Výsledky vyhledávání

Identification and bioevaluation of SRI-12742 as an antimicrobial agent against multidrug-resistant Acinetobacter baumannii

Autor: Tran Tran, Karen Matsuyama, Leyi Gong, Isha Soni, Manjulika Shukla, Sidharth Chopra, Mary J. Tanga

Publikováno v: International Journal of Antimicrobial Agents. 52:22-27

Multidrug-resistant Acinetobacter baumannii (MDR-Ab) is one of the most significant nosocomial pathogens that is being increasingly isolated in healthcare settings worldwide. Owing to its inherent drug-resistant nature, coupled with its ability to re

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::baf1474392492b2709fdc8e4556dda26
https://doi.org/10.1016/j.ijantimicag.2018.02.018

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Short Communication: Preferential Killing of HIV Latently Infected CD4+T Cells by MALT1 Inhibitor

Autor: Tony T. Wang, Leyi Gong, Mingui Fu, Hui He, Hongmei Li

Publikováno v: AIDS Research and Human Retroviruses. 32:174-177

We report that the addition of an host paracaspase MALT1 inhibitor, MI-2, to HIV latently infected ACH-2, Jurkat E4, and J-LAT cells accelerated cell death in the presence of cell stimuli or the protein kinase C agonist, bryostatin 1. MI-2-mediated c

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5095c3ce2443310e0f6fd481fea64b5c
https://doi.org/10.1089/aid.2015.0343

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Discovery of N-[4-[6-tert-Butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide (RG7109), a Potent Inhibitor of the Hepatitis C Virus NS5B Polymerase

Publikováno v: Journal of Medicinal Chemistry. 57:1914-1931

In the past few years, there have been many advances in the efforts to cure patients with hepatitis C virus (HCV). The ultimate goal of these efforts is to develop a combination therapy consisting of only direct-antiviral agents (DAAs). In this paper

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5f8b3c89c500a0233782f42b5f71c4d4
https://doi.org/10.1021/jm401329s

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Development of amino-pyrimidine inhibitors of c-Jun N-terminal kinase (JNK): Kinase profiling guided optimization of a 1,2,3-benzotriazole lead

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 23:1486-1492

A series of amino-pyrimidines was developed based upon an initial kinase cross-screening hit from a CDK2 program. Kinase profiling and structure-based drug design guided the optimization from the initial 1,2,3-benzotriazole hit to a potent and select

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1b003a69164deb7db8c54e3d4d75bb7b
https://doi.org/10.1016/j.bmcl.2012.12.047

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Anti-inflammatory effects of selective glucocorticoid receptor modulators are partially dependent on up-regulation of dual specificity phosphatase 1

Autor: Jeremy Saklatvala, Philip Kong, Qize Ding, Eugenie Joanny, Andrew R. Clark, Leyi Gong

Publikováno v: British Journal of Pharmacology. 165:1124-1136

BACKGROUND AND PURPOSE It is thought that the anti-inflammatory effects of glucocorticoids (GCs) are largely due to GC receptor (GR)-mediated transrepression of NF-κB and other transcription factors, whereas side effects are caused by activation of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::7bdf19113330438bbdfb78dc9620cb78
https://doi.org/10.1111/j.1476-5381.2011.01574.x

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CCR3 antagonists: a survey of the patent literature

Autor: Leyi Gong, Robert S Wilhelm

Publikováno v: Expert Opinion on Therapeutic Patents. 19:1109-1132

Background: Since the mid-1990s, there has been significant effort invested in the discovery and clinical development of CC chemokine receptor-3 (CCR3) antagonists as potential therapeutics for airway disease. Objectives/methods: A patent literature

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f40d297aeb77d665b25fa2a3a575b87c
https://doi.org/10.1517/13543770903008544

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Pharmacological characterization of GPR120 ligands

Autor: Leyi Gong, Surendra Kumar Nayak, Bejan Rasoul, Willma Polgar, Wei Zhou, Amina S Adem, William J Thomsen

Publikováno v: The FASEB Journal. 27

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::68da50d8874229706f2ed51fca903f79
https://doi.org/10.1096/fasebj.27.1_supplement.655.9

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Development of indole/indazole-aminopyrimidines as inhibitors of c-Jun N-terminal kinase (JNK): optimization for JNK potency and physicochemical properties

Publikováno v: Bioorganicmedicinal chemistry letters. 23(12)

A novel series of indole/indazole-aminopyrimidines was designed and synthesized with an aim to achieve optimal potency and selectivity for the c-Jun kinase family or JNKs. Structure guided design was used to optimize the series resulting in a signifi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2e1d571f35d6a4f78286cd06b8fa7d5d
https://pubmed.ncbi.nlm.nih.gov/23664880

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Synthesis of the 3H-labelled 5-HT3 antagonist (RS-25259-197) at high specific activity

Autor: Leyi Gong, Howard Parnes

Publikováno v: Journal of Labelled Compounds and Radiopharmaceuticals. 38:425-433

The preparation of the title compound, a selective 5-HT 3 antagonist with anti-emetic properties, is described. The key intermediate involved is 6-bromo-1,2-dihydronaphthoic acid (5), which was synthesized from 4-bromophenylacetic acid by Micheal add

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::fdfb949798299ba6266b336de9333fd7
https://doi.org/10.1002/(sici)1099-1344(199605)38:5<425::aid-jlcr860>3.0.co

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