60-23-1Relevant articles and documents
Fatty Acid Cysteamine Conjugates as Novel and Potent Autophagy Activators That Enhance the Correction of Misfolded F508del-Cystic Fibrosis Transmembrane Conductance Regulator (CFTR)
Vu, Chi B.,Bridges, Robert J.,Pena-Rasgado, Cecilia,Lacerda, Antonio E.,Bordwell, Curtis,Sewell, Abby,Nichols, Andrew J.,Chandran, Sachin,Lonkar, Pallavi,Picarella, Dominic,Ting, Amal,Wensley, Allison,Yeager, Maisy,Liu, Feng
, p. 458 - 473 (2017)
A depressed autophagy has previously been reported in cystic fibrosis patients with the common F508del-CFTR mutation. This report describes the synthesis and preliminary biological characterization of a novel series of autophagy activators involving fatty acid cysteamine conjugates. These molecular entities were synthesized by first covalently linking cysteamine to docosahexaenoic acid. The resulting conjugate 1 synergistically activated autophagy in primary homozygous F508del-CFTR human bronchial epithelial (hBE) cells at submicromolar concentrations. When conjugate 1 was used in combination with the corrector lumacaftor and the potentiator ivacaftor, it showed an additive effect, as measured by the increase in the chloride current in a functional assay. In order to obtain a more stable form for oral dosing, the sulfhydryl group in conjugate 1 was converted into a functionalized disulfide moiety. The resulting conjugate 5 is orally bioavailable in the mouse, rat, and dog and allows a sustained delivery of the biologically active conjugate 1.
"dual Layer" Self-Sorting with Cucurbiturils
Barbero, Héctor,Masson, Eric,Thompson, Nathan A.
, p. 867 - 873 (2020)
Platinum(II) complexes bearing terpyridyl (tpy) and thiolate ligands were used to test the design of a "dual layer" self-sorting system in the presence of Cucurbit[8]uril (CB[8]). Pt(II) thiolates and CB[8] form 2:1 assemblies, with both metallic centers sitting on top of one another at one of the macrocycle portals. We showed that any pair of these CB[8]-secured Pt(II) complex dimers bearing different tpy "heads" and thiolate "tails" scrambles to afford up to 10 ternary assemblies via two processes: (1) supramolecular exchanges (i.e., the egression and ingression of Pt complexes from and into CB[8]) and (2) ligand exchanges between the Pt thiolates. The mixtures of 10 assemblies were fully characterized by nuclear magnetic resonance spectroscopy. While the thiolate tails do not significantly affect the rate of the supramolecular exchanges, they were found to control (1) the kinetics of ligand exchange, with bulkier thiolates causing dramatic rate retardations, as well as (2) the thermodynamics of the self-sorting process, i.e., the distribution of assemblies at equilibrium, via intra-CB[8] assembly interactions between pairs of thiolates. Ligand exchanges are consistently slower than supramolecular exchanges. An associative pathway that involves the formation of dimers of CB[8]-secured Pt dimers (a total of 4 Pt complexes) during the ligand exchange process was invoked to rationalize the observed kinetics.
LINAC/LASER determination of the absolute rate constant for thiyl and hydroxyl radical reaction with sulfhydryls in aqueous solution: Mercaptoethanol, cysteamine, and N-acetyl-L-cysteine
Mezyk, Stephen P.
, p. 8295 - 8301 (1996)
The technique of combined pulse radiolysis/laser photolysis has been used to investigate the disulfide radical anion formation reactions for mercaptoethanol, cysteamine, and N-acetyl-L-cysteine over the pH range 7.0-13.0. The photolysis of the transient radical anions, formed by the one electron oxidation of the sulfhydryl, perturbs the disulfide radical anion/thiyl radical equilibrium, allowing rate constants for thiyl radical reaction with the parent sulfhydryl to be uniquely determined from the absorption bleach and subsequent recovery. These pH-dependent values were combined with measured disulfide radical anion equilibrium constants to calculate first-order disulfide radical anion dissociation rate constants. By computer modeling of established mechanisms for the disulfide radical anion growths, rate constants for the reaction of hydroxyl radicals with individual sulfhydryl species were calculated. These values are contrasted with previously reported values determined by using competition kinetics.
