Zobrazeno 1 - 10
of 49
pro vyhledávání: '"Martin R. Tremblay"'
Autor:
Norma Rogers, Stephan Krapp, Faika Mseeh, Richard T. Lewis, Keith Mikule, Michelle Han, Jay Theroff, Yongying Jiang, Keith M. Wilcoxen, Cross Jason, Dana Pfaffinger, Michael J. Soth, Paul G. Leonard, Philip Jones, Pijus K. Mandal, Angela L. Harris, Martin R. Tremblay, Simon S. Yu, Jason P Burke, Connor A. Parker, Barbara Czako, Alessia Petrocchi, Naphtali J. Reyna, Joseph R. Marszalek, Matthew M. Hamilton, Timothy McAfoos, Brett W. Virgin-Downey, Graham Trevitt, Alfred Lammens, Alan Xu
Publikováno v:
Journal of Medicinal Chemistry. 64:11302-11329
Indoleamine 2,3-dioxygenase 1 (IDO1), a heme-containing enzyme that mediates the rate-limiting step in the metabolism of l-tryptophan to kynurenine, has been widely explored as a potential immunotherapeutic target in oncology. We developed a class of
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec33cf6551a670d4d40eaab2894a6f60
https://doi.org/10.1021/acs.jmedchem.1c00679
https://doi.org/10.1021/acs.jmedchem.1c00679
Autor:
Brian H. White, Yaguang Si, Sarah Cappucci, Zhi Li, Jessica D. Ramirez, Charles M. Ponthier, Erica Visness, Peicheng Du, Minjung Choi, Pieter C. Beerepoot, Paula C. Ortet, Ivan T. Jewett, Josue Alfaro-Lopez, Sorabh Agarwal, Daniel La, Aaron Fulgham, John H. McGee, Keith Orford, Jonathan B. Hurov, Martin R. Tremblay, Gregory L. Verdine
Publikováno v:
Cancer Research. 83:3094-3094
Wnt signaling pathway mutations leading to constitutive activation of the driver oncogene β-catenin occur in at least 20% of all human cancers, but β-catenin itself has remained undruggable by traditional modalities. In order to inhibit the activit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::8c51d264aae8f3a219530f16aa966065
https://doi.org/10.1158/1538-7445.am2023-3094
https://doi.org/10.1158/1538-7445.am2023-3094
Autor:
Timothy P. Heffernan, Angela L. Harris, Martin R. Tremblay, Connor A. Parker, Yongying Jiang, Robert A. Mullinax, Cross Jason, Jihai Pang, Qi Wu, Edward Q. Chang, Sonal Gera, Keith M. Wilcoxen, Paul G. Leonard, Zhen Liu, Jeffrey J. Kovacs, Erika Suzuki, Barbara Czako, Ningping Feng, Joseph R. Marszalek, Nakia D. Spencer, Pijus K. Mandal, Jason P Burke, Simon S. Yu, Keith Mikule, Faika Mseeh, Philip Jones, Giulio Draetta
Publikováno v:
Journal of Medicinal Chemistry. 63:9888-9911
Tumor-associated macrophages (TAMs) have a significant presence in the tumor stroma across multiple human malignancies and are believed to be beneficial to tumor growth. Targeting CSF1R has been proposed as a potential therapy to reduce TAMs, especia
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::477eb096ec2e1d0be3af1800c7acd0a9
https://doi.org/10.1021/acs.jmedchem.0c00936
https://doi.org/10.1021/acs.jmedchem.0c00936
Autor:
Christian M. Martin, Jennifer Proctor, Patrick O'Hearn, Janid A. Ali, Andre Lescarbeau, Jennifer Hoyt, Jonathan P. DiNitto, Ann M. Rowley, Thomas T. Tibbitts, Catherine A. Evans, Martin R. Tremblay, Tao Liu, Vito J. Palombella, John Soglia, Johan A. Pradeilles, Somarajan J. Nair, Melissa Pink, David G. Winkler, Stanley Goldstein, Quentin Glenadel, Erin L. O’Hearn, Culver Cheung, Erin Brophy, Alfredo C. Castro, Louis Grenier
Publikováno v:
ACS Medicinal Chemistry Letters. 7:862-867
Optimization of isoquinolinone PI3K inhibitors led to the discovery of a potent inhibitor of PI3K-γ (26 or IPI-549) with >100-fold selectivity over other lipid and protein kinases. IPI-549 demonstrates favorable pharmacokinetic properties and robust
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::10f2e63c8dbb32a50d02e0a4d22c2564
https://doi.org/10.1021/acsmedchemlett.6b00238
https://doi.org/10.1021/acsmedchemlett.6b00238
Autor:
Michael Foley, Andre Lescarbeau, Martin R. Tremblay, Lombardy Richard John, Grogan Michael John, Andrew B. Hague, Kristopher M. Depew, Jimin Xiong, Joseph Helble, Priscilla L. White, Julian Adams, Brian C. Austad, Caroline D. Lory, Somarajan J. Nair, Stéphane Peluso, Lin-Chen Yu, Alfredo C. Castro, André B. Charette, Benjamin S. Lane, Jeanne Shaffer, Louis Grenier, James R. Porter, Matthew Campbell, Koney Nii O, Mark L. Behnke
