Zobrazeno 1 - 10 of 71 pro vyhledávání: '"David C. Heimbrook"'
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Preclinical Optimization of MDM2 Antagonist Scheduling for Cancer Treatment by Using a Model-Based Approach
Autor: Michael Linn, Sazzad Hussain, Zoran Filipovic, Packman Kathryn E, Christophe Meille, Edmund J.D. Lee, Kenneth Kolinsky, David C. Heimbrook, Antje Walz, Lyubomir T. Vassilev, Brian Higgins, Rosario Garrido, Violeta Adames, Kelli Glenn, Christian Tovar, Shahid Tannu
Publikováno v: Clinical Cancer Research. 20:3742-3752
Purpose: Antitumor clinical activity has been demonstrated for the MDM2 antagonist RG7112, but patient tolerability for the necessary daily dosing was poor. Here, utilizing RG7388, a second-generation nutlin with superior selectivity and potency, we
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e26acc8e595553533cbc45a5f24324fb
https://doi.org/10.1158/1078-0432.ccr-14-0460
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3
Discovery of siRNA Lipid Nanoparticles to Transfect Suspension Leukemia Cells and Provide In Vivo Delivery Capability
Autor: Leopoldo Luistro, Packman Kathryn E, James Cai, Daisy Carvajal, Thomas D. Nevins, Michael J. Bennett, David C. Heimbrook, Gaurav Tyagi, Wei He, Xin Wei, John Frederick Boylan, Melissa Smith, Tai-An Lin
Publikováno v: Molecular Therapy. 22(2):359-370
As a powerful research tool, siRNA's therapeutic and target validation utility with leukemia cells and long-term gene knockdown is severely restricted by the lack of omnipotent, safe, stable, and convenient delivery. Here, we detail our discovery of
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f08284d83e9c6581253a436065608e5
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4
Resistance to Selective BRAF Inhibition Can Be Mediated by Modest Upstream Pathway Activation
Autor: Hong Yang, Jim Rosinski, Kathleen Schostack, Packman Kathryn E, Fei Su, Kenneth Kolinsky, Lizhong Xu, Thomas J. Albert, William D. Bradley, David C. Heimbrook, Mary Simcox, Mitchell Martin, Brian Lestini, Jade Carter, Brian Higgins, Kerstin Trunzer, Richard T. Lee, Qiongqing Wang, Gideon Bollag, Soren Germer, Min Jung Kim
Publikováno v: Cancer Research. 72:969-978
A high percentage of patients with BRAFV600E mutant melanomas respond to the selective RAF inhibitor vemurafenib (RG7204, PLX4032) but resistance eventually emerges. To better understand the mechanisms of resistance, we used chronic selection to esta
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::206a965312fd6821ba18d853133f8223
https://doi.org/10.1158/0008-5472.can-11-1875
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5
Antitumor Activity of BRAF Inhibitor Vemurafenib in Preclinical Models of BRAF-Mutant Colorectal Cancer
Autor: Hong Yang, William D. Bradley, Brian Lestini, David C. Heimbrook, Gideon Bollag, Brian Higgins, Richard J. Lee, Kathleen Schostack, Scott Kopetz, Fei Su, Kenneth Kolinsky, Mary Simcox, Packman Kathryn E
Publikováno v: Cancer Research. 72:779-789
The protein kinase BRAF is a key component of the RAS–RAF signaling pathway which plays an important role in regulating cell proliferation, differentiation, and survival. Mutations in BRAF at codon 600 promote catalytic activity and are associated
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9060dacfefaf4ca0be811e46c0544e44
https://doi.org/10.1158/0008-5472.can-11-2941
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6
Identification of the MEK1(F129L) Activating Mutation as a Potential Mechanism of Acquired Resistance to MEK Inhibition in Human Cancers Carrying the B-RafV600E Mutation
Autor: Huisheng Wang, Christine Rizzo, Neal Rosen, Brian Higgins, Huifeng Niu, Sherif Daouti, Yang Wen, Wen-hui Li, David C. Heimbrook, Packman Kathryn E, Boylan John Frederick