Non-specific reaction inhibitor, method for inhibiting non-specific reaction, and kit
-
, (2021/09/22)
Provided is a non-specific reaction inhibitor for achieving the accurate detection and quantitation of a trace component (a target substance) contained in a sample, in an immunoassay, by simply and effectively inhibiting a non-specific reaction associated with the measurement. The non-specific reaction inhibitor comprises a substance of the formula I: wherein R1 and R2 together form a double bond between carbons, to which they are respectively bonded directly, or R1 is a hydrogen atom and R2 is a group formed by removing H from an SH-group-containing compound, B is a support, and L is a spacer arm portion.
Taurine synthesis method (by machine translation)
-
Paragraph 0036; 0038; 0041; 0043; 0045; 0047; 0049; 0051, (2020/07/15)
The invention provides a taurine synthesis method, and solves the problems of by-product accumulation, high temperature and high pressure in ammonia decomposition reaction, strong strong acid and strong base in acidification and the like in an addition reaction in a traditional taurine synthesis process. The method comprises the following steps: 1) carrying out cyclization reaction of sulfur solution and ethylene contact to obtain a solution of sulfur dissolved in carbon disulfide; 2) carrying out an addition reaction with ammonia or liquid ammonia contact to obtain an amino thiol; 3) carrying out an oxidation reaction in the presence of a catalyst to obtain the crude taurine. (by machine translation)
Engineering a cleavable disulfide bond into a natural product siderophore using precursor-directed biosynthesis
Richardson-Sanchez, Tomas,Codd, Rachel
supporting information, p. 9813 - 9816 (2018/09/10)
An analogue of the bacterial siderophore desferrioxamine B (DFOB) containing a disulfide motif in the backbone was produced from Streptomyces pilosus cultures supplemented with cystamine. Cystamine competed against native 1,5-diaminopentane during assembly. DFOB-(SS)1[001] and its complexes with Fe(iii) or Ga(iii) were cleaved upon incubation with dithiothreitol. Compounds such as DFOB-(SS)1[001] and its thiol-containing cleavage products could expand antibiotic strategies and Au-S-based nanotechnologies.
TUNABLE FLUORESCENCE USING CLEAVABLE LINKERS
-
Paragraph 00118-00119, (2014/11/11)
The invention relates to cleavable chemistry in general, and in particular, to tunable fluoresence using cleavable linkers present in fluorochrome-quencher conjugates.
Thiols and selenols as electron-relay catalysts for disulfide-bond reduction
Lukesh III, John C.,VanVeller, Brett,Raines, Ronald T.
supporting information, p. 12901 - 12904 (2014/01/06)
Pass them on! Dithiobutylamine immobilized on a resin is a useful reagent for the reduction of disulfide bonds. Its ability to reduce a disulfide bond in a protein is enhanced greatly if used along with a soluble strained cyclic disulfide or mixed diselenide that relays electrons from the resin to the protein. This electron-relay catalysis system provides distinct advantages over the use of excess soluble reducing agent alone. Copyright
POLY(ORGANOPHOSPHAZENE) COMPOSITION FOR BIOMATERIALS
-
, (2013/02/28)
Provided are a use of chemically-crosslinkable, poly(organophosphazene)s for biomaterials, chemically-crosslinkable poly(organophosphazene)s with a physiologically active substance covalently-bonded thereto, a use thereof for biomaterials, and a process for preparing the same. The chemical crosslinkings can be made by UV irradiation, and/or a crosslinker, and/or an additive, and/or an enzyme, and/or a mixing of at least one polymer.
Poly(organophosphazene) composition for biomaterials
-
, (2013/02/28)
Provided are a use of chemically-crosslinkable, poly(organophosphazene)s for biomaterials, chemically-crosslinkable poly(organophosphazene)s with a physiologically active substance covalently-bonded thereto, a use thereof for biomaterials, and a process for preparing the same. The chemical crosslinkings can be made by UV irradiation, and/or a crosslinker, and/or an additive, and/or an enzyme, and/or a mixing of at least one polymer.
