2887-07-2

Upstream product

• 572-09-8 2,3,4,6-tetra-O-acetyl-D-glucopyranosyl bromide 
• 123-08-0 4-hydroxy-benzaldehyde 
• 70128-27-7 2,3,4,6-tetra-O-acetyl-α-D-glucopyranosylamine 
• 26993-16-8 4-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)benzaldehyde 
• 108-24-7 acetic anhydride 
• 3068-32-4 1-bromo-2,3,4,6-tetra-O-acetyl-D-galactopyranose 
• 7732-18-5 water 
• 86520-63-0 2,3,4,6-tetra-O-acetyl-α-galactopyranosyl trichloroacetimidate 
• 4163-60-4 β-D-galactose peracetate 
• 572-09-8 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl bromide 
• 25878-60-8 D-galactose pentaacetate 
• 83-87-4 penta-O-acetyl-α-D-galactopyranose 
• 7296-64-2 β-D-galactopyranoside 
• 70191-05-8 2,3,4,6-tetra-O-acetyl-β-D-galactopyranose 

Downstream Products

• 141054-29-7 5,10,15,20-tetrakis[4-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)phenyl]porphyrin 
• 59252-47-0 4-(tetra-O-acetyl-β-D-glucopyranosyloxy)benzyl acetate 
• 136337-48-9 6-Methyl-2-oxo-4-[4-((2S,3R,4S,5R,6R)-3,4,5-triacetoxy-6-acetoxymethyl-tetrahydro-pyran-2-yloxy)-phenyl]-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid ethyl ester 
• 138743-97-2 Acetic acid (2S,3R,4S,5R,6R)-4,5-diacetoxy-6-acetoxymethyl-2-[4-(1,8-dioxo-1,2,3,4,5,6,7,8,9,10-decahydro-acridin-9-yl)-phenoxy]-tetrahydro-pyran-3-yl ester 
• 129395-86-4 1-O-(m-Trifluoromethylphenylaminobenzylidene)-2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside 
• 121358-51-8 Acetic acid (2S,3R,4S,5R,6R)-4,5-diacetoxy-6-acetoxymethyl-2-{4-[3-methyl-5-oxo-1,5-dihydro-pyrazol-(4Z)-ylidenemethyl]-phenoxy}-tetrahydro-pyran-3-yl ester 
• 64291-41-4 (2R,3R,4S,5R,6S)-2-(acetoxymethyl)-6-(4-(hydroxymethyl)phenoxy)-tetrahydro-2H-pyran-3,4,5-triyl triacetate 
• 25440-14-6 tetrakis(pentafluorophenyl)porphyrin 

Relevant academic research and scientific papers

Pd(II)-Mediated C?H Activation for Cysteine Bioconjugation

Selective bioconjugation remains a significant challenge for the synthetic chemist due to the stringent reaction conditions required by biomolecules coupled with their high degree of functionality. The current trailblazer of transition-metal mediated bioconjugation chemistry involves the use of Pd(II) complexes prepared via an oxidative addition process. Herein, the preparation of Pd(II) complexes for cysteine bioconjugation via a facile C?H activation process is reported. These complexes show bioconjugation efficiency competitive with what is seen in the current literature, with a user-friendly synthesis, common Pd(II) sources, and a more cost-effective ligand. Furthermore, these complexes need not be isolated, and still achieve high conversion efficiency and selectivity of a model peptide. These complexes also demonstrate the ability to selectively arylate a single surface cysteine residue on a model protein substrate, further demonstrating their utility.

Transmembrane signal transduction by cofactor transport

Information processing and cell signalling in biological systems relies on passing chemical signals across lipid bilayer membranes, but examples of synthetic systems that can achieve this process are rare. A synthetic transducer has been developed that tr

Fluorescent probe for rapidly detecting β - galactosidase and preparation method and application thereof

The invention relates to a fluorescent probe for rapidly detecting β - galactosidase and a preparation method and application thereof. The fluorescent probe for rapidly detecting β - galactosidase has a chemical structural formula as shown in (I). The nea

Two-Dimensional Design Strategy to Construct Smart Fluorescent Probes for the Precise Tracking of Senescence

The tracking of cellular senescence usually depends on the detection of senescence-associated β-galactosidase (SA-β-gal). Previous probes for SA-β-gal with this purpose only cover a single dimension: the accumulation of this enzyme in lysosomes. However, this is insufficient to determine the destiny of senescence because endogenous β-gal enriched in lysosomes is not only related to senescence, but also to some other physiological processes. To address this issue, we introduce our fluorescent probes including a second dimension: lysosomal pH, since de-acidification is a unique feature of the lysosomes in senescent cells. With this novel design, our probes achieved excellent discrimination of SA-β-gal from cancer-associated β-gal, which enables them to track cellular senescence as well as tissue aging more precisely. Our crystal structures of a model enzyme E. coli β-gal mutant (E537Q) complexed with each probe further revealed the structural basis for probe recognition.

