RGD peptides

Horton MA, Taylor ML, Arnett TR et al (1991) Arg-Gly-Asp (RGD) peptides and the anti-vitronectin receptor antibody 23C6 inhibit dentine resorption and cell spreading by osteoclasts. Exp Cell Res 195 368-375... 

H. N-methylated cyclic RGD peptides as highly active and selective (X,P3 integrin antagonists. J. Med. Chem. 1999, 42, 3033-3040. 

The neoangiogenic tumor vasculature overexpresses certain integrins and other surface markers, which can also be used for targeting of polyplexes. The RGD peptide motif has been successfully applied for integrin-targeted pDNA [125-128] and siRNA [129, 130] delivery. In many cases, the PEG motif-containing peptide was attached to the polycation via a PEG spacer. For RGD-PEG-PEI/pDNA polyplexes, an optimum grafting with RGD-PEG was required because transfection... 

Park JH, Kwona S, Nam JO et al (2004) Self-assembled nanoparticles based on glycol chitosan bearing 5h-cholanic acid for RGD peptide delivery. J Control Release 95 579-588... 

Guo, C.X., et al., RGD-Peptide functionalized graphene biomimetic live-cell sensor for realtime detection of nitric oxide molecules. ACS Nano, 2012. 6(8) p. 6944-6951. 

Integrin receptor-binding peptides have been used to enhance liposome binding, uptake, and expression (25,47 9). The inclusion of an 0(5pi integrin-targeted peptide into a liposomal complex enhanced transfection efficiency four- to five-fold in Jurkat cells and 10- to 13-fold in TF-1 cells (48). Confocal and electron microscopy revealed that the mechanism of cell entry conferred by RGD peptides on liposomes is predominantly by clathrin-coated endocytosis rather than by phagocytosis (50). 

Colin M, Moritz S, Fontanges P, et al. The nuclear pore complex is involved in nuclear transfer of plasmid DNA condensed with an oligolysine-RGD peptide containing nuclear localisation properties. J Biol Chem 2001 8(21) 1643-1653. 

Annis, D. A. Helluin, 0. Jacobsen, E. N. (1998) Stereochemistry as a diversity element solid-phase synthesis of cyclic RGD peptide derivatives via asymmetric Catalysis., Chem., Int. Ed. Engl, 37, 1907-1909. 

MRX408/phospholipid + RGD peptide-PEG-lipid Thrombus imaging and accelerated thrombolysis [94]... 

Cyclic RGD peptides GPIIb/IIIa/platelets Thrombosis 94-106... 

Five novel RGD peptides 81 containing either one or twice furanoid SAAs 80 were recently synthesized via an efficient solid-phase strategy based on Kaiser s oxime resin 71d (Scheme 43). 

M. Ogawa, K. Hatano, S. Oishi, Y. Kawasumi, N. Fujii, M. Kawaguchi, R. Doi, M. Imamura, M. Yamamoto, K. Ajito, T. Mukai, H. Saji, K. Ito, Direct electrophilic radiofluorination of a cyclic RGD peptide for in vivo alpha(v)beta(3) integrin related tumor imaging, Nucl. Med. Biol. 30 (2003) 1-9. 

W. Cal, X. Zhan, Y. Wu, X. Chen, A thiol-reactive F-labeling agent, N-[2-(4-i8F-f uorobenzamido)ethyl]maleimide, and synthesis of RGD peptide-based tracer for PET imaging of alpha-v-beta-3-integrin expression, J. Nucl. Med. 47 (2006) 1172-1180. 

Respiratory syncytial virus protein G related peptides containing two multiple disulfide bridges rice bran peptides RGD peptides... 

The osteoclast is unique in mobilizing massive quantities of calcium from mineralized tissue. Dissolving hydroxyapatite requires the addition of protons, just as deposition of hydroxyapatite liberates acid (see Equation 1). To allow acidification, the osteoclast produces an isolated micro-compartment on the bone surface. This is achieved by close apposition to the matrix via adhesion of av integrins to matrix RGD peptides, with (33 the major complementary subunit (Miyauchi et al., 1991). Inside the osteoclast the cytoskeleton (Akisaka et al., 2006), and transport activities (Vaananen et al., 2000 Schlesinger et al., 1994) are reorganized to support the resorption compartment. 

Meinecke, R. and Meyer, B., Determination of the binding specificity of an integral membrane protein by saturation transfer difference NMR RGD peptide ligands binding to integrin alphallbbeta3. J Med Chem, 2001, 44, 3059-3065. 

Figure 8. An IL-2 receptor antagonist (1) RGD peptide mimetic gpllb/llla receptor antagonists.

Figure 10. RGD peptide mimetic avP3 receptor antagonists.

The hexon for knob-independent transduction of smooth muscle cells by incorporation of an integrin-recognizing RGD-peptide [27]. 

In an alternative scenario, 7-mer or 20-mer oligolysine sequences (which interact with heparan sulfate) have been fused to the C terminus of the fiber protein. This modification led to a dramatically increased and CAR-independent transduction of endothelial cells, smooth muscle cells, and macrophages in vitro and in vivo (up to > 100-fold) [33, 34], of myeloma cells and AML blast cells in vitro [35, 36], and of cultured glioma cells in vitro [37, 38], A similar approach has been used to fuse an RGD peptide (RDG-4C) to the C terminus of the fiber, which led to an increased transduction of endothelial cells in vitro and in vivo [33, 39], The same RGD-containing peptide has also been incorporated into the HI-loop of the fiber protein, resulting in an up to 1000-fold increased and CAR-independent transduction of primary endothelial cells and ovarian and head and neck cancer cells in vitro [40, 41]. 

De Scheerder I, Wang K, Wilczek K, et al, Local methylpred-nisolone inhibition of foreign body response to coated intracoronary stents, Coronary Artery Dis 1996 7 161-166. Baker J, Nikolaychik V Zulich A, et al, Fibrin coated stents as depot to deliver RGD peptide inhibit vascular reaction in atherosclerosis rabbit model [abstr], J Am Coll Cardiol I 996 27 197A,... 

We modified a polyethersulfone membrane (PES) surface with a plasma-deposited acrylic acid coating (PES-pdAA) and RGD peptide covalently immobilized through a spacer arm molecule (SA), obtaining PES-pdAA-SA-RGD membranes. The same method was used to immobilize galadose in its acid form (Galadonic acid) to obtain the PES-PdAA-SA-GAL membranes. 

Kessler and coworkers immobilized RGD peptides to a PMMA surface via a spacer incorporating an azobenzene unit [ 187]. The molecules were arranged in such a way that the RGD motifs were accessible to cells approaching the surface when the azo unit was in the E-form, and were hidden from the cells when the azo unit was in the Z-form. This enabled the reversible modulation of mouse osteoblast adhesion by irradiation with visible or UV light. However, the difference between on and off states is not very pronounced. Possibly, the accessibility of the RGD motif is not... 

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