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Journal Articles

Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia

Andreas Varkaris, Ermira Pazolli, Hakan Gunaydin, Qi Wang, Levi Pierce, Alessandro A. Boezio, Artemisa Bulku, Lucian DiPietro, Cary Fridrich, Adam Frost, Fabrizio Giordanetto, Erika P. Hamilton, Katherine Harris, Michael Holliday, Tamieka L. Hunter, Amanda Iskandar, Yongli Ji, Alexandre Larivée, Jonathan R. LaRochelle, André Lescarbeau, Fabien Llambi, Brenda Lormil, Mary M. Mader, Brenton G. Mar, Iain Martin, Thomas H. McLean, Klaus Michelsen, Yakov Pechersky, Erika Puente-Poushnejad, Kevin Raynor, Dipali Rogala, Ramin Samadani, Alison M. Schram, Kelley Shortsleeves, Sweta Swaminathan, Shahein Tajmir, Gege Tan, Yong Tang, Roberto Valverde, Bryan Wehrenberg, Jeremy Wilbur, Bret R. Williams, Hongtao Zeng, Hanmo Zhang, W. Patrick Walters, Beni B. Wolf, David E. Shaw, Donald A. Bergstrom, James Watters, James S. Fraser, Pascal D. Fortin, D. Randal Kipp
Journal: Cancer Discovery
Cancer Discov (2024) 14 (2): 240–257.
https://doi.org/10.1158/2159-8290.CD-23-0944
Published: 08 February 2024
View articletitled, Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia
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Includes: Supplementary data
Journal Articles

Comutations and KRASG12C Inhibitor Efficacy in Advanced NSCLC

Marcelo V. Negrao, Haniel A. Araujo, Giuseppe Lamberti, Alissa J. Cooper, Neal S. Akhave, Teng Zhou, Lukas Delasos, J. Kevin Hicks, Mihaela Aldea, Gabriele Minuti, Jacobi Hines, Jacqueline V. Aredo, Michael J. Dennis, Turja Chakrabarti, Susan C. Scott, Paolo Bironzo, Matthias Scheffler, Petros Christopoulos, Albrecht Stenzinger, Jonathan W. Riess, So Yeon Kim, Sarah B. Goldberg, Mingjia Li, Qi Wang, Yun Qing, Ying Ni, Minh Truong Do, Richard Lee, Biagio Ricciuti, Joao Victor Alessi, Jing Wang, Blerina Resuli, Lorenza Landi, Shu-Chi Tseng, Mizuki Nishino, Subba R. Digumarthy, Waree Rinsurongkawong, Vadeerat Rinsurongkawong, Ara A. Vaporciyan, George R. Blumenschein, Jr, Jianjun Zhang, Dwight H. Owen, Collin M. Blakely, Giannis Mountzios, Catherine A. Shu, Christine M. Bestvina, Marina Chiara Garassino, Kristen A. Marrone, Jhanelle E. Gray, Sandip Pravin Patel, Amy L. Cummings, Heather A. Wakelee, Juergen Wolf, Giorgio Vittorio Scagliotti, Federico Cappuzzo, Fabrice Barlesi, Pradnya D. Patil, Leylah Drusbosky, Don L. Gibbons, Funda Meric-Bernstam, J. Jack Lee, John V. Heymach, David S. Hong, Rebecca S. Heist, Mark M. Awad, Ferdinandos Skoulidis
Journal: Cancer Discovery
Cancer Discov (2023) 13 (7): 1556–1571.
https://doi.org/10.1158/2159-8290.CD-22-1420
Published: 07 July 2023
View articletitled, Comutations and KRASG12C Inhibitor Efficacy in Advanced NSCLC
Open the PDF for Comutations and KRASG12C Inhibitor Efficacy in Advanced NSCLC in another window
Includes: Supplementary data
Journal Articles

Exploiting Allosteric Properties of RAF and MEK Inhibitors to Target Therapy-Resistant Tumors Driven by Oncogenic BRAF Signaling

Christos Adamopoulos, Tamer A. Ahmed, Maxwell R. Tucker, Peter M.U. Ung, Min Xiao, Zoi Karoulia, Angelo Amabile, Xuewei Wu, Stuart A. Aaronson, Celina Ang, Vito W. Rebecca, Brian D. Brown, Avner Schlessinger, Meenhard Herlyn, Qi Wang, David E. Shaw, Poulikos I. Poulikakos
Journal: Cancer Discovery
Cancer Discov (2021) 11 (7): 1716–1735.
https://doi.org/10.1158/2159-8290.CD-20-1351
Published: 01 July 2021
View articletitled, Exploiting Allosteric Properties of RAF and MEK Inhibitors to Target Therapy-Resistant Tumors Driven by Oncogenic BRAF Signaling
Open the PDF for Exploiting Allosteric Properties of RAF and MEK Inhibitors to Target Therapy-Resistant Tumors Driven by Oncogenic BRAF Signaling in another window
Includes: Multimedia, Supplementary data