d to the influenceof linker muiecuiesinmlitivaentRGDPe:tides ntlelrdiss cat1 n(1nfr fromtumor thedissociatiun kinetics uL99 ic_iaheied hexava etRG1PePtideswhichhave(:H:-CH2 0) (n = 4 [9nrc]['c(l1)6]+ldn=12'[99nTc][Tcr'2\6]Tor()pt0-Gly)(n=i[99mTc][Te(L3\6]'1=6' 99mTcTc(L4)61+,and molecule.[9n iLTe(L:)] dtsplayedsl)erdiss clati nuneticsand[9mTc1 rL4/6+sI vedexcefti 1allYhighin1it!ocellIiarnptake (203.1+i6.700,,/lg protein}andtnehighesttumurt bi drati cl38.l 26.3 at 4 hP.1.) inthn rbear11gnu"emice.These findings indicate that the use ofaPproprlate length of (DPru-GlY)w0uidnwimizethe bludtng fmultivaiertRGDPePtidest clustered integrin avP_3-
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.1c01396