82082-83-5

Upstream product

• 56-86-0 L-glutamic acid 
• 104-15-4 toluene-4-sulfonic acid 
• 2791-84-6 L-glutamic acid dibenzyl ester 4-toluenesulfonate 
• 100-51-6 benzyl alcohol 
• 2768-50-5 dibenzyl L-glutamate 
• 13574-13-5 Boc-Glu(OBzl)-OH 
• 89092-61-5 N-tertbutyloxycarbonyl dipeptide of benzyl glutamate 
• 133981-03-0 (S)-2-[(S)-4-Benzyloxycarbonyl-2-(4-methoxy-benzyloxycarbonylamino)-butyrylamino]-pentanedioic acid dibenzyl ester 

Downstream Products

• 159828-36-1 (S)-2-((S)-4-Benzyloxycarbonyl-2-octanoylamino-butyrylamino)-pentanedioic acid dibenzyl ester 
• 121445-54-3 Boc-Glu(OBzl)3-OBzl 
• 146552-87-6 (S)-2-{(S)-4-Benzyloxycarbonyl-2-[(S)-4-benzyloxycarbonyl-2-((S)-4-benzyloxycarbonyl-2-octanoylamino-butyrylamino)-butyrylamino]-butyrylamino}-pentanedioic acid dibenzyl ester 
• 146552-86-5 (S)-2-[(S)-4-Benzyloxycarbonyl-2-((S)-4-benzyloxycarbonyl-2-octanoylamino-butyrylamino)-butyrylamino]-pentanedioic acid dibenzyl ester 
• 146552-80-9 (S)-2-((S)-4-Benzyloxycarbonyl-2-{(S)-4-benzyloxycarbonyl-2-[(S)-4-benzyloxycarbonyl-2-((S)-4-benzyloxycarbonyl-2-tert-butoxycarbonylamino-butyrylamino)-butyrylamino]-butyrylamino}-butyrylamino)-pentanedioic acid dibenzyl ester 
• 89107-69-7 Boc-Glu(OBzl)4-OBzl 
• 89107-70-0 Glu(OBzl)4-OBzl 
• 133981-04-1 L-lactoyl-γ-L-glutamyl-L-glutamic acid tribenzyl ester 

Relevant academic research and scientific papers

Polyethylene glycol coupling medicine as well as preparation method and application thereof

The invention relates to the technical field of medicines, relates to a polyethylene glycol coupled drug as well as a preparation method and an application thereof, and in particular relates to a polyethylene glycol coupled drug as shown in a formula I or pharmaceutically acceptable salt thereof. The invention also relates to a preparation method of the polyethylene glycol coupled drug or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing the polyethylene glycol coupled drug or the pharmaceutically acceptable salt thereof, and the application of the polyethylene glycol coupled drug or the pharmaceutically acceptable salt thereof in preparation of drugs.

Dual-targeting liposome modified by glutamic hexapeptide and folic acid for bone metastatic breast cancer

Bone is the most common organ affected by metastatic breast cancer. Targeting delivery of drugs to bone may not only enhance the treatment efficacy, but also reduce the quantity of drug administered. In order to increase the distribution of paclitaxel (PTX) in bone, herein, a novel bone metastasis-targeted glutamic hexapeptide-folic acid (Glu6-FA) derivative was designed and synthesized as liposome ligand to deliver PTX to bone metastasis effectively. The liposomes were prepared by thin film hydration method and its particle size, zeta potential, encapsulation efficiency, release profile, stability, hemolysis were also characterized. What's more, the anti-tumor effects of PTX-Glu6-FA-Lip were confirmed by the detection of cell cycle, migration, and further measurement of microtubule stabilization. In addition, the PTX-Glu6-FA-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-FA-modified liposome showed excellent targeting activity to metastatic bone cancer. These findings suggested that Glu6-FA-Lip was a promising bone metastasis-targeting carrier for the delivery of PTX. This study may therefore be conducive to the field of bone-targeting drugs delivery.

