L. Friedman

发表

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

M. Belvin, S. Seshagiri, B. Jaiswal, 2010, Nature.

Corrigendum: Inactivation of PI(3)K p110δ breaks regulatory T-cell-mediated immune tolerance to cancer

Dalya R. Soond, K. Okkenhaug, M. Turner, 2016, Nature.

Drosophila p53 Is a Structural and Functional Homolog of the Tumor Suppressor p53

M. Belvin, L. M. Young, C. Kopczynski, 2000, Cell.

First-in-Human Phase I Study of Pictilisib (GDC-0941), a Potent Pan–Class I Phosphatidylinositol-3-Kinase (PI3K) Inhibitor, in Patients with Advanced Solid Tumors

J. Ware, J. Spoerke, P. Workman, 2014, Clinical Cancer Research.

Systematic generation of high-resolution deletion coverage of the Drosophila melanogaster genome

D. Curtis, T. Kaufman, M. Belvin, 2004, Nature Genetics.

220 POSTER Combination of class I PI3K inhibitor, GDC-0941, with standard of care therapeutics results in enhanced anti-tumor responses in human cancer models in vitro and in vivo

M. Belvin, L. Friedman, D. Sampath, 2008 .

217 POSTER Pre-clinical evaluation of efficacy and PK/PD biomarkers of GDC-0941, a potent class 1 PI3K inhibitor

M. Belvin, L. Friedman, H. Stern, 2008 .

The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer .

Gary Box, Paul Workman, Christian Wiesmann, 2008, Journal of medicinal chemistry.

Discovery of 2-{3-[2-(1-isopropyl-3-methyl-1H-1,2-4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl]-1H-pyrazol-1-yl}-2-methylpropanamide (GDC-0032): a β-sparing phosphoinositide 3-kinase inhibitor with high unbound exposure and robust in vivo antitumor activity.

Steve Price, E. Bradley, BinQing Wei, 2013, Journal of medicinal chemistry.

Isoform-specific phosphoinositide 3-kinase inhibitors exert distinct effects in solid tumors.

M. Belvin, L. Friedman, Leslie B. Lee, 2010, Cancer research.

Discovery of a potent, selective, and orally available class I phosphatidylinositol 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) kinase inhibitor (GDC-0980) for the treatment of cancer.

BinQing Wei, D. Sutherlin, L. Friedman, 2011, Journal of medicinal chemistry.

Hormone-Targeted Therapy and Resistance

L. Friedman, J. Hager, C. Metcalfe, 2018 .

Cancer Therapy: Preclinical TargetingActivatedAktwithGDC-0068, aNovel SelectiveAkt Inhibitor That Is Efficacious in Multiple Tumor Models

Tyler T. Risom, M. Belvin, S. Gross, 2013 .

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors for the treatment of cancer.

D. Sutherlin, S. Sideris, L. Friedman, 2010, Journal of medicinal chemistry.

Brief Definitive Report

A. Angulo, H. Gerhardt, B. Vanhaesebroeck, 2022 .

Nuclear Phospho-Akt Increase Predicts Synergy of PI3K Inhibition and Doxorubicin in Breast and Ovarian Cancer

M. Belvin, L. Friedman, D. Sampath, 2010, Science Translational Medicine.

Discovery of GNE-149 as a Full Antagonist and Efficient Degrader of Estrogen Receptor alpha for ER+ Breast Cancer.

Jun Liang, Y. Ran, L. Friedman, 2020, ACS medicinal chemistry letters.

Inhibition of p110δ PI3K prevents inflammatory response and restenosis after artery injury

A. Bilancio, B. Vanhaesebroeck, L. Friedman, 2017, Bioscience reports.

Predictive and Pharmacodynamic Biomarkers of Response to the Phosphatidylinositol 3-Kinase Inhibitor Taselisib in Breast Cancer Preclinical Models

E. Sokol, T. Wilson, L. Friedman, 2019, Molecular Cancer Therapeutics.

Abstract S6-04: The PI3K inhibitor, taselisib, has enhanced potency in PIK3CA mutant models through a unique mechanism of action

Kyung Song, L. Friedman, D. Sampath, 2016 .

