Zobrazeno 1 - 10
of 12
pro vyhledávání: '"Gail M. Freiberg"'
Autor:
Tanya Parish, Lindsay Flint, Anuradha Kumar, Lisa M. Massoudi, Paul Scullion, Gregory T. Robertson, Shilah A. Bonnett, Simon Green, Nicola Caldwell, Jennifer Riley, Gail M. Freiberg, Philip Arthur Hipskind, Michael Mathieson, Thierry Masquelin, Laste Stojanovski, Curtis A. Engelhart, Margaret Huggett, Dinakaran Murugesan, Abraham Lopez Moure, Fabio Zuccotto, Julie V. Early, Ola Epemolu, Paul G. Wyatt, Dale J. Kempf, Kevin D. Read, Susan Davis, Laura A. T. Cleghorn, James Johnson, Steven Mullen, Malcolm Taylor, Anne J. Lenaerts, Penelope A. Turner, Peter C. Ray, Joshua Odingo, Dirk Schnappinger, Aaron Korkegian, Douglas Joerss
Publikováno v:
ACS Omega
ACS Omega, Vol 6, Iss 3, Pp 2284-2311 (2021)
ACS Omega, Vol 6, Iss 3, Pp 2284-2311 (2021)
With the emergence of multi-drug-resistant strains of Mycobacterium tuberculosis, there is a pressing need for new oral drugs with novel mechanisms of action. A number of scaffolds with potent anti-tubercular in vitro activity have been identified fr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::372e1778402b9efb43904bc638481606
http://europepmc.org/articles/PMC7841955
http://europepmc.org/articles/PMC7841955
Autor:
Robert C. Hackman, Matthew A. Hulverson, Kayode K. Ojo, Molly C. McCloskey, Bruce E. Leroy, Michael W. Riggs, James J. Lynch, Wenlin Huang, Grant R. Whitman, Wesley C. Van Voorhis, Samuel L.M. Arnold, Lynn K. Barrett, Ryan Choi, Dale J. Kempf, Andrew Hemphill, Eugenio L. de Hostos, Rama Subba Rao Vidadala, Dustin J. Maly, Kennan C. Marsh, Luis Miguel Ortega-Mora, Dana P. Betzer, Robert K. M. Choy, Erkang Fan, J. Stone Doggett, Deborah A. Schaefer, Gail M. Freiberg
Publikováno v:
Int J Parasitol
Bumped Kinase Inhibitors (BKIs), targeting Calcium-dependent Protein Kinase 1 (CDPK1) in apicomplexan parasites with a glycine gatekeeper, are promising new therapeutics for apicomplexan diseases. Here we will review advances, as well as challenges a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::899e6279ed341e193be6d60874abe419
Autor:
Adrian D. Hobson, Russell A. Judge, Ana L. Aguirre, Brian S. Brown, Yifang Cui, Ping Ding, Eric Dominguez, Enrico DiGiammarino, David A. Egan, Gail M. Freiberg, Sujatha M. Gopalakrishnan, Christopher M. Harris, Marie P. Honore, Karen L. Kage, Nicolas J. Kapecki, Christopher Ling, Junli Ma, Helmut Mack, Mulugeta Mamo, Stefan Maurus, Bradford McRae, Nigel S. Moore, Bernhard K. Mueller, Reinhold Mueller, Marian T. Namovic, Kaushal Patel, Steve D. Pratt, C. Brent Putman, Kara L. Queeney, Kathy K. Sarris, Lisa M. Schaffter, Vincent Stoll, Anil Vasudevan, Lei Wang, Lu Wang, William Wirthl, Kimberly Yach
Publikováno v:
Journal of Medicinal Chemistry. 61:11074-11100
A HTS campaign identified compound 1, an excellent hit-like molecule to initiate medicinal chemistry efforts to optimize a dual ROCK1 and ROCK2 inhibitor. Substitution (2-Cl, 2-NH
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba127f0c7da3013553a7215d8180f4bd
https://doi.org/10.1021/acs.jmedchem.8b01098
https://doi.org/10.1021/acs.jmedchem.8b01098
Autor:
