Zobrazeno 1 - 10
of 55
pro vyhledávání: '"Bertrand Le Bourdonnec"'
Autor:
Benjamin M. Vincent, Daniel F. Tardiff, Jeff S. Piotrowski, Rebecca Aron, Matthew C. Lucas, Chee Yeun Chung, Helene Bacherman, YiQun Chen, Michelle Pires, Radha Subramaniam, Dimple B. Doshi, Heather Sadlish, Waseem K. Raja, Eric J. Solís, Vikram Khurana, Bertrand Le Bourdonnec, Robert H. Scannevin, Kenneth J. Rhodes
Publikováno v:
Cell Reports, Vol 25, Iss 10, Pp 2742-2754.e31 (2018)
Summary: The lack of disease-modifying treatments for neurodegenerative disease stems in part from our rudimentary understanding of disease mechanisms and the paucity of targets for therapeutic intervention. Here we used an integrated discovery parad
Externí odkaz:
https://doaj.org/article/b5e6241913a94966ac7db88b4002e1b5
Autor:
Timothy M. Caldwell, Michael D. Kaufman, Scott C. Wise, Yu Mi Ahn, Molly M. Hood, Wei-Ping Lu, William C. Patt, Thiwanka Samarakoon, Lakshminarayana Vogeti, Subha Vogeti, Karen M. Yates, Stacie L. Bulfer, Bertrand Le Bourdonnec, Bryan Smith, Daniel Flynn
Publikováno v:
Bioorganicmedicinal chemistry letters. 74
Based on the structure of an early lead identified in Deciphera's proprietary compound collection of switch control kinase inhibitors and using a combination of medicinal chemistry guided structure activity relationships and structure-based drug desi
Autor:
Stacie L. Bulfer, Bertrand Le Bourdonnec, Jeffery D. Zwicker, Yu Mi Ahn, Gada Al-Ani, Hikmat Al-Hashimi, Chase Crawley, Kristin M. Elliott, Saqib Faisal, Andrew M. Harned, Cale L. Heiniger, Molly M. Hood, Salim Javed, Michael Kennedy, Joshua W. Large, Cynthia B. Leary, Wei-Ping Lu, Kylie Luther, Max D. Petty, Hunter R. Picard, Justin T. Proto, Yeni K. Romero, Forrest A. Stanley, Kristen L. Stoltz, Daniel C. Tanner, Hanumaiah Telikepalli, Mary J. Timson, Lakshminarayana Vogeti, Subha Vogeti, Sihyung Yang, Lexy H. Zhong, Bryan D. Smith, Daniel L. Flynn
Publikováno v:
Cancer Research. 83:4045-4045
Background: Mutations in the RAS/MAPK pathway are a frequent driver of cancer, with oncogenic RAS or RAF mutations occurring in >30% of all cancers. First generation BRAF inhibitors are approved for use for tumors with Class I BRAF mutations (V600X).
