Zobrazeno 1 - 10
of 90
pro vyhledávání: '"Thomas D, Meek"'
Autor:
Jiyun Zhu, Linfeng Li, Aleksandra Drelich, Bala C. Chenna, Drake M. Mellott, Zane W. Taylor, Vivian Tat, Christopher Z. Garcia, Ardala Katzfuss, Chien-Te K. Tseng, Thomas D. Meek
Publikováno v:
Frontiers in Chemistry, Vol 10 (2022)
Cysteine proteases comprise an important class of drug targets, especially for infectious diseases such as Chagas disease (cruzain) and COVID-19 (3CL protease, cathepsin L). Peptide aldehydes have proven to be potent inhibitors for all of these prote
Externí odkaz:
https://doaj.org/article/83d373bc5b624e3288eb3d76ea8c126b
Publikováno v:
PLoS Neglected Tropical Diseases, Vol 16, Iss 2, p e0009926 (2022)
Human African Trypanosomiasis (HAT), also known as sleeping sickness, is a Neglected Tropical Disease endemic to 36 African countries, with approximately 70 million people currently at risk for infection. Current therapeutics are suboptimal due to to
Externí odkaz:
https://doaj.org/article/8ecb1189bbf841f5bef22a3e772a75bd
Autor:
Kayla Glockzin, Demetrios Kostomiris, Yacoba V. T. Minnow, Kajitha Suthagar, Keith Clinch, Sinan Gai, Joshua N. Buckler, Vern L. Schramm, Peter C. Tyler, Thomas D. Meek, Ardala Katzfuss
Publikováno v:
Biochemistry. 61:2088-2105
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::096601ad40718831ebb2727725e2e636
https://doi.org/10.1021/acs.biochem.2c00312
https://doi.org/10.1021/acs.biochem.2c00312
Autor:
Anthony J. O’Donoghue, Michael C Yoon, Max J. Bedding, Vivian Hook, Pavla Fajtová, Arthur H Tang, Mark Larance, Linfeng Li, Chien-Te Tseng, Stuart Turville, James H. McKerrow, Dustin Pwee, Laura Beretta, Alexander Stoye, Danielle E. Skinner, William H. Gerwick, Anneliese S. Ashhurst, Thomas D. Meek, Anupriya Aggarwal, Aleksandra Drelich, Richard J. Payne
Publikováno v:
bioRxiv
Cathepsin L is a key host cysteine protease utilized by coronaviruses for cell entry and is a promising drug target for novel antivirals against SARS-CoV-2. The marine natural product gallinamide A and several synthetic analogues were identified as p
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::66e9010452bb0a2bc93e68d7e3db2d8a
https://doi.org/10.1021/acs.jmedchem.1c01494
https://doi.org/10.1021/acs.jmedchem.1c01494
Autor:
Scott A. Cameron, Lawrence Harris, Arthur Laganowsky, Zahra Moghadamchargari, Dan Torres, James C. Sacchettini, Inna Krieger, Thomas D. Meek, Drake M. Mellott
Publikováno v:
Journal of the American Chemical Society. 143:17666-17676
The isocitrate lyase paralogs of Mycobacterium tuberculosis (ICL1 and 2) are essential for mycobacterial persistence and constitute targets for the development of antituberculosis agents. We report that (2R,3S)-2-hydroxy-3-(nitromethyl)succinic acid
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c351d3ec7a29a2edb7258f6679913f0a
https://doi.org/10.1021/jacs.1c07970
https://doi.org/10.1021/jacs.1c07970
Autor:
Thomas D. Meek
Publikováno v:
Burger's Medicinal Chemistry and Drug Discovery
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::54fabe28b35f2d702f02b0e24a981317
https://doi.org/10.1002/0471266949.bmc260
https://doi.org/10.1002/0471266949.bmc260
Autor:
Aleksandra Drelich, Miriam A. Giardini, Pavla Fajtová, Drake M. Mellott, Vivian Hook, Thomas D. Meek, Jason C. Hsu, Demetrios H. Kostomiris, Aaron F. Carlin, Frank M. Raushel, Klaudia I. Kocurek, Jair L. Siqueira-Neto, Zane W. Taylor, Anthony J. O’Donoghue, Felix W Frueh, Jiyun Zhu, Ardala Katzfuss, Chien Te K. Tseng, Sungjun Beck, Hong Wang, Brett L. Hurst, Laura Beretta, Ken Hirata, James H. McKerrow, Alex E. Clark, Linfeng Li, Daniel C Maneval, Danielle E. Skinner, Balachandra Chenna, Vivian Tat, Michael C Yoon
Publikováno v:
ACS Chemical Biology. 16:642-650
Host-cell cysteine proteases play an essential role in the processing of the viral spike protein of SARS coronaviruses. K777, an irreversible, covalent inactivator of cysteine proteases that has recently completed phase 1 clinical trials, reduced SAR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::ef76261f31ca7bfffc0f062695cd8aeb
https://doi.org/10.1021/acschembio.0c00875
https://doi.org/10.1021/acschembio.0c00875
Autor:
Thomas D. Meek, Drake M. Mellott, Truc Viet Pham, Inna Krieger, Zahra Moghadamchargari, Kevin Chen, James C. Sacchettini, Arthur Laganowsky
Publikováno v:
ACS Chemical Biology. 16:463-470
The isocitrate lyases (ICL1/2) are essential enzymes of Mycobacterium tuberculosis (Mtb), the causative agent of tuberculosis. At present, no ICL1/2 inhibitors have progressed to clinical evaluation, despite extensive drug discovery efforts. Herein,
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::5dfbb8c22455b348ac4f277806bb4fa3
https://doi.org/10.1021/acschembio.0c00740
https://doi.org/10.1021/acschembio.0c00740
Autor:
Zane W. Taylor, Marcetta Y. Darensbourg, Drake M. Mellott, Thomas D. Meek, Christopher R DeLaney, Ardala Katzfuss, Jiyun Zhu, D Chase Pectol
Publikováno v:
Chemical Communications. 57:8352-8355
By repurposing DNICs designed for other medicinal purposes, the possibility of protease inhibition was investigated in silico using AutoDock 4.2.6 (AD4) and in vitro via a FRET protease assay. AD4 was validated as a predictive computational tool for
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a7ce972e690c2e08a2572c6ece48eafe
https://doi.org/10.1039/d1cc03103a
https://doi.org/10.1039/d1cc03103a
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 376:106-117
The active form of transforming growth factor-β1 (TGF-β1) plays a key role in potentiating fibrosis. TGF-β1 is sequestered in an inactive state by a latency-associated glycopeptide (LAP). Sialidases (also called neuraminidases (NEU)) cleave termin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::127abc4058564d421a5f5b1615d3c8a0
https://doi.org/10.1124/jpet.120.000258
https://doi.org/10.1124/jpet.120.000258