Patricia N. Banfor, Alison Kondratiuk, Deborah A. Schaefer, Dale J. Kempf, Samuel L.M. Arnold, Kayode K. Ojo, Kasey Rivas, Molly C. McCloskey, Gail M. Freiberg, James J. Lynch, Robert C. Hackman, Lynn K. Barrett, Wesley C. Van Voorhis, Joachim Müller, Grant R. Whitman, Thomas K. Shaughnessy, Case W. McNamara, Matthew D Kurnick, Michael W. Riggs, Rama Subba Rao Vidadala, Matthew A. Hulverson, Melissa S. Love, Ryan Choi, Dana P. Betzer, Andrew Hemphill, Dustin J. Maly
Publikováno v:
International Journal for Parasitology. 47:753-763
Improvements have been made to the safety and efficacy of bumped kinase inhibitors, and they are advancing toward human and animal use for treatment of cryptosporidiosis. As the understanding of bumped kinase inhibitor pharmacodynamics for cryptospor
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bcacbb6263341cfb6ff4033d88f815ea
https://doi.org/10.1016/j.ijpara.2017.08.006
https://doi.org/10.1016/j.ijpara.2017.08.006
Autor:
Abhijit Kundu, Matthias Witschel, Marc Siggel, Pimchai Chaiyen, Wanwipa Ittarat, Anja Schäfer, Susan A. Charman, Raphael Aponte, Ubolsree Leartsakulpanich, Geoffrey Schwertz, Karen L. White, François Diederich, Aritsara Jaruwat, Gail M. Freiberg, Roger Bonnert, Adrian Zwyssig, Surajit Sadhukhan, Penchit Chitnumsub, Matthias Rottmann, Mel Lloyd, Myron Srikumaran
Publikováno v:
Journal of Medicinal Chemistry. 60:4840-4860
Target-based approaches toward new antimalarial treatments are highly valuable to prevent resistance development. We report several series of pyrazolopyran-based inhibitors targeting the enzyme serine hydroxymethyltransferase (SHMT), designed to impr
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::392cac0ad516603577a9626aa1cf6733
https://doi.org/10.1021/acs.jmedchem.7b00008
https://doi.org/10.1021/acs.jmedchem.7b00008
Publikováno v:
Bioorganicmedicinal chemistry letters. 29(19)
Effective treatments of neuropathic pain have been a focus of many discovery programs. KCNQ (kv7) are voltage gated potassium channel openers that have the potential for the treatment of CNS disorders including neuropathic pain. Clinical studies have
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::eb13a234d6f8b2c019d7a664d31128ec
https://pubmed.ncbi.nlm.nih.gov/31416667
https://pubmed.ncbi.nlm.nih.gov/31416667
Autor:
Lucy Ellis, Yumi Park, Ola Epemolu, Paul G. Wyatt, Stefano Donini, Laura E. Via, Carolyn Selenski, Matthew Axtman, Thomas R. Ioerger, Menico Rizzi, Tom L. Blundell, Nian Zhou, Simon Green, Olalla Sanz, Maria Osuna-Cabello, David B. Ascher, Helena I. Boshoff, Laste Stojanovski, Travis Hartman, Dale J. Kempf, Clifton E. Barry, Joël Lelièvre, Tracy Bayliss, Zhe Wang, Fred Simeons, Claire J. MacKenzie, Hannah Pflaumer, Valerie Mizrahi, Fabio Zuccotto, James C. Sacchettini, Gracia Santos Diaz, Véronique Dartois, Angela Pacitto, Susan Davis, Kyu Y. Rhee, Laura A. T. Cleghorn, Margaret Huggett, Matthew D. Kurnick, Dinakaran Murugesan, Penelope A. Turner, Kriti Arora, Gerard Drewes, Lluis Ballell, Markus Bösche, Gail M. Freiberg, Kevin D. Read, Surendranadha Reddy Jonnala, Kirsteen I. Buchanan, Maria Jose Lafuente-Monasterio, María José Rebollo-López, Sonja Ghidelli-Disse, Peter C. Ray, Alasdair Smith, Myron Srikumaran, Ardala Breda
Publikováno v:
Repositorio Institucional de la Consejería de Sanidad de la Comunidad de Madrid
Consejería de Sanidad de la Comunidad de Madrid
Consejería de Sanidad de la Comunidad de Madrid