CONJUGATES OF WATER SOLUBLE POLYMER-AMINO ACID OLIGOPEPTIDE-DRUG, PREPARATION METHOD AND USE THEREOF

A conjugate of water soluble polymer-amino acid oligopeptide-drug of Formula (I) below and a pharmaceutical composition comprising the conjugate are provided. In the conjugate, P is a water soluble polymer; X is a linking group, wherein the linking group links P and A1; each of A1, A2 and A3 is independently same or different amino acid residue or amino acid analogue residue; each of D1 and D2 is independently same or different drug molecule residue; a is 0 or 1; b is an integer of 2-12; c is an integer of 0-7; d is 0 or 1. The conjugate could improve drug load capacity, water solubility, stability and activity of the drug.

Synthesis and preliminary evaluation of novel bone-targeting NSAIDs prodrugs based on glutamic acid oligopeptides

Osteoarthritis is no doubt a difficult disease to manage. Targeted delivery of drugs to bone may not only enhance the treatment efficacy, but also reduces the quantity of drug administered. In this paper, we have synthesized two series of NSAID-Glu oligop

The β-Type Structures of Very Simple N-Octanoyl-L-glutamic Acid Oligomers (Residue Number, N = 2 - 6) and Their β1 -> β2 - Type Transition

N-Octanoyl-L-glutamic acid oligomers (residue number, N = 2 - 6) have been synthesized in order to study their molecular conformations in the solid state.The X-ray powder diffraction patterns and vibrational spectra of these oligomers have been investigat

Synthesis of a Proposed Isomer of F420 having α-Glutamyl Bonding.

A proposed isomer of redox coenzyme F420 having α-glutamyl bonding, has been synthesized from 8-benzyloxy-10-D-ribityl-5-deazaflavin and α-L-glutamyl-L-glutamic acid moiety, by the phosphite triester approach followed by deprotection procedures.

Synthesis of acyclic and dehydroaspartic acid analogues of Ac-Asp-Glu-OH and their inhibition of rat brain N-acetylated α-linked acidic dipeptidase (NAALA dipeptidase)

The following structural and conformationally constrained analogues of Ac-Asp-Glu-OH (1) were synthesized: Ac-Glu-Glu-OH (2), Ac-D-Asp-Glu-OH (3), Ac-Glu-Asp-OH (4), Ac-Asp-Asp-OH (5), Ac-Asp-3-aminohexanedioic acid (6), Ac-3-amino-3-(carboxymethyl)propanoyl-Glu-OH (7), N-succinyl-Glu-OH (8), N-maleyl-Glu-OH (9), N-fumaryl-Glu-OH (10), and Ac-Δ(z)Asp-Glu-OH (11). These analogues were evaluated for their ability to inhibit the hydrolysis of Ac-Asp-[3,4-3H]-Glu-OH by N-acetylated α-linked acidic dipeptidase (NAALA dipeptidase) in order to gain some insight into the structural requirements for the inhibition of this enzyme. Analogues 4-6 and 9 were very weak inhibitors of NAALA dipeptidase (K(i) > 40 μM), while 2, 3, and 7 with K(i) values ranging from 3.2-8.5 μM showed intermediate inhibitory activity. The most active inhibitors of NAALA dipeptidase were compounds 8, 10, and 11 with K(i) values of 0.9, 0.4, and 1.4 μM, respectively. These results suggest that the relative spacing between the side chain carboxyl and the α-carboxyl group of the C-terminal residue may be important for binding to the active site of the enzyme. They also indicate that the χ1 torsional angle for the aspartyl residue is in the vicinity of 0°.

First total synthesis of coenzyme factor 420

The first total synthesis of Methanobacterium redox coenzyme Factor 420 (F420) has been achieved by the formation of a phosphotriester bond between a protected 8-hydroxy-10-D-ribityl-5-deazaisoalloxazine moiety and a peptide moiety, (L-lactoyl-γ-L-glutamyl)-L-glutamic acid tribenzyl ester, by the phosphite triester approach using 2,2,2-trichloroethyl phosphorodichloridite, followed by successive deprotection procedures.