List of works - Stephen E. Gould

A cell identity switch allows residual BCC to survive Hedgehog pathway inhibition

scientific article published in Nature

A paracrine requirement for hedgehog signalling in cancer

scientific article

Antitumor Activity of Targeted and Cytotoxic Agents in Murine Subcutaneous Tumor Models Correlates with Clinical Response ⬇️

scientific article published on May 30, 2012

Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma

scientific article

Canonical hedgehog signaling augments tumor angiogenesis by induction of VEGF-A in stromal perivascular cells ⬇️

scientific article published on May 19, 2011

Carcinogenicity assessment of the Hedgehog pathway inhibitor, vismodegib in Tg.rasH2 mice and Sprague-Dawley rats

scientific article

Chemotherapy Combines Effectively with Anti-PD-L1 Treatment and Can Augment Antitumor Responses

article

Discovery and preclinical development of vismodegib

scientific article published on 23 May 2014

Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development

scientific article

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2

scientific article

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.

scientific article published on 16 February 2016

Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2

scientific article

Dogs are more sensitive to antagonists of inhibitor of apoptosis proteins than rats and humans: a translational toxicokinetic/toxicodynamic analysis ⬇️

scientific article published on July 28, 2012

GDC-0449-a potent inhibitor of the hedgehog pathway

scientific article

Generalized additive mixed modeling of longitudinal tumor growth reduces bias and improves decision making in translational oncology

scientific article published on 25 September 2020

Hedgehog signaling is dispensable for adult murine hematopoietic stem cell function and hematopoiesis

scientific article

Identification, Characterization, and Implications of Species-Dependent Plasma Protein Binding for the Oral Hedgehog Pathway Inhibitor Vismodegib (GDC-0449) ⬇️

scientific article published on March 25, 2011

Immunization associated with primary tumor growth leads to rejection of commonly used syngeneic tumors upon tumor rechallenge

scientific article published on 01 July 2020

Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist

scientific article published on 16 September 2013

MAP Kinase Inhibition Promotes T Cell and Anti-tumor Activity in Combination with PD-L1 Checkpoint Blockade

scientific article published on 29 February 2016

Nanosuspension delivery of paclitaxel to xenograft mice can alter drug disposition and anti-tumor activity

scientific article published on April 2014

PRC2-mediated repression of SMARCA2 predicts EZH2 inhibitor activity in SWI/SNF mutant tumors

scientific article

PTEN loss mitigates the response of medulloblastoma to Hedgehog pathway inhibition

scientific article published on 23 October 2013

Pharmacokinetic–Pharmacodynamic Analysis of Vismodegib in Preclinical Models of Mutational and Ligand-Dependent Hedgehog Pathway Activation ⬇️

scientific article published on May 24, 2011

Potent and Selective Aminopyrimidine-Based B-Raf Inhibitors with Favorable Physicochemical and Pharmacokinetic Properties ⬇️

scientific article published on February 29, 2012

Preclinical assessment of novel BRAF inhibitors: integrating pharmacokinetic-pharmacodynamic modelling in the drug discovery process.

scientific article

Prediction of drug distribution in subcutaneous xenografts of human tumor cell lines and healthy tissues in mouse: application of the tissue composition-based model to antineoplastic drugs

scientific article published on 14 January 2015

Pyrazolopyridine Inhibitors of B-Raf V600E . Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors

scientific article

Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway ⬇️

scientific article published on September 15, 2010

Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance ⬇️

scientific article published on January 15, 2011

Smoothened mutation confers resistance to a Hedgehog pathway inhibitor in medulloblastoma.

scientific article

Targeting the PI3K pathway in the brain--efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier

scientific article

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.

scientific article published on 11 September 2012

Translational pharmacokinetic/pharmacodynamic analysis in cancer pharmacology: a tool to maximize the value of antitumor efficacy from tumor bearing mice

scientific article published on September 2016

Translational value of mouse models in oncology drug development

scientific article published on May 2015

Treatment of medulloblastoma with hedgehog pathway inhibitor GDC-0449

scientific article published on 2 September 2009

X chromosome-linked inhibitor of apoptosis regulates cell death induction by proapoptotic receptor agonists

scientific article published on 23 October 2009

List of works by Stephen E. Gould

A cell identity switch allows residual BCC to survive Hedgehog pathway inhibition

