56612-93-2

Upstream product

• 4530-20-5 BOC-glycine 
• 2791-79-9 dibenzyl L-aspartate 
• 2886-33-1 dibenzyl L-aspartate toluene-4-sulphonate 
• 144-55-8 sodium hydrogencarbonate 
• 77-92-9 citric acid 
• 543-27-1 isobutyl chloroformate 

Downstream Products

• 1421866-04-7 C₃₀H₃₄N₇O₁₀P 
• 257940-90-2 dibenzyl glycyl-L-aspartate trifluoroacetate 
• 186379-70-4 Arg(NO₂)-Gly-Asp(OBzl)-OBzl 
• 4530-20-5 BOC-glycine 
• 2791-79-9 dibenzyl L-aspartate 

Relevant academic research and scientific papers

Dual-active targeting liposomes drug delivery system for bone metastatic breast cancer: Synthesis and biological evaluation

Bone is the most common organ affected by metastatic breast cancer. Targeting cancers within the bone remains a great challenge due to the inefficient delivery of therapeutic to bone. In order to increase the distribution of paclitaxel (PTX) in bone metastases, in this study, a novel bone-targeted glutamic oligopeptides-RGD peptide (Glu6-RGD) derivative was designed and synthesized as liposome ligand for preparing liposome to effectively deliver PTX to bone metastases. The liposome was prepared and its particle size, zeta potential, encapsulation efficiency, release profile, stability, hemolysis and cytotoxicity were also characterized. What's more, the Glu6-RGD-Lip showed superior targeting ability in vitro and in vivo evaluation as compared to naked PTX, non-coated, singly-modified and co-modified by physical blending liposomes. All the results suggested that Glu6-RGD-modified liposome showed excellent targeting activity to metastatic bone cancer. This study may be conducive to the field of bone-targeting drugs delivery.

Dual-targeting liposomes with active recognition of GLUT5 and αvβ3 for triple-negative breast cancer

At present, chemo- and radiotherapies remain to be the mainstream methods for treating triple-negative breast cancer (TNBC), which is known for poor prognosis and high rate of mortality. Two types of novel dual-targeting TNBC liposomes (Fru-RGD-Lip and Fru+RGD-Lip) that actively recognize both fructose transporter GLUT5 and integrin αvβ3 were designed and prepared in this work. Firstly, a Y-shaped Fru-RGD-chol ligand, where a fructose and peptide Arg-Gly-Asp (RGD) were covalently attached to cholesterol, was designed and synthesized. Then, the Fru-RGD-Lip was constructed by inserting Fru-RGD-chol into liposomes, while Fru+RGD-Lip was obtained by inserting both Fru-chol and RGD-chol (with the molar ratio of 1:1) into liposomes. The particle size, zeta potential, encapsulation efficiency and serum stability of the paclitaxel-loaded liposomes were characterized. The results indicated that the paclitaxel-loaded Fru-RGD-Lip had the strongest growth inhibition against GLUT5 and αvβ3 overexpressed MDA-MB-231 and 4T1 cells. The cellular uptake of Fru-RGD-Lip on MDA-MB-231 cells and 4T1 cells was 3.19- and 3.23-fold more than that of the uncoated liposomes (Lip). The uptake of Fru+RGD-Lip was slightly lower, giving a 2.81- and 2.90-fold increase than that of Lip in two cell lines, respectively. The mechanism study demonstrated that the cellular uptake of both dual-targeting liposomes was likely to be recognized and mediated by GLUT5 and αvβ3 firstly, then endocytosed through comprehensive pathways in an energy-dependent manner. Moreover, Fru-RGD-Lip displayed the maximum accumulation, which was 2.62-fold higher than that of Lip for instance, at the tumor sites compared to other liposomes using in vivo imaging. Collectively, the liposomes co-modified by fructose and RGD have enormous potential in the development of targeted TNBC treatment, especially the covalently modified Fru-RGD-Lip, making it a promising multifunctional liposome.

Novel double brain tumor-targeted lipid material and application thereof

The invention discloses a novel lipid material. The novel lipid material is used for prolonging the circulating time and increasing the transfer amount of medicine to brain tumor tissues in a target way. The novel lipid material is characterized in that polyethylene glycol is used as a bridge, one side of the bridge is connected with cholesterol, and one side of the bridge is connected with glucose and RGD (arginine-glycine-aspartic acid) peptide, so that the lack of brain tumor targeting ability by the lipid modified by the single glucose or the RGD peptide is overcome, and the brain tumor can be effectively targeted after blood brain barrier crossing. The novel lipid material can be used for different preparation types of lipids, nanoparticles, micelles and the like; the prepared paclitaxel-carrying lipid has obvious brain tumor targeting function, and broad application prospect.

Stereoselective and Site-Specific Allylic Alkylation of Amino Acids and Small Peptides via a Pd/Cu Dual Catalysis

We report a stereoselective and site-specific allylic alkylation of Schiff base activated amino acids and small peptides via a Pd/Cu dual catalysis. A range of noncoded α,α-dialkyl α-amino acids were easily synthesized in high yields and with excellent enantioselectivities (up to >99% ee). Furthermore, a direct and highly stereoselective synthesis of small peptides with enantiopure α-alkyl or α,α-dialkyl α-amino acids residues incorporated at specific sites was accomplished using this dual catalyst system.

Dipeptides as leaving group in the enzyme-catalyzed DNA synthesis

Conjugates of 2′-deoxyadenosine monophosphate with dipeptides have been synthesized and tested as substrates for several polymerases. Although the incorporation efficiency is not very high, it demonstrates that some of these dipeptides can be accommodated in the active site of polymerases and function as leaving groups in the enzymatic synthesis of DNA. Copyright

Effect of Polyethylene Glycol on the Synthesis of Oligopeptide by Papain in an Organic Medium

The enzymic peptide synthesis in an organic medium was investigated by using papain in the presence of PEG.The added PEG enhanced the enzyme activity of papain for synthesis of the peptide, Boc-Gly-Asp(OBzl)OBzl.The activity of papain in the PEG-added system was higher than that in a PEG-free system.

Tripeptides useful as immunostimulants as well as in the prevention of metastases

The present invention is referred to tripeptides having the following general formula: where X=L-Arg or D-Arg and Y=L-Asp or D-Asp. These tripeptides, endowed with both immunostimulant and antimetastatic properties, are active not only after parenteral administration, but also after oral treatment. The invention is also related to the procedure for the preparation of said compounds.