Výsledky vyhledávání - "Joseph L, Duffy"

Akademický článek

Inhibition of O-GlcNAcase leads to elevation of O-GlcNAc tau and reduction of tauopathy and cerebrospinal fluid tau in rTg4510 mice

Publikováno v: Molecular Neurodegeneration, Vol 12, Iss 1, Pp 1-16 (2017)

Abstract Background Hyperphosphorylation of microtubule-associated protein tau is a distinct feature of neurofibrillary tangles (NFTs) that are the hallmark of neurodegenerative tauopathies. O-GlcNAcylation is a lesser known post-translational modifi

Externí odkaz: https://doaj.org/article/1ce645702743455b9fc3c2ca7c604062

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Discovery of Ethyl Ketone-Based Highly Selective HDACs 1, 2, 3 Inhibitors for HIV Latency Reactivation with Minimum Cellular Potency Serum Shift and Reduced hERG Activity

Autor: James I. Fells, Wensheng Yu, Younong Yu, Richard J. O. Barnard, Christine C. Chung, Bonnie J. Howell, Shouning Xu, Daniel J. Klein, Joseph A. Kozlowski, Joseph L. Duffy, Dane Clausen, Jian Liu, M. Katharine Holloway, Robert W. Myers, Guoxin Wu, Takao Suzuki, Lin Deng, Jin Wu, Ming Wang

Publikováno v: Journal of Medicinal Chemistry. 64:4709-4729

We describe the discovery of histone deacetylase (HDACs) 1, 2, and 3 inhibitors with ethyl ketone as the zinc-binding group. These HDACs 1, 2, and 3 inhibitors have good enzymatic and cellular activity. Their serum shift in cellular potency has been

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a4c8b7b2d8a7b239d36c3d11df82ab88
https://doi.org/10.1021/acs.jmedchem.0c02150

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Mild Condition for the Deoxygenation of α-Heteroaryl-Substituted Methanol Derivatives

Autor: Wensheng Yu, Maofen Chen, Takao Suzuki, Zhiqi Qi, Bin Hu, Jianming Bao, John S. Debenham, Na Meng, Joseph L. Duffy, Robert Mazzola

Publikováno v: The Journal of Organic Chemistry. 86:5560-5567

A mild condition via PPh3/I2/imidazole for the deoxygenation of substituted methanol derivatives has been identified. This metal-free process was found to proceed well on secondary or tertiary alcohols substituted with one or two heteroaryl groups, a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b6e46bfea57fcf3b5d4f09671845422e
https://doi.org/10.1021/acs.joc.1c00067

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Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2-Substituted Benzamide Zinc Binding Group

Autor: Wensheng Yu, Deyou Sha, Abdul-Basit Alhassan, Joseph Kelly, Joseph L. Duffy, M. Katharine Holloway, Bonnie J. Howell, Joseph A. Kozlowski, Jian Liu, Richard J. O. Barnard, Milana Maletic, Daniel J. Klein, Scott E. Wolkenberg, Steve S. Carroll, Younong Yu

Publikováno v: ACS Med Chem Lett

[Image: see text] The selectivity of histone deacetylase inhibitors (HDACis) is greatly impacted by the zinc binding groups. In an effort to search for novel zinc binding groups, we applied a parallel medicinal chemistry (PMC) strategy to quickly syn

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b8cfd7d537a63ac4577faba274ff15e5
https://doi.org/10.1021/acsmedchemlett.0c00462

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Pharmacological Characterization of the Novel and Selective α7 Nicotinic Acetylcholine Receptor–Positive Allosteric Modulator BNC375

Autor: Joshua D. Vardigan, Anton A. Grishin, Fiona Thomson, Michelle Pearson, Joseph L. Duffy, Corin O. Miller, Jason M. Uslaner, Xiaoping Zhou, Christopher Daley, Andrew John Harvey, Sue O'connor, Lee Warren, Ian M. Bell, Carolyn J. Coles, Michelle Belden, Henry S. Lange, Xiaohai Wang, Vanita Gakhar

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 373:311-324

Treatments for cognitive deficits associated with central nervous system (CNS) disorders such as Alzheimer disease and schizophrenia remain significant unmet medical needs that incur substantial pressure on the health care system. The α7 nicotinic a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::9c3e2e8af05e10d005297f7acb0e5f63
https://doi.org/10.1124/jpet.119.263483

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Cholesteryl ester transfer protein (CETP) inhibitors based on cyclic urea, bicyclic urea and bicyclic sulfamide cores

Autor: Kaushik Mitra, Anne-Marie Cumiskey, Beth Ann Murphy, Qiaolin Deng, Deodial Guiadeen, Douglas G. Johns, Wanying Sun, Joseph L. Duffy, Arto D. Krikorian, Ruth A. Duffy, Patrick P. Shao, Petr Vachal, Jian Liu

Publikováno v: Bioorganicmedicinal chemistry letters. 32

Cholesteryl ester transfer protein (CETP) inhibitors reduce the transfer of cholesteryl esters from the high-density lipoprotein (HDL-C) to apolipoprotein such as VLDL/LDL, with exchange of triglycerides. Thus, this inhibition increases the HDL-C lev

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7da9a02fbe73b1ba256c4a4723c4306f
https://pubmed.ncbi.nlm.nih.gov/33161125

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Selective Class I HDAC Inhibitors Based on Aryl Ketone Zinc Binding Induce HIV-1 Protein for Clearance

Autor: Joseph L. Duffy, James I. Fells, Younong Yu, Bonnie J. Howell, Hyunjin M. Kim, Wensheng Yu, Dane Clausen, M. Katharine Holloway, Christine C. Chung, Robert W. Myers, Jin Wu, Richard J. O. Barnard, Daniel J. Klein, Joseph A. Kozlowski, Steve S. Carroll, Guoxin Wu, Jian Liu, Joseph Kelly

Publikováno v: ACS Med Chem Lett

[Image: see text] HIV persistence in latently infected, resting CD4(+) T cells is broadly considered a barrier to eradicate HIV. Activation of the provirus using latency-reversing agents (LRAs) followed by immune-mediated clearance to purge reservoir

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::525b4192080895b98514a52d14d59d11
https://europepmc.org/articles/PMC7357218/

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Selective N7 Alkylation of 7-Azaindazoles

Autor: Bin Hu, Song Yang, Salman Jabri, Lianyun Zhao, Joseph L. Duffy, Weichen Jin, Jianming Bao, Wensheng Yu, Christopher Joseph Sinz, Zhiyu Lei, Chen Cheng

Publikováno v: The Journal of organic chemistry. 85(11)

A general and mild procedure for alkylation of 7-azaindazoles at the N7 position using alkyl halides in butanone is reported, which requires no additives such as acids or bases. The scope of the reaction regarding substituents on 7-azaindazoles and t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b39221df48cdc2d393b1c1cbc3c4afa9
https://pubmed.ncbi.nlm.nih.gov/32362114

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