Publikováno v:
Organic Process Research & Development. 20:786-798
The formation of the d-homocyclopamine ring system in IPI-926 is the key step in its semisynthesis and proceeds via a chemoselective cyclopropanation followed by a stereoselective acid-catalyzed carbocation rearrangement. In order to perform large-sc
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::4a9debb0b604cbda59d104def86c7642
https://doi.org/10.1021/acs.oprd.6b00048
https://doi.org/10.1021/acs.oprd.6b00048
Autor:
Joi Dunbar, Margaret A. Read, Joseph D. Manna, Alexander Constan, Alfredo C. Castro, Sherri Smith, Gordon Loewen, John Lee, Somarajan J. Nair, Jennifer Hoyt, Martin R. Tremblay, Julian Adams, Jeanne A. Ferguson, Jens Sydor, Veronica Campbell, Matthew Campbell, Karen McGovern, Brendan Arsenault, Marisa O. Peluso, Jylle Nevejans, Vito J. Palombella, Nigel Whitebread, Grogan Michael John, Kerrie Faia, John Soglia, Bennett Carter
Publikováno v:
Xenobiotica. 43:875-885
1. IPI-926 is a novel semisynthetic cyclopamine derivative that is a potent and selective Smoothened inhibitor that blocks the hedgehog signal transduction pathway. 2. The in vivo clearance of IPI-926 is low in mouse and dog and moderate in monkey. T
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::50620a2c18fbef25785c49cf6a0c9deb
https://doi.org/10.3109/00498254.2013.780671
https://doi.org/10.3109/00498254.2013.780671
Autor:
Patrick O'Hearn, Janid A. Ali, Kelly Slocum, Jitendra D. Belani, Sherri Smith, Tao Liu, Adilah Bahadoor, Andre Lescarbeau, Somarajan J. Nair, Christian C. Fritz, Karen McGovern, Kip A. West, Joseph Helble, Bonnie Tillotson, Martin R. Tremblay, Wylie Andrew A, Vito J. Palombella, Alfredo C. Castro, Stéphane Peluso, James M. Conley, Mark Douglas
Publikováno v:
Journal of Medicinal Chemistry. 55:8859-8878
Misregulation of protein translation plays a critical role in human cancer pathogenesis at many levels. Silvestrol, a cyclopenta[b]benzofuran natural product, blocks translation at the initiation step by interfering with assembly of the eIF4F transla
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca8e686d0a86b9c6d0b9d6e0f79d708d
https://doi.org/10.1021/jm3011542
https://doi.org/10.1021/jm3011542
Publikováno v:
Expert Opinion on Therapeutic Patents. 19:1039-1056
There is increasing evidence suggesting that blocking aberrant Hedgehog (Hh) signaling can be a novel therapeutic avenue for the treatment of cancer. During the past decade, efforts from academic and industrial groups have led to the discovery of a v
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::824cca7040930a9813cdcd4052174b26
https://doi.org/10.1517/13543770903008551
https://doi.org/10.1517/13543770903008551
Autor:
Matthew Campbell, Caroline N. Woodward, Jens Sydor, Alfredo C. Castro, James R. Porter, Margaret A. Read, Kerrie Faia, Kerry White, Martin R. Tremblay, Jill Cushing, Julian Adams, Lin-Chen Yu, Mark L. Behnke, Jennifer Hoyt, Vito J. Palombella, Karen McGovern, Somarajan J. Nair, Jeffrey K. Tong, Margit Hagel, Marta Nevalainen, Louis Grenier, Michael Foley
Publikováno v:
Journal of Medicinal Chemistry. 51:6646-6649
Herein is reported the synthesis of a novel class of hedgehog antagonists derived from cyclopamine. The acid sensitive D-ring of cyclopamine was homologated utilizing a sequence of chemoselective cyclopropanation and stereoselective acid-catalyzed re
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e0d0752adc424ed0f2bb4f871b70a4f4
https://doi.org/10.1021/jm8008508
https://doi.org/10.1021/jm8008508
Autor:
Alois Fürstner, Mario Waser, Carine Chevrier, Oliver Müller, Christophe Aïssa, Filip Teplý, Cristina Nevado, Martin R. Tremblay, Emilie Moulin
Publikováno v:
Journal of the American Chemical Society. 129:9150-9161
A concise and convergent total synthesis of the highly cytotoxic marine natural products iejimalide A-D (1-4) is reported, which relies on an effective ring-closing metathesis (RCM) reaction of a cyclization precursor containing no less than 10 doubl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e60ec2a9ddf5ff82547b1365abb25caf
https://doi.org/10.1021/ja072334v
https://doi.org/10.1021/ja072334v