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
收藏
页码：16008 / 16019
页数：12
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