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Journal Articles

Abstract IA-04: Targeting the oncogenic state of RAS with tri-complex inhibitors

Mallika Singh

Cancer Res (2024) 84 (17_Supplement_2): IA-04.

https://doi.org/10.1158/1538-7445.PANCREATIC24-IA-04

Published: 15 September 2024

View article titled, Abstract IA-04: Targeting the oncogenic state of RAS with tri-complex inhibitors

Journal Articles

Abstract 3340: RMC-5127, a first-in-class, orally bioavailable mutant-selective RASG12V(ON) inhibitor is central nervous system (CNS)-penetrant and demonstrates anti-tumor activity in a preclinical intracranial xenograft model

Zhe Chen, Andre Eriksson, Bianca Lee, Jay Dinglasan, Nilufar Montazer, Jim Cregg, Anne Edwards, Kate Sanders, Jacqueline A. Smith, David Wildes, Mallika Singh, Zhican Wang, Jingjing Jiang

Cancer Res (2024) 84 (6_Supplement): 3340.

https://doi.org/10.1158/1538-7445.AM2024-3340

Published: 22 March 2024

View article titled, Abstract 3340: RMC-5127, a first-in-class, orally bioavailable mutant-selective RASG12V(ON) inhibitor is central nervous system (CNS)-penetrant and demonstrates anti-tumor activity in a preclinical intracranial xenograft model

Journal Articles

Abstract 1924: RTK signaling and WT RAS activity as vulnerabilities in tumors with acquired resistance to GDP-state selective KRAS^G12C inhibitors in preclinical models

Hitendra S. Solanki, Harshit Shah, Denis Imbody, Bina Desai, Paul A. Stewart, Bin Fang, Yaakov Stern, Lancia N. Darville, John M. Koomen, Andriy Marusyk, Ethan Ahler, Ida Aronchik, Mallika Singh, Eric B. Haura

Cancer Res (2024) 84 (6_Supplement): 1924.

https://doi.org/10.1158/1538-7445.AM2024-1924

Published: 22 March 2024

View article titled, Abstract 1924: RTK signaling and WT RAS activity as vulnerabilities in tumors with acquired resistance to GDP-state selective KRASG12C inhibitors in preclinical models

Journal Articles

Abstract 1927: Resistance to RAS-GTP inhibition in models of pancreatic ductal adenocarcinoma arises downstream of RAS effectors

Cancer Res (2024) 84 (6_Supplement): 1927.

https://doi.org/10.1158/1538-7445.AM2024-1927

Published: 22 March 2024

View article titled, Abstract 1927: Resistance to RAS-GTP inhibition in models of pancreatic ductal adenocarcinoma arises downstream of RAS effectors

Journal Articles

Abstract 6585: Combination RAS^G12C(ON) and RAS^MULTI(ON) inhibition overcomes resistance and prolongs durability in preclinical models of mutant KRAS^G12C-driven cancers

Xing Wei, Matthew Holderfield, Yu Chi Yang, Kyle Seamon, Jay Dinglasan, Nilufar Montazar, Bianca Lee, Shurui Cai, Lick Lai, Ida Aronchik, Stephanie Chang, Zhican Wang, Pete Wildes, Jacqueline A. Smith, Jingjing Jiang, Mallika Singh

Cancer Res (2024) 84 (6_Supplement): 6585.

https://doi.org/10.1158/1538-7445.AM2024-6585

Published: 22 March 2024

View article titled, Abstract 6585: Combination RASG12C(ON) and RASMULTI(ON) inhibition overcomes resistance and prolongs durability in preclinical models of mutant KRASG12C-driven cancers

Journal Articles

Abstract B101: Tumor-selective inhibition of active RAS in pancreatic ductal adenocarcinoma

Urszula N. Wasko, Jingjing Jiang, Lorenzo Tomassoni, Yingyun Wang, Bianca Lee, Margo Orlen, Kristina Drizyte-Miller, Marie Menard, Julien Dilly, Steven A. Sastra, Carmine F. Palermo, Stephanie Chang, Andrew J. Aguirre, Channing J. Der, Robert H. Vonderheide, Ben Z. Stanger, Andrea Califano, Mallika Singh, Kenneth P. Olive

Cancer Res (2024) 84 (2_Supplement): B101.

https://doi.org/10.1158/1538-7445.PANCA2023-B101

Published: 16 January 2024

View article titled, Abstract B101: Tumor-selective inhibition of active RAS in pancreatic ductal adenocarcinoma

Journal Articles

Abstract B080: Mutant-selective KRAS^G12D(ON) inhibitor suppresses proliferation in vitro and tumor growth in vivo of Kras^G12D GEMM-derived PDAC organoids

