A bioconjugate of Lys and Arg mimics biological activity of the Arg-Gly-Asp peptide sequence.
A bioconjugate of Lys and Arg mimics biological activity of the Arg-Gly-Asp peptide sequence.
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Lys 和 Arg 的生物结合物模拟 Arg-Gly-Asp 肽序列的生物活性。
DOI：
10.1016/j.actbio.2004.09.005
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发表时间：
2005
影响因子：
9.7
通讯作者：
Massia,StephenP
中科院分区：
文献类型：
--
作者：
Ehteshami,Gholamreza;Brune,DanielC;Lopez,JohnC;Massia,StephenP
用赖氨酸和精氨酸合成了一种肽模拟物2-氨基-6-[（2-氨基-5 {胍基}戊酰基）氨基]己酸，以产生一种模拟细胞粘附性Arg-Gly-Asp（RGD）肽GRGDSP的生物活性的化合物。当固定在固体基质上时，肽模拟物促进细胞粘附类似于具有固定化GRGDSP的基质。配体竞争研究表明，细胞与肽模拟物的相互作用是整合素介导的。与蛋白水解不稳定的肽相比，肽模拟物对蛋白水解降解非常稳定。GRGDSP和肽模拟物固定在固体基质上时都是稳定的。该肽模拟物具有RGD肽的广泛治疗用途，具有更高的稳定性和潜在的增强的治疗功效。
A peptidomimetic, 2-amino-6-[(2-amino-5{guanidino}pentanoyl) amino] hexanoic acid, was synthesized using Lys and Arg to produce a compound that mimics the biological activity of a cell adhesive Arg–Gly–Asp (RGD) peptide, GRGDSP. When immobilized on solid substrates, the peptidomimetic promoted cell adhesion similar to substrates with immobilized GRGDSP. Ligand competition studies demonstrated that cell interactions with the peptidomimetic were integrin-mediated. The peptidomimetic was very stable to proteolytic degradation in comparison to proteolytically unstable peptides. Both GRGDSP and peptidomimetic were stabilized when immobilized on solid substrates. This peptidomimetic has the broad therapeutic utility of the RGD peptides with higher stability and potentially enhanced therapeutic efficacy.