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RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers

Nature cell biology, 2018-09, Vol.20 (9), p.1064

2018

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A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development

Current topics in medicinal chemistry, 2007-07, Vol.7 (14), p.1408

2007

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Allosteric Inhibition of SHP2 Stimulates Antitumor Immunity by Transforming the Immunosuppressive Environment

Cancer research (Chicago, Ill.), 2020-07, Vol.80 (13), p.2889-2902

2020

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Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS

Science (American Association for the Advancement of Science), 2023-08, Vol.381 (6659), p.794-799

2023

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Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy

Nature (London), 2024-05, Vol.629 (8013), p.919-926

2024

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Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors

Journal of medicinal chemistry, 2023-01, Vol.66 (1), p.149-169

2023

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Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity

Journal of medicinal chemistry, 2009-01, Vol.52 (2), p.379-388

2009

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Kinetic efficiency: the missing metric for enhancing compound quality?

Drug discovery today, 2011-11, Vol.16 (21), p.910-913

2011

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Automated iterative Csp3–C bond formation

Nature (London), 2022-04, Vol.604 (7904), p.92-97

2022

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Identification of Novel p38α MAP Kinase Inhibitors Using Fragment-Based Lead Generation

Journal of medicinal chemistry, 2005-01, Vol.48 (2), p.414-426

2005

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A general approach to the galanthamine ring system

Tetrahedron letters, 2001-03, Vol.42 (11), p.2209-2211

2001

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Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors

Bioorganic & medicinal chemistry letters, 2012-11, Vol.22 (21), p.6756-6761

2012

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Direct targeting of RAS in pancreatic ductal adenocarcinoma with RMC-6236, a first-in-class, RAS-selective, orally bioavailable, tri-complex RAS MULTI (ON) inhibitor

Journal of clinical oncology, 2022-02, Vol.40 (4_suppl), p.591-591

2022

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Abstract 1261: A next generation tri-complex KRASG12C(ON) inhibitor directly targets the active, GTP-bound state of mutant RAS and may overcome resistance to KRASG12C(OFF) inhibition

Cancer research (Chicago, Ill.), 2021-07, Vol.81 (13_Supplement), p.1261-1261

2021

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Abstract 1260: First-in-class, orally bioavailable KRASG12V(ON) tri-complex inhibitors, as single agents and in combinations, drive profound anti-tumor activity in preclinical models of KRASG12V mutant cancers

Cancer research (Chicago, Ill.), 2021-07, Vol.81 (13_Supplement), p.1260-1260

2021

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Abstract 1273: Discovery of a potent, selective, and orally bioavailable SOS1 inhibitor, RMC-023, an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction

Cancer research (Chicago, Ill.), 2021-07, Vol.81 (13_Supplement), p.1273-1273

2021

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Abstract 1943: SHP2 inhibition as the backbone of targeted therapy combinations for the treatment of cancers driven by oncogenic mutations in the RAS pathway

Cancer research (Chicago, Ill.), 2020-08, Vol.80 (16_Supplement), p.1943-1943

2020

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Abstract PR04: 4EBP1 reactivation by potent and selective bi-steric inhibitors of mTORC1

Molecular cancer research, 2020-10, Vol.18 (10_Supplement), p.PR04-PR04

2020

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Abstract PR10: Tri-complex inhibitors of the oncogenic, GTP-bound form of KRASG12C overcome RTK-mediated escape mechanisms and drive tumor regressions in vivo

Molecular cancer therapeutics, 2019-12, Vol.18 (12_Supplement), p.PR10-PR10

2019

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Abstract 4878: RMC-4550, an allosteric inhibitor of SHP2: Synthesis, structure, and anti-tumor activity

Cancer research (Chicago, Ill.), 2018-07, Vol.78 (13_Supplement), p.4878-4878

2018

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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

Cancer research (Chicago, Ill.), 2022-06, Vol.82 (12_Supplement), p.3596-3596

2022

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Automated iterative Csp 3 -C bond formation

Nature (London), 2022-04, Vol.604 (7904), p.92

2022

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

Cancer research (Chicago, Ill.), 2022-06, Vol.82 (12_Supplement), p.3595-3595

2022

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

Cancer research (Chicago, Ill.), 2022-06, Vol.82 (12_Supplement), p.3598-3598

2022

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RAS nucleotide cycling underlies the SHP2 phosphatase dependence of mutant BRAF-, NF1- and RAS-driven cancers

A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development

Allosteric Inhibition of SHP2 Stimulates Antitumor Immunity by Transforming the Immunosuppressive Environment

Chemical remodeling of a cellular chaperone to target the active state of mutant KRAS

Concurrent inhibition of oncogenic and wild-type RAS-GTP for cancer therapy

Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors

Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity

Kinetic efficiency: the missing metric for enhancing compound quality?

Automated iterative Csp3–C bond formation

Translational and Therapeutic Evaluation of RAS-GTP Inhibition by RMC-6236 in RAS-Driven Cancers

Identification of Novel p38α MAP Kinase Inhibitors Using Fragment-Based Lead Generation

A general approach to the galanthamine ring system

Optimisation of pharmacokinetic properties in a neutral series of 11β-HSD1 inhibitors

Direct targeting of RAS in pancreatic ductal adenocarcinoma with RMC-6236, a first-in-class, RAS-selective, orally bioavailable, tri-complex RAS MULTI (ON) inhibitor

Abstract 1261: A next generation tri-complex KRASG12C(ON) inhibitor directly targets the active, GTP-bound state of mutant RAS and may overcome resistance to KRASG12C(OFF) inhibition

Abstract 1260: First-in-class, orally bioavailable KRASG12V(ON) tri-complex inhibitors, as single agents and in combinations, drive profound anti-tumor activity in preclinical models of KRASG12V mutant cancers

Abstract 1273: Discovery of a potent, selective, and orally bioavailable SOS1 inhibitor, RMC-023, an in vivo tool compound that blocks RAS activation via disruption of the RAS-SOS1 interaction

Abstract 1943: SHP2 inhibition as the backbone of targeted therapy combinations for the treatment of cancers driven by oncogenic mutations in the RAS pathway

Abstract PR04: 4EBP1 reactivation by potent and selective bi-steric inhibitors of mTORC1

Abstract PR10: Tri-complex inhibitors of the oncogenic, GTP-bound form of KRASG12C overcome RTK-mediated escape mechanisms and drive tumor regressions in vivo

Abstract 4878: RMC-4550, an allosteric inhibitor of SHP2: Synthesis, structure, and anti-tumor activity

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

Automated iterative Csp 3 -C bond formation

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

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

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