Výsledky vyhledávání - "Chad. S. Hewitt"

Akademický článek

Structure-activity relationship studies for inhibitors for vancomycin-resistant Enterococcus and human carbonic anhydrases

Autor: Weiwei An, Katrina J. Holly, Alessio Nocentini, Ryan D. Imhoff, Chad. S. Hewitt, Nader S. Abutaleb, Xufeng Cao, Mohamed N. Seleem, Claudiu T. Supuran, Daniel P. Flaherty

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 1838-1844 (2022)

Vancomycin-resistant enterococci (VRE), consisting of pathogenic Enterococcus faecalis and E. faecium, is a leading cause of hospital-acquired infections (HAIs). We recently repurposed the FDA-approved human carbonic anhydrase (CA) inhibitor acetazol

Externí odkaz: https://doaj.org/article/289046e46d9a42fe9840d656ae4ed36e

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Coumarins effectively inhibit bacterial α-carbonic anhydrases

Autor: Simone Giovannuzzi, Chad S. Hewitt, Alessio Nocentini, Clemente Capasso, Daniel P. Flaherty, Claudiu T. Supuran

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 333-338 (2022)
Journal of Enzyme Inhibition and Medicinal Chemistry
article-version (VoR) Version of Record

Coumarins are known to act as prodrug inhibitors of mammalian α-carbonic anhydrases (CAs, EC 4.2.1.1) but they were not yet investigated for the inhibition of bacterial α-CAs. Here we demonstrate that such enzymes from the bacterial pathogens Neiss

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::94dc358b1dab05167ca2d2b6bd41f2c6
https://doaj.org/article/28b2248586f446c9ba2b17701ba77732

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Repurposing FDA-approved sulphonamide carbonic anhydrase inhibitors for treatment of Neisseria gonorrhoeae

Autor: Nader S. Abutaleb, Ahmed E. M. Elhassanny, Alessio Nocentini, Chad S. Hewitt, Ahmed Elkashif, Bruce R. Cooper, Claudiu T. Supuran, Mohamed N. Seleem, Daniel P. Flaherty

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 51-61 (2022)

Neisseria gonorrhoeae is a high-priority pathogen of concern due to the growing prevalence of resistance development against approved antibiotics. Herein, we report the anti-gonococcal activity of ethoxzolamide, the FDA-approved human carbonic anhydr

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5014c4847d7ad81c22e1c78e47fa19ea
https://doaj.org/article/908f9289255d400d818e259d8b402431

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Dithiocarbamates effectively inhibit the α-carbonic anhydrase from Neisseria gonorrhoeae

Autor: Simone Giovannuzzi, Nader S. Abutaleb, Chad S. Hewitt, Fabrizio Carta, Alessio Nocentini, Mohamed N. Seleem, Daniel P. Flaherty, Claudiu T. Supuran

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 1-8 (2022)

Recently, inorganic anions and sulphonamides, two of the main classes of zinc-binding carbonic anhydrase inhibitors (CAIs), were investigated for inhibition of the alpha-class carbonic anhydrase (CA, EC 4.2.1.1) from Neisseria gonorrhoeae, NgCA. As a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::77621c902506f0ac0b7d3a153e3617f1
https://doi.org/10.1080/14756366.2021.1988945

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Structure–Activity Relationship Studies of Acetazolamide-Based Carbonic Anhydrase Inhibitors with Activity against Neisseria gonorrhoeae

Autor: Amanda L. Graboski, Xufeng Cao, Yehia Elgammal, Devon P. Amos, Molly S. Youse, Alessio Nocentini, Nader S. Abutaleb, Anil Kumar Marapaka, Weiwei An, Mohamed N. Seleem, Claudiu T. Supuran, Ahmed E. M. Elhassanny, Katrina J. Holly, Chad S. Hewitt, Daniel P. Flaherty, Jatinder Kaur, Aaron D Krabill, Ahmed Elkashif