A potent, noncytotoxic indazole sulfonamide was identified by high-throughput screening of >100,000 synthetic compounds for activity against Mycobacterium tuberculosis (Mtb). This noncytotoxic compound did not directly inhibit cell wall biogenesis bu
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::896be08dd9046b3b0b9f82d81de880f5
https://doi.org/10.1021/acsinfecdis.6b00103
https://doi.org/10.1021/acsinfecdis.6b00103
Autor:
Amy E. DeRocher, Kasey Rivas, Nina Isoherranen, Suzanne Scheele, Dale J. Kempf, J. Stone Doggett, Eugenio L. de Hostos, Keshia M. Kerchner, Marilyn Parsons, Dustin J. Maly, Matthew A. Hulverson, Gail M. Freiberg, Lynn K. Barrett, Wesley C. Van Voorhis, Ryan Choi, Rama Subba Rao Vidadala, Georg Neckermann, Wim G. J. Hol, Zhongsheng Zhang, Kayode K. Ojo, Latha Kallur Siddaramaiah, Igor Bruzual, Wenlin Huang, Erkang Fan, Matthew D Kurnick, Ethan A. Merritt
Publikováno v:
ACS Medicinal Chemistry Letters. 6:1184-1189
We previously discovered compounds based on a 5-aminopyrazole-4-carboxamide scaffold to be potent and selective inhibitors of CDPK1 from T. gondii. The current work, through structure–activity relationship studies, led to the discovery of compounds
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::44ee330f738daadc910040ed11d341d5
https://doi.org/10.1021/acsmedchemlett.5b00319
https://doi.org/10.1021/acsmedchemlett.5b00319
Autor:
Nina Isoherranen, Tracey L. Schultz, Amy E. DeRocher, Kayode K. Ojo, Jennifer A. Zambriski, Erkang Fan, Dale J. Kempf, Marilyn Parsons, Dustin J. Maly, Wesley C. Van Voorhis, Gail M. Freiberg, Wim G. J. Hol, Latha Kallur Siddaramaiah, Ethan A. Merritt, Rama Subba Rao Vidadala, Ryan Choi, Kasey Rivas, Matthew A. Hulverson, J. Stone Doggett, Suzanne Scheele, Kennan C. Marsh, Lynn K. Barrett, Wenlin Huang, Vern B. Carruthers, Igor Bruzual, Zhongsheng Zhang
Publikováno v:
Journal of medicinal chemistry. 59(13)
New therapies are needed for the treatment of toxoplasmosis, which is a disease caused by the protozoan parasite Toxoplasma gondii. To this end, we previously developed a potent and selective inhibitor (compound 1) of Toxoplasma gondii calcium-depend
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::33961f2dc3871efeccd309e75ef92b2f
https://pubmed.ncbi.nlm.nih.gov/27309760
https://pubmed.ncbi.nlm.nih.gov/27309760
Autor:
Wenlin, Huang, Kayode K, Ojo, Zhongsheng, Zhang, Kasey, Rivas, Rama Subba Rao, Vidadala, Suzanne, Scheele, Amy E, DeRocher, Ryan, Choi, Matthew A, Hulverson, Lynn K, Barrett, Igor, Bruzual, Latha Kallur, Siddaramaiah, Keshia M, Kerchner, Matthew D, Kurnick, Gail M, Freiberg, Dale, Kempf, Wim G J, Hol, Ethan A, Merritt, Georg, Neckermann, Eugenio L, de Hostos, Nina, Isoherranen, Dustin J, Maly, Marilyn, Parsons, J Stone, Doggett, Wesley C, Van Voorhis, Erkang, Fan
Publikováno v:
ACS Medicinal Chemistry Letters
We previously discovered compounds based on a 5-aminopyrazole-4-carboxamide scaffold to be potent and selective inhibitors of CDPK1 from T. gondii. The current work, through structure–activity relationship studies, led to the discovery of compounds
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::551bdf7e4f0d7c3e9fd7f8c2a88fa30a
https://pubmed.ncbi.nlm.nih.gov/26693272
https://pubmed.ncbi.nlm.nih.gov/26693272