Zobrazeno 1 - 10
of 26
pro vyhledávání: '"Timothy S. Heuer"'
Autor:
Timothy S. Heuer, Richard Ventura, Kasia Mordec, Julie Lai, Marina Fridlib, Douglas Buckley, George Kemble
Publikováno v:
EBioMedicine, Vol 16, Iss C, Pp 51-62 (2017)
Palmitate, the enzymatic product of FASN, and palmitate-derived lipids support cell metabolism, membrane architecture, protein localization, and intracellular signaling. Tubulins are among many proteins that are modified post-translationally by acyla
Externí odkaz:
https://doaj.org/article/6f1c25fe440a4d5bb962bf5f6a378714
Autor:
Richard Ventura, Kasia Mordec, Joanna Waszczuk, Zhaoti Wang, Julie Lai, Marina Fridlib, Douglas Buckley, George Kemble, Timothy S. Heuer
Publikováno v:
EBioMedicine, Vol 2, Iss 8, Pp 808-824 (2015)
Inhibition of de novo palmitate synthesis via fatty acid synthase (FASN) inhibition provides an unproven approach to cancer therapy with a strong biological rationale. FASN expression increases with tumor progression and associates with chemoresistan
Externí odkaz:
https://doaj.org/article/28834e3476c148f1a56469f98d334506
Publikováno v:
Poster presentations.
Background Lupus is a heterogeneous, systemic disease that affects millions of patients globally with a high unmet medical need. We present results from our powerful and efficient computational drug discovery platform that identifies hits with first-
Autor:
Jinpeng Liu, Ji Tae Kim, Teresa W.-M. Fan, B. Mark Evers, Tianyan Gao, Anh-Thu Le, Andrew J. Morris, Jennifer W. Harris, George Kemble, Theru A. Sivakumaran, Heidi L. Weiss, Chi Wang, Hunter N. B. Moseley, Timothy S. Heuer, Piotr G. Rychahou, Eun Y. Lee, Robert M. Flight, Yekaterina Y. Zaytseva, Timothy L. Scott
Publikováno v:
Oncotarget
// Yekaterina Y. Zaytseva 1 , Piotr G. Rychahou 2, 3 , Anh-Thu Le 3 , Timothy L. Scott 4 , Robert M. Flight 4 , Ji Tae Kim 2 , Jennifer Harris 3 , Jinpeng Liu 2 , Chi Wang 2 , Andrew J. Morris 5 , Theru A. Sivakumaran 2 , Teresa Fan 4 , Hunter Mosele
Autor:
Allan S. Wagman, George Kemble, Gregory Duke, Marie O'Farrell, William McCulloch, Timothy S. Heuer, Douglas Buckley
Publikováno v:
Pharmacology & Therapeutics. 177:23-31
Decades of preclinical and natural history studies have highlighted the potential of fatty acid synthase (FASN) as a bona fide drug target for oncology. This review will highlight the foundational concepts upon which this perspective is built. Publis
Autor:
Douglas Buckley, Timothy S. Heuer, Julie Lai, George Kemble, Kasia Mordec, Richard Benn Abegania Ventura, Marina Fridlib
Publikováno v:
EBioMedicine, Vol 16, Iss C, Pp 51-62 (2017)
EBioMedicine
EBioMedicine
Palmitate, the enzymatic product of FASN, and palmitate-derived lipids support cell metabolism, membrane architecture, protein localization, and intracellular signaling. Tubulins are among many proteins that are modified post-translationally by acyla
Autor:
Samuel So, Mei-Sze Chua, Aaron C Daugherty, Elizabeth S Noblin, Isaac Hakim, Timothy S Heuer, Wei Wei, Li Ma
Publikováno v:
Cancer Research. 80:LB-110
Hepatocellular carcinoma (HCC) and pancreatic ductal adenocarcinoma (PDAC) have among the lowest 5-year survival rates of all cancer types at 18% and 9%, respectively. Treatment options for patients with liver or pancreatic cancer are relatively unch
Publikováno v:
Annals of the Rheumatic Diseases. 79:1489.2-1489
Background:Lupus is a heterogeneous, systemic disease that affects millions of patients globally with a high unmet medical need. We present results from our powerful and efficient computational drug discovery platform that identifies hits with first-
Autor:
Joanna Waszczuk, Marina Fridlib, Zhaoti Wang, Kasia Mordec, Douglas Buckley, Richard Benn Abegania Ventura, Julie Lai, George Kemble, Timothy S. Heuer
Publikováno v:
EBioMedicine
EBioMedicine, Vol 2, Iss 8, Pp 808-824 (2015)
EBioMedicine, Vol 2, Iss 8, Pp 808-824 (2015)
Inhibition of de novo palmitate synthesis via fatty acid synthase (FASN) inhibition provides an unproven approach to cancer therapy with a strong biological rationale. FASN expression increases with tumor progression and associates with chemoresistan
Autor:
Sunghoon Ma, Julie Lougheed, Christopher Jaeger, Scott W. Womble, Jean-Claire Limun Manalo, Chris A. Buhr, Longcheng Wang, Wentao Zhang, Kenneth D. Rice, Steven Charles Defina, Abigail R. Kennedy, Timothy S. Heuer, Michael Yakes, Neel Kumar Anand, Tae-Gon Baik, Curtis Jeff Kimo, Joerg Bussenius, Angie I. Kim, Jonathan C. Li, Michael Pack, Csaba J. Peto, Monique Nicoll, Naing Aay, Simona Costanzo, Jae Lee, Garth Joseph Mcgrath, Charles M. Blazey, Tsze H. Tsang, Shiva Malek, Anagha Abhijit Joshi, Arlyn Arcalas, Ping Huang, Larisa Dubenko, Jean-Francois Martini, Katherine Lara, John M. Nuss, Owen Joseph Bowles
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:5396-5404
With structural guidance, tropane-derived HTS hits were modified to optimize for HSP90 inhibition and a desirable in vivo profile. Through an iterative SAR development process 12i (XL888) was discovered and shown to reduce HSP90 client protein conten