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Combined inhibition of KRASG12C and mTORC1 kinase is synergistic in non-small cell lung cancer

Nature communications, 2024-07, Vol.15 (1), p.6076-15, Article 6076

2024

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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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Relative contributions of norepinephrine and serotonin transporters to antinociceptive synergy between monoamine reuptake inhibitors and morphine in the rat formalin model

PloS one, 2013-09, Vol.8 (9), p.e74891

2013

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Shp1 Loss Enhances Macrophage Effector Function and Promotes Anti-Tumor Immunity

Frontiers in immunology, 2020-09, Vol.11, p.576310-576310

2020

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Efficacy of a Novel Bi-Steric mTORC1 Inhibitor in Models of B-Cell Acute Lymphoblastic Leukemia

Frontiers in oncology, 2021-08, Vol.11, p.673213-673213

2021

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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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Prediction of human serotonin and norepinephrine transporter occupancy of duloxetine by pharmacokinetic/pharmacodynamic modeling in the rat

The Journal of pharmacology and experimental therapeutics, 2012-04, Vol.341 (1), p.137

2012

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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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Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor

The international journal of neuropsychopharmacology, 2015-01, Vol.18 (2), p.1-11

2015

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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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Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT4 receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation

Bioorganic & medicinal chemistry letters, 2012-10, Vol.22 (19), p.6048-6052

2012

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Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: Clinical compound TD-2749

Bioorganic & medicinal chemistry letters, 2012-07, Vol.22 (14), p.4849-4853

2012

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Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer

Nature (London), 2024-05, Vol.629 (8013), p.927-936

2024

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A Multivalent Approach to the Design and Discovery of Orally Efficacious 5-HT4 Receptor Agonists

Journal of medicinal chemistry, 2009-09, Vol.52 (17), p.5330-5343

2009

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Influence of ligand binding kinetics on functional inhibition of human recombinant serotonin and norepinephrine transporters

Journal of pharmacological and toxicological methods, 2010-03, Vol.61 (2), p.192-204

2010

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Increased acid-sensing ion channel ASIC-3 in inflamed human intestine

European journal of gastroenterology & hepatology, 2001-08, Vol.13 (8), p.891-896

2001

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A Novel Multivalent Ligand That Bridges the Allosteric and Orthosteric Binding Sites of the M2 Muscarinic Receptor

Molecular pharmacology, 2007-08, Vol.72 (2), p.291-302

2007

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P2Y receptor regulation of cultured rat cerebral cortical cells: calcium responses and mRNA expression in neurons and glia

British journal of pharmacology, 2003-05, Vol.139 (2), p.279-288

2003

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Prostaglandin E2-induced sensitization of bradykinin-evoked responses in rat dorsal root ganglion neurons is mediated by cAMP-dependent protein kinase A

The European journal of neuroscience, 2000-09, Vol.12 (9), p.3250-3258

2000

Volltextzugriff (PDF)

214 The KRASG12D(ON) covalent tricomplex inhibitor RM-044 increases tumor antigen presentation and TCR repertoire diversity to promote anti-tumor immunity in a preclinical model of KRASG12D mutant cancer

Journal for immunotherapy of cancer, 2023-11, Vol.11 (Suppl 1), p.A242-A242

2023

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Characterization of prostanoid receptor‐evoked responses in rat sensory neurones

British journal of pharmacology, 1998-06, Vol.124 (3), p.513-523

1998

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5-HT4 receptor agonist mediated enhancement of cognitive function in vivo and amyloid precursor protein processing in vitro: A pharmacodynamic and pharmacokinetic assessment

Neuropharmacology, 2011-07, Vol.61 (1-2), p.69-79

2011

Volltextzugriff (PDF)

Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer

Nature (London), 2024-05, Vol.629 (8013), p.927-6

2024

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Combined inhibition of KRASG12C and mTORC1 kinase is synergistic in non-small cell lung cancer

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

Relative contributions of norepinephrine and serotonin transporters to antinociceptive synergy between monoamine reuptake inhibitors and morphine in the rat formalin model

Shp1 Loss Enhances Macrophage Effector Function and Promotes Anti-Tumor Immunity

Efficacy of a Novel Bi-Steric mTORC1 Inhibitor in Models of B-Cell Acute Lymphoblastic Leukemia

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

Prediction of human serotonin and norepinephrine transporter occupancy of duloxetine by pharmacokinetic/pharmacodynamic modeling in the rat

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

Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor

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

Discovery, oral pharmacokinetics and in vivo efficacy of velusetrag, a highly selective 5-HT4 receptor agonist that has achieved proof-of-concept in patients with chronic idiopathic constipation

Discovery, oral pharmacokinetics and in vivo efficacy of a highly selective 5-HT4 receptor agonist: Clinical compound TD-2749

Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer

A Multivalent Approach to the Design and Discovery of Orally Efficacious 5-HT4 Receptor Agonists

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

Influence of ligand binding kinetics on functional inhibition of human recombinant serotonin and norepinephrine transporters

Increased acid-sensing ion channel ASIC-3 in inflamed human intestine

A Novel Multivalent Ligand That Bridges the Allosteric and Orthosteric Binding Sites of the M2 Muscarinic Receptor

P2Y receptor regulation of cultured rat cerebral cortical cells: calcium responses and mRNA expression in neurons and glia

Prostaglandin E2-induced sensitization of bradykinin-evoked responses in rat dorsal root ganglion neurons is mediated by cAMP-dependent protein kinase A

214 The KRASG12D(ON) covalent tricomplex inhibitor RM-044 increases tumor antigen presentation and TCR repertoire diversity to promote anti-tumor immunity in a preclinical model of KRASG12D mutant cancer

Characterization of prostanoid receptor‐evoked responses in rat sensory neurones

5-HT4 receptor agonist mediated enhancement of cognitive function in vivo and amyloid precursor protein processing in vitro: A pharmacodynamic and pharmacokinetic assessment

Tumour-selective activity of RAS-GTP inhibition in pancreatic cancer

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