Výsledky vyhledávání - "Jonathan B Baell"

Akademický článek

Identification of compounds with anti-proliferative activity against Trypanosoma brucei brucei strain 427 by a whole cell viability based HTS campaign.

Autor: Melissa L Sykes, Jonathan B Baell, Marcel Kaiser, Eric Chatelain, Sarah R Moawad, Danny Ganame, Jean-Robert Ioset, Vicky M Avery

Publikováno v: PLoS Neglected Tropical Diseases, Vol 6, Iss 11, p e1896 (2012)

Human African Trypanosomiasis (HAT) is caused by two trypanosome sub-species, Trypanosoma brucei rhodesiense and Trypanosoma brucei gambiense. Drugs available for the treatment of HAT have significant issues related to difficult administration regime

Externí odkaz: https://doaj.org/article/89a7928a2afc4ed9b42b742e35074888

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Akademický článek

A small molecule inhibitor of PTP1B and PTPN2 enhances T cell anti-tumor immunity

Autor: Shuwei Liang, Eric Tran, Xin Du, Jiajun Dong, Harrison Sudholz, Hao Chen, Zihan Qu, Nicholas D. Huntington, Jeffrey J. Babon, Nadia J. Kershaw, Zhong-Yin Zhang, Jonathan B. Baell, Florian Wiede, Tony Tiganis

Publikováno v: Nature Communications, Vol 14, Iss 1, Pp 1-27 (2023)

Abstract The inhibition of protein tyrosine phosphatases 1B (PTP1B) and N2 (PTPN2) has emerged as an exciting approach for bolstering T cell anti-tumor immunity. ABBV-CLS-484 is a PTP1B/PTPN2 inhibitor in clinical trials for solid tumors. Here we hav

Externí odkaz: https://doaj.org/article/0cb5e14e733040fe85a8642c25963be7

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Akademický článek

Reference compounds for characterizing cellular injury in high-content cellular morphology assays

Publikováno v: Nature Communications, Vol 14, Iss 1, Pp 1-16 (2023)

Cellular nuisance compounds are a burden in chemical biology and drug screening. Here the authors profile prototypical cytotoxic and nuisance compounds using the cell painting assay to systematically characterise cellular morphologies associated with

Externí odkaz: https://doaj.org/article/a0652f03d5554808827f7867140b6ae5

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Akademický článek

Novel Perspectives on the Design and Development of a Long-Acting Subcutaneous Raltegravir Injection for Treatment of HIV—In Vitro and In Vivo Evaluation

Autor: Heba S. Abd-Ellah, Ramesh Mudududdla, Glen P. Carter, Jonathan B. Baell

Publikováno v: Pharmaceutics, Vol 15, Iss 5, p 1530 (2023)

Antiretrovirals (ARVs) are a highly effective therapy for treatment and prevention of HIV infection, when administered as prescribed. However, adherence to lifelong ARV regimens poses a considerable challenge and places HIV patients at risk. Long-act

Externí odkaz: https://doaj.org/article/94384584fd5f4aa5bf15e2bd634b06a2

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Akademický článek

Design, Development, and Optimisation of Smart Linker Chemistry for Targeted Colonic Delivery—In Vitro Evaluation

Autor: Heba S. Abd-Ellah, Ramesh Mudududdla, Glen P. Carter, Jonathan B. Baell

Publikováno v: Pharmaceutics, Vol 15, Iss 1, p 303 (2023)

Drug targeting is necessary to deliver drugs to a specific site of action at a rate dictated by therapeutic requirements. The pharmacological action of a drug can thereby be optimised while minimising adverse effects. Numerous colonic drug delivery s

Externí odkaz: https://doaj.org/article/f5c66296317f42a89799f9685098aeb0

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Electrochemical Synthesis of Polysubstituted Sulfonated Pyrazoles via Cascade Intermolecular Condensation, Radical–Radical Cross Coupling Sulfonylation, and Pyrazole Annulation

Autor: Jiajun Feng, Yuzhi Wang, Luoyu Gao, Yang Yu, Jonathan B. Baell, Fei Huang

Publikováno v: The Journal of Organic Chemistry. 87:13138-13153

Electrochemical synthesis of polysubstituted sulfonated pyrazoles from enaminones and sulfonyl hydrazides was established under metal-free, exogenous-oxidant-free, and mild conditions. By judicious choice of different electrochemical reaction conditi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::73ac178dc4f23fbd124f1892c2638b5b
https://doi.org/10.1021/acs.joc.2c01609

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Visible light-induced borylation and arylation of small organic molecules using carbon dots

Autor: Tiantong He, Heping Wei, Yuanbo Zhou, Li-ya Jiang, Jonathan B. Baell, Yang Yu, Fei Huang

Publikováno v: Organic Chemistry Frontiers.

Efficient synthetic protocols for borylation of haloarenes and arylation of heteroarenes using nonmetal-doped CDots as metal-free photocatalysts under visible-light irradiation at room temperature are reported.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::bf53c02c8248db912a1fc20706b842b1
https://doi.org/10.1039/d3qo00458a

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Discovery of Anti‐tubercular Analogues of Bedaquiline with Modified A‐, B‐ and C‐Ring Subunits

Autor: Lisa Barbaro, Gayathri Nagalingam, James A. Triccas, Lendl Tan, Nicholas P. West, Daniel L. Priebbenow, Jonathan B. Baell

Publikováno v: ChemMedChem. 18

To date, the clinical use of the anti-tubercular therapy bedaquiline has been somewhat limited due to safety concerns. Recent investigations determined that modification of the B- and C-ring units of bedaquiline delivered new diarylquinolines (for ex

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::badb44da4195461af288f3ab13ded42a
https://doi.org/10.1002/cmdc.202200533

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