130111-08-9Relevant academic research and scientific papers
Targeting the APP-Mint2 Protein-Protein Interaction with a Peptide-Based Inhibitor Reduces Amyloid-β Formation
Bartling, Christian R. O.,Jensen, Thomas M. T.,Henry, Shawna M.,Colliander, Anna L.,Sereikaite, Vita,Wenzler, Marcella,Jain, Palash,Maric, Hans M.,Harps?e, Kasper,Pedersen, S?ren W.,Clemmensen, Louise S.,Haugaard-Kedstr?m, Linda M.,Gloriam, David E.,Ho, Angela,Str?mgaard, Kristian
supporting information, p. 891 - 901 (2021/02/05)
There is an urgent need for novel therapeutic approaches to treat Alzheimer's disease (AD) with the ability to both alleviate the clinical symptoms and halt the progression of the disease. AD is characterized by the accumulation of amyloid-β (Aβ) peptides
PROTEIN TYROSINE PHOSPHATASE DEGRADERS AND METHODS OF USE THEREOF
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Page/Page column 491, (2021/06/26)
Provided herein are compounds, compositions, and methods useful for degrading protein tyrosine phosphatase, e.g., protein tyrosine phosphatase non-receptor type 2 (PTPN2) and/or protein tyrosine phosphatase non-receptor type 1 (PTPN1), and for treating related diseases favorably responsive to PTPN1 or PTPN2 inhibitor treatment, e.g., a cancer 5 or a metabolic disease.
Total Synthesis of the Cyclic Depsipeptide Vioprolide D via its (Z)-Diastereoisomer
Bach, Thorsten,Grab, Hanusch A.,Kirsch, Volker C.,Sieber, Stephan A.
supporting information, p. 12357 - 12361 (2020/05/05)
The first total synthesis of vioprolide D was accomplished in an overall yield of 2.0 % starting from methyl (2S)-3-benzyloxy-2-hydroxypropanoate (16 steps in the longest linear sequence). The cyclic depsipeptide was assembled from two building blocks of
Synthesis of carbohydrate-grafted glycopolymers using a catalyst-free, perfluoroarylazide-mediated fast staudinger reaction
Ndugire, William,Wu, Bin,Yan, Mingdi
, (2019/01/21)
Glycopolymers have gained increasing importance in investigating glycan-lectin interactions, as drug delivery vehicles and in modulating interactions with proteins. The synthesis of these glycopolymers is still a challenging and rigorous exercise. In this
JAK1 SELECTIVE INHIBITORS
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Page/Page column 64; 65, (2018/08/12)
Disclosed herein are compounds of Formula (I), and pharmaceutically acceptable salts thereof, wherein R1-R8 have any of the meanings defined herein. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I) and methods of using the same.
POLYMYXIN ANALOGS USEFUL AS ANTIBIOTIC POTENTIATORS
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Paragraph 0211, (2017/12/09)
The disclosure provides compounds of the formula (I) or a tautomer thereof, or a pharmaceutically acceptable salt of either of the foregoing. The variables A, R1, and R2 are defined in the disclosure. The disclosure further includes pharmaceutical compositions comprising a compound of formula I together with at least one pharmaceutically acceptable carrier. The disclosure also includes a method of sensitizing bacteria to an antibacterial agent, comprising administering to a patient infected with the bacteria, simultaneously or sequentially, a therapeutically effective amount of the antibacterial agent and a compound of formula (I).
Facile synthesis of α-hydroxy carboxylic acids from the corresponding α-amino acids
Stuhr-Hansen, Nicolai,Padrah, Shahrokh,Str?mgaard, Kristian
supporting information, p. 4149 - 4151 (2015/02/02)
An effective and improved procedure is developed for the synthesis of α-hydroxy carboxylic acids by treatment of the corresponding protonated α-amino acid with tert-butyl nitrite in 1,4-dioxane-water. The amino moiety must be protonated and located α to a carboxylic acid function in order to undergo initial diazotization and successive hydroxylation, since neither β-amino acids nor acid derivatives such as esters and amides undergo hydroxylations. The method is successfully applied for the synthesis of 18 proteinogenic amino acids.
Facile synthesis of α-hydroxy carboxylic acids from the corresponding α-amino acids
Stuhr-Hansen, Nicolai,Padrah, Shahrokh,Str?mgaard, Kristian
supporting information, p. 4149 - 4151 (2014/07/22)
An effective and improved procedure is developed for the synthesis of α-hydroxy carboxylic acids by treatment of the corresponding protonated α-amino acid with tert-butyl nitrite in 1,4-dioxane-water. The amino moiety must be protonated and located α to a carboxylic acid function in order to undergo initial diazotization and successive hydroxylation, since neither β-amino acids nor acid derivatives such as esters and amides undergo hydroxylations. The method is successfully applied for the synthesis of 18 proteinogenic amino acids.
Glycan arrays containing synthetic Clostridium difficile lipoteichoic acid oligomers as tools toward a carbohydrate vaccine
Martin, Christopher E.,Broecker, Felix,Eller, Steffen,Oberli, Matthias A.,Anish, Chakkumkal,Pereira, Claney L.,Seeberger, Peter H.
supporting information, p. 7159 - 7161 (2013/08/23)
Clostridium difficile is a leading cause of severe nosocomial infections. Cell-surface carbohydrate antigens are promising vaccine candidates. Here we report the first total synthesis of oligomers of the lipoteichoic acid antigen repeating unit. Synthetic glycan microarrays revealed anti-glycan antibodies in the blood of patients that help to define epitopes for vaccine development.
In vitro chemoenzymatic and in vivo biocatalytic syntheses of new beauvericin analogues
Matthes, Diana,Richter, Lennart,Mueller, Jane,Denisiuk, Alexander,Feifel, Sven C.,Xu, Yuquan,Espinosa-Artiles, Patricia,Suessmuth, Roderich D.,Molnar, Istvan
supporting information; experimental part, p. 5674 - 5676 (2012/07/27)
New beauvericins have been synthesized using the nonribosomal peptide synthetase BbBEAS from the entomopathogenic fungus Beauveria bassiana. Chemical diversity was generated by in vitro chemoenzymatic and in vivo whole cell biocatalytic syntheses using ei
