Influence of Linker Molecules in Hexavalent RGD Peptides on Their Multivalent Interactions with Integrin αv3β

被引：10

作者：

Mizuno, Yuki ^{[1
,2
,3
]}

Kimura, Kohta ^{[1
]}

Onoe, Satoru ^{[1
]}

Shukuri, Miho ^{[1
]}

Kuge, Yuji ^{[2
,3
]}

Akizawa, Hiromichi ^{[1
]}

机构：

[1] Showa Pharmaceut Univ, Lab Phys Chem, Machida, Tokyo 1948543, Japan

[2] Hokkaido Univ, Cent Inst Isotope Sci, Sapporo, Hokkaido 0600815, Japan

[3] Hokkaido Univ, Grad Sch Biomed Sci & Engn, Dept Biomed Imaging, Sapporo, Hokkaido 0608638, Japan

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2021年 / 64卷 / 21期

关键词：

LIGANDS; BIVALENT; AVIDITY; PROBES;

D O I：

10.1021/acs.jmedchem.1c01396

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

'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-

引用

页码：16008 / 16019

页数：12

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