Synthetic Lethality of Retinoblastoma Mutant Cells in the Drosophila Eye by Mutation of a Novel Peptidyl Prolyl Isomerase Gene

F. Chen, M. Belvin, L. M. Young, 2005, Genetics.

Abstract DDT02-01: Discovery of GDC-0032: A beta-sparing PI3K inhibitor active against PIK3CA mutant tumors.

M. Belvin, E. Bradley, M. Ultsch, 2013 .

The PI3K inhibitor GDC-0941 combines with existing clinical regimens for superior activity in multiple myeloma

P. L. Bergsagel, A. Ebens, L. Friedman, 2014, Oncogene.

Abstract A250: Preclinical combination efficacy and identification of biomarkers of MEK and PI3K inhibitors in phase I

M. Belvin, K. Hoeflich, H. Koeppen, 2009 .

Multimodal microvascular imaging reveals that selective inhibition of class I PI3K is sufficient to induce an antivascular response.

N. van Bruggen, H. Koeppen, L. Friedman, 2013, Neoplasia.

Targeting Activated Akt with GDC-0068, a Novel Selective Akt Inhibitor That Is Efficacious in Multiple Tumor Models

Tyler T. Risom, M. Belvin, S. Gross, 2013, Clinical Cancer Research.

In vivo Antitumor Activity of MEK and Phosphatidylinositol 3-Kinase Inhibitors in Basal-Like Breast Cancer Models

Wei Zhou, Guy Cavet, Zachary Boyd, 2009, Clinical Cancer Research.

The oral selective estrogen receptor degrader GDC-0810 (ARN-810) in postmenopausal women with hormone receptor-positive HER2-negative (HR + /HER2 −) advanced/metastatic breast cancer

Carlos L. Arteaga, H. Linden, A. Bardia, 2022, Breast Cancer Research and Treatment.

Abstract 4717:In vitropotency of dual PI3K/mTORC1/C2 inhibitor, GDC-0980 in ER+ and HER2 overexpressing breast cancer cells

B. Leyland-Jones, L. Friedman, P. De, 2015 .

Structure-based optimization of pyrazolo-pyrimidine and -pyridine inhibitors of PI3-kinase.

D. Sutherlin, L. Friedman, Leslie B. Lee, 2010, Bioorganic & medicinal chemistry letters.

Predictive Biomarkers of Sensitivity to the Phosphatidylinositol 3′ Kinase Inhibitor GDC-0941 in Breast Cancer Preclinical Models

M. Belvin, D. Guhathakurta, L. Amler, 2010, Clinical Cancer Research.

Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility

Mamie Yu, A. Daemen, R. Houtman, 2019, Cell.

Hominoid-specific enzyme GLUD2 promotes growth of IDH1R132H glioma

M. Hedehus, A. Daemen, F. Peale, 2014, Proceedings of the National Academy of Sciences.

The PI3K inhibitor taselisib overcomes letrozole resistance in a breast cancer model expressing aromatase

R. Neve, T. Wilson, K. Hoeflich, 2016, Genes & cancer.

GDC-0980 Is a Novel Class I PI3K/mTOR Kinase Inhibitor with Robust Activity in Cancer Models Driven by the PI3K Pathway

M. Belvin, J. Spoerke, D. Sutherlin, 2011, Molecular Cancer Therapeutics.

GDC-0980IsaNovelClassIPI3K/mTORKinaseInhibitorwith RobustActivityinCancerModelsDrivenbythePI3KPathway

M. Belvin, J. Spoerke, D. Sutherlin, 2011 .

Suppression of HER2/HER3-Mediated Growth of Breast Cancer Cells with Combinations of GDC-0941 PI3K Inhibitor, Trastuzumab, and Pertuzumab

M. Belvin, M. Sliwkowski, N. Lewin-Koh, 2009, Clinical Cancer Research.

Akt inhibition promotes autophagy and sensitizes PTEN-null tumors to lysosomotropic agents

David P. Davis, K. Hoeflich, L. Friedman, 2008, The Journal of cell biology.

Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers

Ariana Peck, Shiuh-Ming Luoh, Steve Price, 2013, Nature.

Phosphoproteomic characterization of DNA damage response in melanoma cells following MEK/PI3K dual inhibition

Amy Young, M. Belvin, K. Hoeflich, 2013, Proceedings of the National Academy of Sciences.

A potent combination of the novel PI3K Inhibitor, GDC-0941, with imatinib in gastrointestinal stromal tumor xenografts: long-lasting responses after treatment withdrawal.

J. Fletcher, R. Sciot, G. Floris, 2013, Clinical cancer research : an official journal of the American Association for Cancer Research.

A tipping-point for apoptosis following dual inhibition of HER2 signaling network by T-DM1 plus GDC-0980 maximizes anti-tumor efficacy.

B. Leyland-Jones, L. Friedman, P. De, 2021, American journal of cancer research.

Ligand-independent HER2/HER3/PI3K complex is disrupted by trastuzumab and is effectively inhibited by the PI3K inhibitor GDC-0941.

M. Sliwkowski, L. Friedman, D. Sampath, 2009, Cancer cell.

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.

Siew K. Yeap, M. Ultsch, C. Eigenbrot, 2022, Journal of medicinal chemistry.

RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy

W. Forrest, Kyung Song, L. Friedman, 2021, bioRxiv.

Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression.

M. Belvin, S. Seshagiri, Z. Modrušan, 2009, Cancer research.

Inactivation of the PI3K p110δ breaks regulatory T cell-mediated immune tolerance to cancer

Dalya R. Soond, K. Okkenhaug, B. Vanhaesebroeck, 2014, Nature.

The ect2 rho Guanine nucleotide exchange factor is essential for early mouse development and normal cell cytokinesis and migration.

C. Der, J. Yeh, L. Friedman, 2011, Genes & cancer.

Doubling down on the PI3K-AKT-mTOR pathway enhances the antitumor efficacy of PARP inhibitor in triple negative breast cancer model beyond BRCA-ness.

B. Leyland-Jones, L. Friedman, P. De, 2014, Neoplasia.

Double PIK3CA mutations in cis increase oncogenicity and sensitivity to PI3Kα inhibitors

Jared L. Johnson, H. Shah, B. Taylor, 2019, Science.

Amphiregulin and PTEN evoke a multimodal mechanism of acquired resistance to PI3K inhibition

R. Neve, M. Belvin, T. Wilson, 2014, Genes & cancer.

Phosphoinositide 3-Kinase (PI3K) Pathway Alterations Are Associated with Histologic Subtypes and Are Predictive of Sensitivity to PI3K Inhibitors in Lung Cancer Preclinical Models

G. Hampton, J. Fridlyand, J. Spoerke, 2012, Clinical Cancer Research.

GDC-0941, a Novel Class I Selective PI3K Inhibitor, Enhances the Efficacy of Docetaxel in Human Breast Cancer Models by Increasing Cell Death In Vitro and In Vivo

M. Belvin, H. Koeppen, L. Friedman, 2012, Clinical Cancer Research.

Cancer Therapy: Preclinical GDC-0941, a Novel Class I Selective PI3K Inhibitor, Enhances the Efficacy of Docetaxel in Human Breast CancerModels by Increasing Cell Death In Vitro and In Vivo

M. Belvin, H. Koeppen, L. Friedman, 2012 .

An ATP-Site On-Off Switch That Restricts Phosphatase Accessibility of Akt

B. Brandhuber, S. Gloor, G. Vigers, 2012, Science Signaling.

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

Harvey Wong, Cornelis E C A Hop, F. Theil, 2012, Clinical Cancer Research.