Publikováno v: Cancer Research. 71:5535-5545
Although targeting the Ras/Raf/MEK pathway remains a promising anticancer strategy, mitogen-activated protein/extracellular signal-regulated kinase (ERK) kinase (MEK) inhibitors in clinical development are likely to be limited in their ability to pro
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::655f034c22fb537391ef3b8d1bd645e7
https://doi.org/10.1158/0008-5472.can-10-4351
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7
Characterization of a Novel Mitogen-Activated Protein Kinase Kinase 1/2 Inhibitor with a Unique Mechanism of Action for Cancer Therapy
Autor: Yang Wen, Yang He, Nader Fotouhi, Sherif Daouti, Packman Kathryn E, Norman Kong, Wen-hui Li, Kenneth Kolinsky, David C. Heimbrook, Anthony Specian, Frank John Podlaski, Qing Xiang, Nicholas John Silvester Huby, Huisheng Wang, Brian Higgins, Huifeng Niu
Publikováno v: Cancer Research. 69:1924-1932
The mitogen-activated protein kinase (MAPK) signal transduction pathway plays a central role in regulating tumor cell growth, survival, differentiation, and angiogenesis. The key components of the Ras/Raf/MEK/ERK signal module are frequently altered
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::88d97f0577a8efa56ee33c335664b715
https://doi.org/10.1158/0008-5472.can-08-2627
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8
In vivoactivity of novel capecitabine regimens alone and with bevacizumab and oxaliplatin in colorectal cancer xenograft models
Autor: Joseph Kohles, Yu-E Zhang, Ben-Quan Shen, Packman Kathryn E, Brian Higgins, David C. Heimbrook, Kenneth Kolinsky, Thomas F. Zioncheck, Ute Dugan
Publikováno v: Molecular Cancer Therapeutics. 8:75-82
Modifying the capecitabine dosing schedule from 14 days on, 7 days off (14/7) to 7 days on, 7 days off (7/7) may enable higher doses and improved antitumor efficacy in colorectal cancer xenografts. Capecitabine 14/7 (267 or 400 mg/kg) and 7/7 (467 or
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::84b0567a6d54020a7eff9a700b33c359
https://doi.org/10.1158/1535-7163.mct-08-0596
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9
Elevated MDM2 boosts the apoptotic activity of p53-MDM2 binding inhibitors by facilitating MDMX degradation
Autor: Baoying Huang, David C. Heimbrook, Christian Tovar, Mingxuan Xia, Lyubomir T. Vassilev, Dejan Knezevic
Publikováno v: Cell Cycle. 7:1604-1612
The p53 tumor suppressor is a powerful growth suppressive and pro-apoptotic molecule frequently inactivated in human cancer. Many tumors overproduce its negative regulator MDM2, a specific p53 ubiquitin ligase and transcriptional inhibitor, to disabl
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bf4fd653027a28ee782f886de3da195c
https://doi.org/10.4161/cc.7.11.5929
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10
In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials
Autor: Sazzad Hussain, Brian Higgins, Packman Kathryn E, Bernardo Felix, Hong Qian, Tom Nevins, Kenneth Kolinsky, Yingsi Chen, Roger Blain, David C. Heimbrook, Allen John Lovey, Wanda DePinto, Christian Tovar, Melissa Smith, Petra Goelzer, Xuefeng Yin, Leopoldo Luistro, Xin-Jie Chu, Qing Xiang, Rachid Hamid
Publikováno v: Molecular Cancer Therapeutics. 5:2644-2658
The cyclin-dependent protein kinases are key regulators of cell cycle progression. Aberrant expression or altered activity of distinct cyclin-dependent kinase (CDK) complexes results in escape of cells from cell cycle control, leading to unrestricted
Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9674b1d60dd3411af49528aad073369e
https://doi.org/10.1158/1535-7163.mct-06-0355
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