Mark P. Labrecque, Lingyan Jiang, Nicole Nasholm, Biswadeep Nayak, Xinxing Yu, Avian Song, Caroline Weller, James W. Evans, Maria Paz Zafra, Marie Parsons, Marie Menard, Lukas E. Dow, Jingjing Jiang, Ida Aronchik, Mallika Singh

Cancer Res (2024) 84 (2_Supplement): B080.

https://doi.org/10.1158/1538-7445.PANCA2023-B080

Published: 16 January 2024

View article titled, Abstract B080: Mutant-selective KRASG12D(ON) inhibitor suppresses proliferation in vitro and tumor growth in vivo of KrasG12D GEMM-derived PDAC organoids

Journal Articles

Abstract LB015: Bi-steric mTORC1-selective inhibitors activate 4EBP1, suppress MYC, restore anti-tumor immunity, and cooperate with immune checkpoint inhibition to elicit tumor regression

Wadie D. Mahauad-Fernandez, Yu Chi Yang, Ian Lai, Jangho Park, Lilian Yao, James W. Evans, Danielle F. Atibalentja, Xinyu Chen, Zihui Zhao, G. Leslie Burnett, Bianca J. Lee, Nuntana Dinglasan, Nataliya Shifrin, Ethan Ahler, Elsa Quintana, Adrian Gill, Jacqueline A. Smith, Mallika Singh, Dean W. Felsher

Cancer Res (2023) 83 (8_Supplement): LB015.

https://doi.org/10.1158/1538-7445.AM2023-LB015

Published: 14 April 2023

View article titled, Abstract LB015: Bi-steric mTORC1-selective inhibitors activate 4EBP1, suppress MYC, restore anti-tumor immunity, and cooperate with immune checkpoint inhibition to elicit tumor regression

Journal Articles

Abstract 1598: RM-046, a first-in-class, mutant-selective, and oral KRAS^Q61H(ON) inhibitor that drives tumor regression in preclinical models and validates KRAS^Q61H as a therapeutic target

Cancer Res (2023) 83 (7_Supplement): 1598.

https://doi.org/10.1158/1538-7445.AM2023-1598

Published: 04 April 2023

View article titled, Abstract 1598: RM-046, a first-in-class, mutant-selective, and oral KRASQ61H(ON) inhibitor that drives tumor regression in preclinical models and validates KRASQ61H as a therapeutic target

Journal Articles

Abstract 526: RMC-9805, a first-in-class, mutant-selective, covalent and oral KRAS^G12D(ON) inhibitor that induces apoptosis and drives tumor regression in preclinical models of KRAS^G12D cancers

Cancer Res (2023) 83 (7_Supplement): 526.

https://doi.org/10.1158/1538-7445.AM2023-526

Published: 04 April 2023

View article titled, Abstract 526: RMC-9805, a first-in-class, mutant-selective, covalent and oral KRASG12D(ON) inhibitor that induces apoptosis and drives tumor regression in preclinical models of KRASG12D cancers

Journal Articles

Abstract 1725: Preclinical evaluation of RM-042, an orally bioavailable inhibitor of GTP-RAS, in models of pancreatic ductal adenocarcinoma

Urszula N. Wasko, Stephen A. Sastra, Carmine F. Palermo, David Wildes, Mallika Singh, Kenneth P. Olive

Cancer Res (2023) 83 (7_Supplement): 1725.

https://doi.org/10.1158/1538-7445.AM2023-1725

Published: 04 April 2023

View article titled, Abstract 1725: Preclinical evaluation of RM-042, an orally bioavailable inhibitor of GTP-RAS, in models of pancreatic ductal adenocarcinoma

Journal Articles

Abstract 4859: Bi-steric mTORC1 inhibitors are superior to rapamycin and induce apoptotic cell death in tumor models with hyperactivated mTORC1

Heng Du, Yu Chi Yang, Heng-Jia Liu, Min Yuan, John Asara, Kwok-Kin Wong, Mallika Singh, David Kwiatkowski

Cancer Res (2023) 83 (7_Supplement): 4859.

https://doi.org/10.1158/1538-7445.AM2023-4859

Published: 04 April 2023

View article titled, Abstract 4859: Bi-steric mTORC1 inhibitors are superior to rapamycin and induce apoptotic cell death in tumor models with hyperactivated mTORC1

Journal Articles

Abstract B071: Preclinical evaluation of RM-042, an orally bioavailable inhibitor of GTP-RAS, in models of pancreatic ductal adenocarcinoma

Urszula N. Wasko, Stephen A. Sastra, Carmine F. Palermo, David Wildes, Mallika Singh, Kenneth P. Olive