Identifying genotype-dependent efficacy of single and combined PI3K- and MAPK-pathway inhibition in cancer

William Pao, Thomas Zander, Martin Peifer, 2009, Proceedings of the National Academy of Sciences.

Enhanced antitumor immunity through sequential targeting of PI3Kδ and LAG3

B. Vanhaesebroeck, L. Friedman, V. Kersemans, 2020, Journal for ImmunoTherapy of Cancer.

The Rational Design of Selective Benzoxazepin Inhibitors of the α-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-Isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).

S. Steinbacher, Steve Price, E. Gancia, 2016, Journal of medicinal chemistry.

Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.

Jianwen A. Feng, M. Belvin, K. Hoeflich, 2014, Journal of medicinal chemistry.

Systems-wide Analysis of K-Ras, Cdc42, and PAK4 Signaling by Quantitative Phosphoproteomics*

F. Gnad, M. Belvin, K. Hoeflich, 2013, Molecular & Cellular Proteomics.

Plasma Metabolomic Changes following PI3K Inhibition as Pharmacodynamic Biomarkers: Preclinical Discovery to Phase I Trial Evaluation

B. Vanhaesebroeck, P. Workman, L. Friedman, 2016, Molecular Cancer Therapeutics.

The selective estrogen receptor downregulator GDC-0810 is efficacious in diverse models of ER+ breast cancer

K. Walter, Andiliy G. Lai, J. Giltnane, 2016, eLife.

Active PI3K Pathway Causes an Invasive Phenotype Which Can Be Reversed or Promoted by Blocking the Pathway at Divergent Nodes

M. Belvin, A. Bardelli, K. Hoeflich, 2012, PloS one.

P21-activated kinase 1 (PAK1) as a therapeutic target in BRAF wild-type melanoma.

A. Harris, M. Belvin, A. Jubb, 2013, Journal of the National Cancer Institute.

ERK Inhibition Overcomes Acquired Resistance to MEK Inhibitors

Wei Zhou, William F. Forrest, Sherry Heldens, 2012, Molecular Cancer Therapeutics.

GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer.

Siew K. Yeap, N. C. Ray, Jun Liang, 2021, Journal of medicinal chemistry.

Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition.

Mark Merchant, M. Belvin, I. Kasman, 2012, Cancer research.

Targeting the PI3K/Akt pathway in murine MDS/MPN driven by hyperactive Ras

L. Friedman, D. Sampath, B. Braun, 2016, Leukemia.

Quantitative phosphoproteomic analysis of the PI3K‐regulated signaling network

F. Gnad, M. Belvin, G. Hatzivassiliou, 2016, Proteomics.

Phosphoproteome analysis of the MAPK pathway reveals previously undetected feedback mechanisms

F. Gnad, M. Belvin, G. Hatzivassiliou, 2016, Proteomics.

Inactivation of PI(3)K p110 delta breaks regulatory T-cell-mediated immune tolerance to cancer (vol 510, pg 407, 2014)

Roberto Piñeiro, Wayne Pearce, Martin Turner, 2016 .

Antitumor Efficacy of the Novel RAF Inhibitor GDC-0879 Is Predicted by BRAF V600E Mutational Status and Sustained Extracellular

M. Belvin, S. Seshagiri, Z. Modrušan, 2009 .

Abstract 5753: RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

M. Belvin, S. Seshagiri, B. Jaiswal, 2010 .

Orally Bioavailable Small Molecule CD73 Inhibitor (OP-5244) Reverses Immunosuppression Through Blockade of Adenosine Production.

L. Friedman, M. Junttila, V. Fantin, 2020, Journal of medicinal chemistry.

Role of the E3 ubiquitin ligase RNF157 as a novel downstream effector linking PI3K and MAPK signaling pathways to the cell cycle

F. Gnad, M. Belvin, G. Hatzivassiliou, 2017, The Journal of Biological Chemistry.

Abstract P5-04-07: GDC-9545: A novel ER antagonist and clinical candidate that combines desirable mechanistic and pre-clinical DMPK attributes

A. Daemen, J. Giltnane, L. Friedman, 2019, Poster Session Abstracts.

Pyrimidoaminotropanes as potent, selective, and efficacious small molecule kinase inhibitors of the mammalian target of rapamycin (mTOR).