Potential Dental Biofilm Inhibitors: Dynamic Combinatorial Chemistry Affords Sugar-Based Molecules that Target Bacterial Glucosyltransferase

We applied dynamic combinatorial chemistry (DCC) to find novel ligands of the bacterial virulence factor glucosyltransferase (GTF) 180. GTFs are the major producers of extracellular polysaccharides, which are important factors in the initiation and development of cariogenic dental biofilms. Following a structure-based strategy, we designed a series of 36 glucose- and maltose-based acylhydrazones as substrate mimics. Synthesis of the required mono- and disaccharide-based aldehydes set the stage for DCC experiments. Analysis of the dynamic combinatorial libraries (DCLs) by UPLC-MS revealed major amplification of four compounds in the presence of GTF180. Moreover, we found that derivatives of the glucose-acceptor maltose at the C1-hydroxy group act as glucose-donors and are cleaved by GTF180. The synthesized hits display medium to low binding affinity (KD values of 0.4–10.0 mm) according to surface plasmon resonance. In addition, they were investigated for inhibitory activity in GTF-activity assays. The early-stage DCC study reveals that careful design of DCLs opens up easy access to a broad class of novel compounds that can be developed further as potential inhibitors.

Synthesis method of gastrodin intermediate and application

The invention relates to a synthesis method of a gastrodin intermediate and application. The synthesis method comprises the following steps that inorganic base, p-hydroxybenzaldehyde and water are mixed to obtain a solution A; a polar aprotic solvent, bromotetraacetylglucose and a phase transfer catalyst are mixed to obtain a solution B; and the solution A, the solution B and fluoride are mixed for reaction, and after the reaction is finished, post-treatment is carried out to obtain the gastrodin intermediate. The synthesis method is simple to operate, green and environment-protecting, and high in yield at the same time.

ANTIBODY-DRUG CONJUGATES COMPRISING ANTI-B7-H3 ANTIBODIES

The present disclosure relates to antibody-drug conjugates (ADCs) wherein one or more active agents are conjugated to an anti-B7-H3 antibody through a linker. The linker may comprise a unit that covalently links active agents to the antibody. The disclosure further relates to monoclonal antibodies and antigen binding fragments, variants, multimeric versions, or bispecifics thereof that specifically bind B7-H3, as well as methods of making and using these anti-B7-H3 antibodies and antigen-binding fragments thereof in a variety of therapeutic, diagnostic and prophylactic indications

Fluorescent probe for simultaneously detecting pH values of beta-galactosidase and lysosome as well as preparation method and application of fluorescent probe

The invention discloses a compound shown in a structural general formula (I) and a preparation method thereof, the compound can simultaneously detect pH of beta-galactosidase and lysosome, the compound is a single-molecule ratio type two-dimensional fluor

COMPOUNDS COMPRISING CLEAVABLE LINKER AND USES THEREOF

Provided are a compound including a cleavable linker, a use thereof, and an intermediate compound for preparing the same, and more particularly, the compound including a cleavable linker of the present invention may include an active agent (for example, a drug, a toxin, a ligand, a probe for detection, etc.) having a specific function or activity, a SO2 functional group which is capable of selectively releasing the active agent, and a functional group which triggers a chemical reaction, a physicochemical reaction and/or a biological reaction by external stimulation, and may further include a ligand (for example, oligopeptide, polypeptide, antibody, etc.) having binding specificity for a desired target receptor.

A General Approach to Enzyme-Responsive Liposomes

Liposomes are effective nanocarriers due to their ability to deliver encapsulated drugs to diseased cells. Nevertheless, liposome delivery would be improved by enhancing the ability to control the release of contents at the target site. While various stimuli have been explored for triggering liposome release, enzymes provide excellent targets due to their common overexpression in diseased cells. We present a general approach to enzyme-responsive liposomes exploiting targets that are commonly aberrant in disease, including esterases, phosphatases, and β-galactosidases. Responsive lipids correlating with each enzyme family were designed and synthesized bearing an enzyme substrate moiety attached via a self-immolating linker to a non-bilayer lipid scaffold, such that enzymatic hydrolysis triggers lipid decomposition to disrupt membrane integrity and release contents. Liposome dye leakage assays demonstrated that each enzyme-responsive liposome yielded significant content release upon enzymatic treatment compared to minimal release in controls. Results also showed that fine-tuning liposome composition was critical for controlling release. DLS analysis showed particle size increases in the cases of esterase- and β-galactosidase-responsive lipids, supporting alterations to membrane properties. These results showcase an effective modular strategy that can be tailored to target different enzymes, providing a promising new avenue for advancing liposomal drug delivery.