Cancer Res (2022) 82 (22_Supplement): B071.

https://doi.org/10.1158/1538-7445.PANCA22-B071

Published: 15 November 2022

View article titled, Abstract B071: Preclinical evaluation of RM-042, an orally bioavailable inhibitor of GTP-RAS, in models of pancreatic ductal adenocarcinoma

Journal Articles

Abstract 3596: RM-036, a first-in-class, orally-bioavailable, Tri-Complex covalent KRAS^G12D(ON) inhibitor, drives profound anti-tumor activity in KRAS^G12D mutant tumor models

John E. Knox, Jingjing Jiang, G. Leslie Burnett, Yang Liu, Caroline E. Weller, Zhican Wang, Laura McDowell, Shelby L. Steele, Shook Chin, Kang Jye Chou, Fang Wang, Mengqi Zhong, Elena S. Koltun, David Wildes, Mallika Singh, Adrian L. Gill, Jacqueline A. Smith

Cancer Res (2022) 82 (12_Supplement): 3596.

https://doi.org/10.1158/1538-7445.AM2022-3596

Published: 15 June 2022

View article titled, Abstract 3596: RM-036, a first-in-class, orally-bioavailable, Tri-Complex covalent KRASG12D(ON) inhibitor, drives profound anti-tumor activity in KRASG12D mutant tumor models

Journal Articles

Abstract 3595: RMC-6291, a next-generation tri-complex KRAS^G12C(ON) inhibitor, outperforms KRAS^G12C(OFF) inhibitors in preclinical models of KRAS^G12C cancers

Cancer Res (2022) 82 (12_Supplement): 3595.

https://doi.org/10.1158/1538-7445.AM2022-3595

Published: 15 June 2022

View article titled, Abstract 3595: RMC-6291, a next-generation tri-complex KRASG12C(ON) inhibitor, outperforms KRASG12C(OFF) inhibitors in preclinical models of KRASG12C cancers

Journal Articles

Abstract 2662: Bi-steric mTORC1 inhibitor RMC-6272 synergizes with immune checkpoint inhibitors to induce sustained regression of MYC-driven hepatocellular carcinoma

Wadie D. Mahauad-Fernandez, Yu C. Yang, Ian Lai, Jangho Park, Lilian Yao, James W. Evans, Jacqueline A. Smith, Mallika Singh, Dean W. Felsher

Cancer Res (2022) 82 (12_Supplement): 2662.

https://doi.org/10.1158/1538-7445.AM2022-2662

Published: 15 June 2022

View article titled, Abstract 2662: Bi-steric mTORC1 inhibitor RMC-6272 synergizes with immune checkpoint inhibitors to induce sustained regression of MYC-driven hepatocellular carcinoma

Journal Articles

Abstract 3598: A first-in-class tri-complex KRAS^G13C(ON) inhibitor validates therapeutic targeting of KRAS^G13Cand drives tumor regressions in preclinical models

Christopher J. Schulze, Jim Cregg, Kyle J. Seamon, Yu Chi Yang, Zhican Wang, Lindsay S. Garrenton, Alun Bermingham, John E. Knox, Aidan Tomlinson, Kang-Jye Chou, Shaoling Li, David P. Wildes, Mallika Singh, Elena S. Koltun, Adrian L. Gill, Robert J. Nichols, Jacqueline A. Smith

Cancer Res (2022) 82 (12_Supplement): 3598.

https://doi.org/10.1158/1538-7445.AM2022-3598

Published: 15 June 2022

View article titled, Abstract 3598: A first-in-class tri-complex KRASG13C(ON) inhibitor validates therapeutic targeting of KRASG13Cand drives tumor regressions in preclinical models

Journal Articles

Abstract 3597: Direct targeting of KRAS^G12X mutant cancers with RMC-6236, a first-in-class, RAS-selective, orally bioavailable, tri-complex RAS^MULTI(ON) inhibitor

Cancer Res (2022) 82 (12_Supplement): 3597.

https://doi.org/10.1158/1538-7445.AM2022-3597

Published: 15 June 2022

View article titled, Abstract 3597: Direct targeting of KRASG12X mutant cancers with RMC-6236, a first-in-class, RAS-selective, orally bioavailable, tri-complex RASMULTI(ON) inhibitor

Journal Articles

Abstract LB089: Effective in vivo treatment of endometrial tumor models with coexistent mutant PI3K and PTEN inactivation with a selective bi-steric mTORC1 kinase inhibitor

Hilla Solomon, Radha Mukherjee, Xiaoping Chen, HuiYong Zhao, Elisa de Stanchina, Britta Weigelt, Alison M. Schram, Carol Aghajanian, Mallika Singh, Jan Smith, Neal Rosen

