68858-20-8Relevant articles and documents
Self-assembly and anion-response of azobenzene-based L-valinamide derivative
Li, Kechang,Xue, Pengchong
, p. 206 - 212 (2018)
An azobenzene-based L-valinamide derivative was synthesized, and its gelation ability and self-assembly in organic solvents were investigated. Results suggested that it is an excellent gelator and formed organogels in many solvents, such as 3-pentanone, aniline, o-dichlorobenzene (ODCB), CH2Cl2, THF, ethanol, DMSO, and DMF. Its self-assembly in ODCB gel was studied. Transmission electron microscopic observation suggested that the gelator can self-assemble into one-dimensional nanofibers in the gel, and this phenomenon is driven by hydrogen bonding between amide units and π-π interaction between azobenzene moieties. With the increase in gelator concentration, the gel-to-sol phase transition temperature increased and the gelation time of the solvent shortened. Moreover, the gel exhibit anion response. A gel-to-sol phase transition was found after fluoride anion was added, exhibiting selective response to F?.
COMPOUNDS, COMPOSITIONS, METHODS, AND USES FOR TREATING CANCER AND IMMUNOLOGICAL DISORDERS
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Paragraph 0546; 0551-0552, (2020/02/06)
The present disclosure provides novel polypeptide-therapeutic compound or hormone-therapeutic compound conjugates using cleavable or non-cleavable linkers, whereby the polypeptide or hormone serves to target specific cells using receptor expression on the targeted cell to bind the ligand (polypeptide or hormone) carrying the therapeutic compound unlike antibody drug conjugates. Upon binding, the ligand and the therapeutic compound (multiples of the therapeutic compound in some embodiments) enter the cell by receptor-mediated endocytosis, and release drugs conjugated to the ligand by linkers, to interact with intracellular components to enhance, restore, or block a signal transduction process. The ligands for the polypeptide-therapeutic compound or hormone-therapeutic compound conjugates include, but are not limited to: cytokines, growth factors and hormones among other proteins with corresponding cell surface specific receptors. The disorders targeted by such polypeptide-therapeutic compound or hormone-therapeutic compound conjugates include, but are not limited to: immunological disorders (e.g., allergy and autoimmune disorders) and cancer.
Unwanted hydrolysis or α/β-peptide bond formation: How long should the rate-limiting coupling step take?
Goldschmidt G?z, Viktória,Nagy, Adrienn,Farkas, Viktor,Keszei, Ern?,Perczel, András
, p. 30720 - 30728 (2019/10/28)
Nowadays, in Solid Phase Peptide Synthesis (SPPS), being either manual, automated, continuous flow or microwave-assisted, the reaction with various coupling reagents takes place via in situ active ester formation. In this study, the formation and stability of these key active esters were investigated with time-resolved 1H NMR by using the common PyBOP/DIEA and HOBt/DIC coupling reagents for both α- and β-amino acids. Parallel to the amide bond formation, the hydrolysis of the α/β-active esters, a side reaction that is a considerable efficacy limiting factor, was studied. Based on the chemical nature/constitution of the active esters, three amino acid categories were determined: (i) the rapidly hydrolyzing ones (t 24 h) in solution. The current insight into the kinetics of this key hydrolysis side reaction serves as a guide to optimize the coupling conditions of α- and β-amino acids, thereby saving time and minimizing the amounts of reagents and amino acids to be used-all key factors of more environmentally friendly chemistry.