Autor:
Gada Al-Ani, Qi Groer, Aaron J. Rudeen, Kristin M. Elliott, Patrick C. Kearney, Jeffery D. Zwicker, Yu Mi Ahn, Stacie L. Bulfer, Cale L. Heiniger, Molly M. Hood, Salim Javed, Joshua W. Large, Max D. Petty, Kristen L. Stoltz, Bertrand Le Bourdonnec, Bryan D. Smith, Daniel L. Flynn
Publikováno v:
Cancer Research. 83:1640-1640
Background: The Integrated Stress Response (ISR) is a major adaptive stress response pathway in cancer cell maintenance. The ISR kinase family member PERK controls one of the three arms of the Unfolded Protein Response (UPR). The UPR is considered an
Autor:
Bryan D. Smith, Subha Vogeti, Timothy M. Caldwell, Hanumaiah Telikepalli, Yu Mi Ahn, Gada Al-Ani, Stacie L. Bulfer, Andrew Greenwood, Cale L. Heiniger, Joshua W. Large, Cynthia B. Leary, Wei-Ping Lu, Kylie Luther, William C. Patt, Max D. Petty, Yeni K. Romero, Forrest A. Stanley, Kristen L. Stoltz, Daniel C. Tanner, Sihyung Yang, Yu Zhan, Bertrand Le Bourdonnec, Daniel L. Flynn
Publikováno v:
Cancer Research. 83:4033-4033
Introduction: Gastrointestinal stromal tumors (GISTs) are typically driven by primary mutations in KIT exons 9 or 11. Heterogeneous drug-resistant secondary mutations arise in patients treated with FDA approved KIT inhibitors, including imatinib and
Autor:
Gada Al-Ani, Kristin M. Elliott, Qi Groer, Aaron J. Rudeen, Patrick C. Kearney, Jeffery D. Zwicker, Yu Mi Ahn, Stacie L. Bulfer, Cale L. Heiniger, Molly M. Hood, Salim Javed, Joshua W. Large, Max D. Petty, Kristen L. Stoltz, Bertrand Le Bourdonnec, Bryan D. Smith, Daniel L. Flynn
Publikováno v:
Cancer Research. 83:4938-4938
Background: The integrated stress response (ISR) is a major adaptive pathway stress response pathway and plays an important role in cell fate determination in response to stress. Oncogene addicted tumors are under high levels of stress, both extrinsi
Autor:
Gada Al-Ani, Aaron J. Rudeen, Qi Groer, Kristin M. Elliott, Patrick C. Kearney, Jeffery D. Zwicker, Yu Mi Ahn, Stacie L. Bulfer, Cale L. Heiniger, Molly M. Hood, Salim Javid, Joshua W. Large, Max D. Petty, Kristen L. Stoltz, Bertrand Le Bourdonnec, Bryan D. Smith, Daniel L. Flynn
Publikováno v:
Cancer Research. 83:1613-1613
Background: The Integrated Stress Response (ISR) is a major adaptive stress response pathway in cancers. The ISR kinase family member PERK controls one of the three arms of the Unfolded Protein Response (UPR). The UPR is considered an Achilles’ hee
Autor:
Gada Al-Ani, Qi Groer, Kristin M. Elliott, Aaron J. Rudeen, Patrick C. Kearney, Jeffery D. Zwicker, Yu Mi Ahn, Stacie L. Bulfer, Cale L. Heiniger, Molly M. Hood, Salim Javid, Joshua W. Large, Max D. Petty, Kristen L. Stoltz, Bertrand Le Bourdonnec, Bryan D. Smith, Daniel L. Flynn
Publikováno v:
Cancer Research. 83:1639-1639
Background: The Integrated Stress Response (ISR) is one of the major adaptive stress response pathways in cancer and plays an important role in cell fate determination. Oncogene addicted solid tumors are under high stress levels, both extrinsic as we
Autor:
Daniel F. Tardiff, Matthew Lucas, Iwona Wrona, Belle Chang, Chee Yeun Chung, Bertrand Le Bourdonnec, Kenneth J. Rhodes, Robert H. Scannevin
Publikováno v:
Molecular neurobiology. 59(4)
Summary Stearoyl-CoA desaturase (SCD) is a potential therapeutic target for Parkinson’s and related neurodegenerative diseases. SCD inhibition ameliorates neuronal toxicity caused by aberrant α-synuclein, a lipid-binding protein implicated in Park
Autor:
Timothy M. Caldwell, Yu Mi Ahn, Stacie L. Bulfer, Cynthia B. Leary, Molly M. Hood, Wei-Ping Lu, Lakshminarayana Vogeti, Subha Vogeti, Michael D. Kaufman, Scott C. Wise, Bertrand Le Bourdonnec, Bryan Smith, Daniel Flynn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 74:128928
Based on knowledge of kinase switch-control inhibition and using a combination of structure-based drug design and standard medicinal chemistry principles, we identified a novel series of dihydropyrimidone-based CSF1R kinase inhibitors displaying exqu