Cancer Res (2022) 82 (12_Supplement): LB089.

https://doi.org/10.1158/1538-7445.AM2022-LB089

Published: 15 June 2022

View article titled, Abstract LB089: Effective in vivo treatment of endometrial tumor models with coexistent mutant PI3K and PTEN inactivation with a selective bi-steric mTORC1 kinase inhibitor

Journal Articles

Abstract 1026: Bi-steric mTORC1-selective inhibitors demonstrate improved potency and efficacy in tumors with mTORC1 hyperactivation

Heng Du, Yu Chi Yang, Mallika Singh, Heng-jia Liu, David Kwiatkowski

Cancer Res (2021) 81 (13_Supplement): 1026.

https://doi.org/10.1158/1538-7445.AM2021-1026

Published: 01 July 2021

View article titled, Abstract 1026: Bi-steric mTORC1-selective inhibitors demonstrate improved potency and efficacy in tumors with mTORC1 hyperactivation

NARROW

Abstract IA-04: Targeting the oncogenic state of RAS with tri-complex inhibitors

Abstract 3340: RMC-5127, a first-in-class, orally bioavailable mutant-selective RASG12V(ON) inhibitor is central nervous system (CNS)-penetrant and demonstrates anti-tumor activity in a preclinical intracranial xenograft model

Abstract 1924: RTK signaling and WT RAS activity as vulnerabilities in tumors with acquired resistance to GDP-state selective KRAS^G12C inhibitors in preclinical models

Abstract 1927: Resistance to RAS-GTP inhibition in models of pancreatic ductal adenocarcinoma arises downstream of RAS effectors

Abstract 6585: Combination RAS^G12C(ON) and RAS^MULTI(ON) inhibition overcomes resistance and prolongs durability in preclinical models of mutant KRAS^G12C-driven cancers

Abstract B101: Tumor-selective inhibition of active RAS in pancreatic ductal adenocarcinoma

Abstract B080: Mutant-selective KRAS^G12D(ON) inhibitor suppresses proliferation in vitro and tumor growth in vivo of Kras^G12D GEMM-derived PDAC organoids

Abstract LB015: Bi-steric mTORC1-selective inhibitors activate 4EBP1, suppress MYC, restore anti-tumor immunity, and cooperate with immune checkpoint inhibition to elicit tumor regression

Abstract 1598: RM-046, a first-in-class, mutant-selective, and oral KRAS^Q61H(ON) inhibitor that drives tumor regression in preclinical models and validates KRAS^Q61H as a therapeutic target

Abstract 526: RMC-9805, a first-in-class, mutant-selective, covalent and oral KRAS^G12D(ON) inhibitor that induces apoptosis and drives tumor regression in preclinical models of KRAS^G12D cancers

Abstract 1725: Preclinical evaluation of RM-042, an orally bioavailable inhibitor of GTP-RAS, in models of pancreatic ductal adenocarcinoma

Abstract 4859: Bi-steric mTORC1 inhibitors are superior to rapamycin and induce apoptotic cell death in tumor models with hyperactivated mTORC1

Abstract B071: Preclinical evaluation of RM-042, an orally bioavailable inhibitor of GTP-RAS, in models of pancreatic ductal adenocarcinoma

Abstract 3596: RM-036, a first-in-class, orally-bioavailable, Tri-Complex covalent KRAS^G12D(ON) inhibitor, drives profound anti-tumor activity in KRAS^G12D mutant tumor models

Abstract 3595: RMC-6291, a next-generation tri-complex KRAS^G12C(ON) inhibitor, outperforms KRAS^G12C(OFF) inhibitors in preclinical models of KRAS^G12C cancers

Abstract 2662: Bi-steric mTORC1 inhibitor RMC-6272 synergizes with immune checkpoint inhibitors to induce sustained regression of MYC-driven hepatocellular carcinoma

Abstract 3598: A first-in-class tri-complex KRAS^G13C(ON) inhibitor validates therapeutic targeting of KRAS^G13Cand drives tumor regressions in preclinical models

Abstract 3597: Direct targeting of KRAS^G12X mutant cancers with RMC-6236, a first-in-class, RAS-selective, orally bioavailable, tri-complex RAS^MULTI(ON) inhibitor

Abstract LB089: Effective in vivo treatment of endometrial tumor models with coexistent mutant PI3K and PTEN inactivation with a selective bi-steric mTORC1 kinase inhibitor

Abstract 1026: Bi-steric mTORC1-selective inhibitors demonstrate improved potency and efficacy in tumors with mTORC1 hyperactivation

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