A paracrine requirement for hedgehog signalling in cancer

Antitumor Activity of Targeted and Cytotoxic Agents in Murine Subcutaneous Tumor Models Correlates with Clinical Response ⬇️

Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma

Canonical hedgehog signaling augments tumor angiogenesis by induction of VEGF-A in stromal perivascular cells ⬇️

Carcinogenicity assessment of the Hedgehog pathway inhibitor, vismodegib in Tg.rasH2 mice and Sprague-Dawley rats

Chemotherapy Combines Effectively with Anti-PD-L1 Treatment and Can Augment Antitumor Responses

Discovery and preclinical development of vismodegib

Discovery of (S)-1-(1-(4-Chloro-3-fluorophenyl)-2-hydroxyethyl)-4-(2-((1-methyl-1H-pyrazol-5-yl)amino)pyrimidin-4-yl)pyridin-2(1H)-one (GDC-0994), an Extracellular Signal-Regulated Kinase 1/2 (ERK1/2) Inhibitor in Early Clinical Development

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR.

Discovery of highly potent, selective, and efficacious small molecule inhibitors of ERK1/2

Dogs are more sensitive to antagonists of inhibitor of apoptosis proteins than rats and humans: a translational toxicokinetic/toxicodynamic analysis ⬇️

GDC-0449-a potent inhibitor of the hedgehog pathway

Generalized additive mixed modeling of longitudinal tumor growth reduces bias and improves decision making in translational oncology

Hedgehog signaling is dispensable for adult murine hematopoietic stem cell function and hematopoiesis

Identification, Characterization, and Implications of Species-Dependent Plasma Protein Binding for the Oral Hedgehog Pathway Inhibitor Vismodegib (GDC-0449) ⬇️

Immunization associated with primary tumor growth leads to rejection of commonly used syngeneic tumors upon tumor rechallenge

Learning and confirming with preclinical studies: modeling and simulation in the discovery of GDC-0917, an inhibitor of apoptosis proteins antagonist

MAP Kinase Inhibition Promotes T Cell and Anti-tumor Activity in Combination with PD-L1 Checkpoint Blockade

Nanosuspension delivery of paclitaxel to xenograft mice can alter drug disposition and anti-tumor activity

PRC2-mediated repression of SMARCA2 predicts EZH2 inhibitor activity in SWI/SNF mutant tumors

PTEN loss mitigates the response of medulloblastoma to Hedgehog pathway inhibition

Pharmacokinetic–Pharmacodynamic Analysis of Vismodegib in Preclinical Models of Mutational and Ligand-Dependent Hedgehog Pathway Activation ⬇️

Potent and Selective Aminopyrimidine-Based B-Raf Inhibitors with Favorable Physicochemical and Pharmacokinetic Properties ⬇️

Preclinical assessment of novel BRAF inhibitors: integrating pharmacokinetic-pharmacodynamic modelling in the drug discovery process.

Prediction of drug distribution in subcutaneous xenografts of human tumor cell lines and healthy tissues in mouse: application of the tissue composition-based model to antineoplastic drugs

Pyrazolopyridine Inhibitors of B-Raf V600E . Part 1: The Development of Selective, Orally Bioavailable, and Efficacious Inhibitors

Second generation 2-pyridyl biphenyl amide inhibitors of the hedgehog pathway ⬇️

Small Molecule Inhibition of GDC-0449 Refractory Smoothened Mutants and Downstream Mechanisms of Drug Resistance ⬇️

Smoothened mutation confers resistance to a Hedgehog pathway inhibitor in medulloblastoma.

Targeting the PI3K pathway in the brain--efficacy of a PI3K inhibitor optimized to cross the blood-brain barrier

The design and identification of brain penetrant inhibitors of phosphoinositide 3-kinase α.

Translational pharmacokinetic/pharmacodynamic analysis in cancer pharmacology: a tool to maximize the value of antitumor efficacy from tumor bearing mice

Translational value of mouse models in oncology drug development

Treatment of medulloblastoma with hedgehog pathway inhibitor GDC-0449

X chromosome-linked inhibitor of apoptosis regulates cell death induction by proapoptotic receptor agonists