170434-11-4Relevant academic research and scientific papers
Non-natural amino acid and application thereof in protein site-specific modification and protein interaction
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Paragraph 0131-0133, (2021/02/13)
The invention relates to a non-natural amino acid compound represented by a general formula (I) and a preparation method thereof, and applications of the non-natural amino acid compound in fixed-pointmodification of bio-macro-molecular proteins, protein i
Terphenyl-Based Small-Molecule Inhibitors of Programmed Cell Death-1/Programmed Death-Ligand 1 Protein-Protein Interaction
Muszak, Damian,Surmiak, Ewa,Plewka, Jacek,Magiera-Mularz, Katarzyna,Kocik-Krol, Justyna,Musielak, Bogdan,Sala, Dominik,Kitel, Radoslaw,Stec, Malgorzata,Weglarczyk, Kazimierz,Siedlar, Maciej,D?mling, Alexander,Skalniak, Lukasz,Holak, Tad A.
supporting information, p. 11614 - 11636 (2021/08/20)
We describe a new class of potent PD-L1/PD-1 inhibitors based on a terphenyl scaffold that is derived from the rigidified biphenyl-inspired structure. Using in silico docking, we designed and then experimentally demonstrated the effectiveness of the terphenyl-based scaffolds in inhibiting PD-1/PD-L1 complex formation using various biophysical and biochemical techniques. We also present a high-resolution structure of the complex of PD-L1 with one of our most potent inhibitors to identify key PD-L1/inhibitor interactions at the molecular level. In addition, we show the efficacy of our most potent inhibitors in activating the antitumor response using primary human immune cells from healthy donors.
PYRAZOLOPYRIMIDIN-2-YL DERIVATIVES AS JAK INHIBITORS
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Page/Page column 103, (2015/06/25)
New pyrazolopyridmiin-2-yl derivatives are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
Water-promoted ortho-selective monohydroxymethylation of phenols in the NaBO2 system
Li, Hui-Jing,Wu, Ying-Ying,Wu, Qin-Xi,Wang, Rui,Dai, Chun-Yang,Shen, Zhi-Lun,Xie, Cheng-Long,Wu, Yan-Chao
, p. 3100 - 3107 (2014/05/06)
Water-promoted ortho-selective monohydroxymethylation of phenols in the NaBO2 system generates salicyl alcohols in 65-97% yields. A remarkable rate-enhancement by water was observed, and NaBO2 appeared to serve the dual role of a suitable base and an efficient chelating reagent. This protocol possesses many advantages such as short reaction times, expanded substrate scope, and high mono- and regio-selectivities. The experimental results were explained by the calculations based on local ionisation energy minima, leading to a possible reaction mechanism.
ANTIDIABETIC BICYCLIC COMPOUNDS
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Page/Page column 128, (2014/09/03)
Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
SUBSTITUTED SPIROCYCLIC PIPERIDINE DERIVATIVES AS HISTAMINE-3 (H3) RECEPTOR LIGANDS
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Page/Page column 59, (2009/09/05)
The present invention provides compounds of Formula (I): their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceuticals compositions thereof.