Publikováno v: ACS Infectious Diseases. 7:1969-1984

Neisseria gonorrhoeae is an urgent threat to public health in the United States and around the world. Many of the current classes of antibiotics to treat N. gonorrhoeae infection are quickly becoming obsolete due to increased rates of resistance. Thu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::506c99f38b00123de518cee832d6beb7
https://doi.org/10.1021/acsinfecdis.1c00055

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Anion inhibition studies of the α-carbonic anhydrases from Neisseria gonorrhoeae

Autor: Alessio Nocentini, Margaret D. Mastrolorenzo, Chad S. Hewitt, Daniel P. Flaherty, Claudiu T. Supuran

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 36, Iss 1, Pp 1061-1066 (2021)
Journal of Enzyme Inhibition and Medicinal Chemistry
article-version (VoR) Version of Record

The bacterial pathogen Neisseria gonorrhoeae encodes for an α-class carbonic anhydrase (CA, EC 4.2.1.1), NgCA, which was investigated for its inhibition with a series of inorganic and organic anions. Perchlorate and hexafluorophosphate did not signi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::37f684d0cec532b31e020eaf5b56248d
https://doaj.org/article/17b4898b97d74981b8db84dbdf49ee91

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Development of Ubiquitin Variants with Selectivity for Ubiquitin C-Terminal Hydrolase Deubiquitinases

Autor: Chittaranjan Das, Chad S. Hewitt, Daniel P. Flaherty, Aaron D Krabill

Publikováno v: Biochemistry. 59:3447-3462

Ubiquitin (Ub) is a highly conserved protein that is covalently attached to substrate proteins as a post-translational modification to regulate signaling pathways such as proteasomal degradation and cell cycle/transcriptional regulation in the eukary

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9e9f41cc7584c01b8dc249f24b3e0698
https://doi.org/10.1021/acs.biochem.9b01076

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Inhibition studies of bacterial α-carbonic anhydrases with phenols

Autor: Simone Giovannuzzi, Chad S. Hewitt, Alessio Nocentini, Clemente Capasso, Gabriele Costantino, Daniel P. Flaherty, Claudiu T. Supuran

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 37, Iss 1, Pp 666-671 (2022)

The α-class carbonic anhydrases (CAs, EC 4.2.1.1) from the bacterial pathogens Neisseria gonorrhoeae (NgCAα) and Vibrio cholerae (VchCAα) were investigated for their inhibition by a panel of phenols and phenolic acids. Mono-, di- and tri-substitut

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b05c14a4297fb128aae992cc88f5c8e7
https://pubmed.ncbi.nlm.nih.gov/35139743

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Repurposing FDA-approved sulphonamide carbonic anhydrase inhibitors for treatment of

Autor: Nader S, Abutaleb, Ahmed E M, Elhassanny, Alessio, Nocentini, Chad S, Hewitt, Ahmed, Elkashif, Bruce R, Cooper, Claudiu T, Supuran, Mohamed N, Seleem, Daniel P, Flaherty

Publikováno v: Journal of Enzyme Inhibition and Medicinal Chemistry
article-version (VoR) Version of Record

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::7e6f5cfcfd105610438db11b3b65bef6
https://pubmed.ncbi.nlm.nih.gov/34894972

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Rational Development and Characterization of a Ubiquitin Variant with Selectivity for Ubiquitin C-Terminal Hydrolase L3

Autor: Chad S. Hewitt, Chittaranjan Das, Daniel P. Flaherty

Publikováno v: Biomolecules
Biomolecules; Volume 12; Issue 1; Pages: 62
Biomolecules, Vol 12, Iss 62, p 62 (2022)

There is currently a lack of reliable methods and strategies to probe the deubiquitinating enzyme UCHL3. Current small molecules reported for this purpose display reduced potency and selectivity in cellular assays. To bridge this gap and provide an a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3f28cc44ccc081ea285e610c659f92bb
https://pubmed.ncbi.nlm.nih.gov/35053210

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