Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Robert J. Aversa"'
Autor:
Sharadha Subramanian, Valery Polyakov, Giordano Caponigro, Amy Lambert, Lina Setti, Ann Van Abbema, Nicholas Keen, Matthew Burger, Mallika Singh, Emma Lees, Michael Patrick Dillon, Alice Rico, Wenlin Shao, Mohamad Hekmat-Nejad, Lesley A. Mathews Griner, Stacey Rivera, Robert J. Aversa, William R. Sellers, Victor Tamez, Joshua M. Korn, Lifeng Wan, Yan Lou, Benjamin R. Taft, Payman Amiri, Savithri Ramurthy, Richard Zang, Darrin Stuart, Jacob R. Haling, Yuji Mishina, Fang Shen, Giselle Nishiguchi, Yun Feng, John Tellew, Vesselina G. Cooke
Publikováno v:
Cancer Research. 78:DDT01-04
The mitogen-activated protein kinase (MAPK) signaling pathway is frequently activated in human cancers due to genetic alterations that can occur at multiple nodes, the most prevalent of which are mutations in RAS or BRAF. While BRAFV600 mutant tumors
Autor:
Gregory A. Michaud, Zinger Yang, Frederic Sigoillot, Carsten Russ, Tiancen Hu, Olga Charlat, Raffaella Zamponi, Robert J. Aversa, John S. Reece-Hoyes, Lei Ji, Xiaoping Zhu, Feng Cong, Jan S. Tchorz, Xiaomo Jiang, Bo Lu
Publikováno v:
Nature Communications
Nature Communications, Vol 10, Iss 1, Pp 1-14 (2019)
Nature Communications, Vol 10, Iss 1, Pp 1-14 (2019)
Axin is a key scaffolding protein responsible for the formation of the β-catenin destruction complex. Stability of Axin protein is regulated by the ubiquitin-proteasome system, and modulation of cellular concentration of Axin protein has a profound
Autor:
Lorena Taricani, George Thomas, Yipin Lu, Yue Pan, Patrick J Rudewicz, Robert Elling, Qin Yue, Rama Jain, Jiong Lan, Xiaodong Lin, Janet Sim, Robert J. Aversa, Linda Xiao, Mark Knapp, Paul A. Barsanti, Xianming Jin
Publikováno v:
ACS Medicinal Chemistry Letters. 6:37-41
A saturation strategy focused on improving the selectivity and physicochemical properties of ATR inhibitor HTS hit 1 led to a novel series of highly potent and selective tetrahydropyrazolo[1,5-a]pyrazines. Use of PI3Kα mutants as ATR crystal structu
Autor:
Giordano Caponigro, Darrin Stuart, William R. Sellers, Yuji Mishina, John Tellew, Wenlin Shao, Stacy Rivera, Mallika Singh, Savithri Ramurthy, Lesley A. Mathews Griner, Gisele Nishiguchi, Mohammad Hekmat-Nejad, Robert J. Aversa, Joshua M. Korn, Payman Amiri, Richard Zang, Yingyun Wang, Yun Feng, Vesselina G. Cooke, Jacob R. Haling, Fang Shen, Valery Polyakov, Nicholas Keen, Michael Patrick Dillon, Emma Lees, Alice Rico
Publikováno v:
Cancer research. 78(6)
Resistance to the RAF inhibitor vemurafenib arises commonly in melanomas driven by the activated BRAF oncogene. Here, we report antitumor properties of RAF709, a novel ATP-competitive kinase inhibitor with high potency and selectivity against RAF kin
Autor:
Yan Lou, Sharadha Subramanian, Yingyun Wang, Lifeng Wan, John Tellew, Laura Tandeske, Benjamin R. Taft, Kalyani Gampa, Jacob R. Haling, Gisele Nishiguchi, Lina Setti, Alice Rico, Sylvia Ma, Payman Amiri, Mallika Singh, Huw Tanner, Brent A. Appleton, Robert J. Aversa, Sepideh Vaziri, Shenlin Huang, Johanna M. Jansen, Anne Van Abbema, Jing Yuan, Vesselina G. Cooke, Hanne Merritt, Aaron Smith, Wenlin Shao, Valery Polyakov, Fei Feng, Savithri Ramurthy, Matthew Burger, Mulugeta Mamo, Lesley A. Mathews Griner, Vijay Sethuraman, Victoriano Tamez, Michael Patrick Dillon, Emma Lees, Ina Dix, Paul A. Barsanti, Richard Zang, Darrin Stuart, Mohammad Hekmat-Nejad
Publikováno v:
Journal of medicinal chemistry. 60(12)
RAS oncogenes have been implicated in30% of human cancers, all representing high unmet medical need. The exquisite dependency on CRAF kinase in KRAS mutant tumors has been established in genetically engineered mouse models and human tumor cells. To d
Publikováno v:
Journal of the American Chemical Society. 132:6855-6861
Maitotoxin (1) continues to fascinate scientists not only because of its size and potent neurotoxicity but also due to its molecular architecture. To provide further support for its structure and facilitate fragment-based biological studies, we devel
Publikováno v:
Angewandte Chemie. 120:7292-7335
Die beispiellose Struktur des marinen Naturstoffs Brevetoxin B wurde 1981 von den Arbeitsgruppen um Nakanishi und Clardy aufgeklart. Das leiterformige Molekulgerust dieses kondensierten Polyethers, die starke Toxizitat und der faszinierende Wirkmecha
Autor:
Kevin P. Cole, Michael O. Frederick, Romelo Gibe, Takahiro Suzuki, Fatima Rivas, Taiki Umezawa, Ross M. Denton, Antonio C. B. Burtoloso, Robert J. Aversa, Kyriacos C. Nicolaou
Publikováno v:
Journal of the American Chemical Society. 130:7466-7476
As the largest secondary metabolite to be discovered as of yet, the polyether marine neurotoxin maitotoxin constitutes a major structural and synthetic challenge. After its originally proposed structure ( 1) had been questioned on the basis of biosyn
Publikováno v:
Angewandte Chemie. 119:9031-9035
Autor:
Lina Setti, Robert J. Aversa, Rama Jain, George Thomas, Savithri Ramurthy, Lorena Taricani, Robert Elling, Mark Knapp, Paul A. Barsanti, Yipin Lu, Matthew Cox, Michelle Mathur, Yue Pan, Xianming Jin, Patrick J Rudewicz, Cheng Hu, Michael Patrick Dillon, Qin Yue, Sharadha Subramanian, Jiong Lan, Linda Xiao
Compound 13 was discovered through morphing of the ATR biochemical HTS hit 1. The ABI series was potent and selective for ATR. Incorporation of a 6-azaindole afforded a marked increase in cellular potency but was associated with poor PK and hERG ion
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::afedc70e6a8e79dca0042a4913c70c0a
https://europepmc.org/articles/PMC4291699/
https://europepmc.org/articles/PMC4291699/