S. Sideris, L. Friedman, S. Malek, 2013, Journal of medicinal chemistry.

Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349.

M. Belvin, C. Ly, S. Sideris, 2013, ACS medicinal chemistry letters.

A Selective PIM Kinase Inhibitor Is Highly Active In Multiple Myeloma: The Biology of Single Agent and PI3K/AKT/mTOR Combination Activity

A. Ebens, L. Friedman, H. Maecker, 2010 .

A Selective PIM Kinase Inhibitor Is Highly Active In Multiple Myeloma: Mechanism of Action and Signal Transduction Studies

A. Ebens, L. Friedman, H. Maecker, 2010 .

Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents

I. Ellis, S. Chin, C. Caldas, 2015, Breast Cancer Research.

Targeting p21-activated kinase 1 (PAK1) to induce apoptosis of tumor cells

A. Harris, M. Belvin, A. Jubb, 2011, Proceedings of the National Academy of Sciences.

p21-activated kinase 1: PAK'ed with potential

A. Harris, M. Belvin, A. Jubb, 2011, Oncotarget.

Discovery of GNE-502 as an Orally Bioavailable and Potent Degrader for Estrogen Receptor Positive Breast Cancer.

Jun Liang, Y. Ran, L. Friedman, 2021, Bioorganic & medicinal chemistry letters.

Abstract 156: Preclinical characterization of GDC-0077, a specific PI3K alpha inhibitor in early clinical development

M. Belvin, Kyung Song, L. Friedman, 2017 .

132 Intermittent dosing of the MEK inhibitor, GDC-0973, and the PI3K inhibitor, GDC-0941, results in prolonged accumulation of Bim and causes strong tumor growth inhibition in vivo

M. Belvin, K. Hoeflich, H. Koeppen, 2010 .

Abstract PD7-05: A first-in-human phase I study to evaluate the oral selective estrogen receptor degrader (SERD), GDC-9545, in postmenopausal women with estrogen receptor-positive (ER+) HER2-negative (HER2-) metastatic breast cancer

E. Winer, S. Loi, A. Bardia, 2020, Poster Spotlight Session Abstracts.

Abstract PD5-10: A first-in-human phase I study to evaluate the oral selective estrogen receptor degrader (SERD), GDC-0927, in postmenopausal women with estrogen receptor positive (ER+) HER2-negative metastatic breast cancer (BC)

A. Bardia, J. Spoerke, J. Giltnane, 2018 .

Abstract 1648: Discovery and evolution of orally bioavailable selective estrogen receptor degraders for ER+ breast cancer: From GDC-0810 to GDC-0927

Jun Liang, A. Daemen, Andiliy G. Lai, 2018, Cancer Chemistry.

mTOR kinase inhibitor potentiates apoptosis of PI3K and MEK inhibitors in diagnostically defined subpopulations.

M. Belvin, L. Friedman, Kui Lin, 2012, Cancer letters.

PAK1 mediates pancreatic cancer cell migration and resistance to MET inhibition

R. Neve, D. Aust, C. Pilarsky, 2014, Journal of Pathology.

Abstract P2-17-01: The PI3K inhibitor GDC-0032 is selectively potent against PIK3CA mutant breast cancer cell lines and tumors

M. Belvin, L. Friedman, D. Sampath, 2013 .

Abstract A11: Antitumor activity of targeted and cytotoxic agents in xenograft models correlates with clinical response: A pharmacokinetic-pharmacodynamic analysis.

L. Friedman, H. Wong, E. Choo, 2011 .

Abstract NG05: Not all “SERDs” are equal: Context-independent ER degradation and full ER antagonism define the next generation of ER therapeutics

May M. Y. Liang-Chu, Mamie Yu, A. Daemen, 2018, Endocrinology.

PI3K inhibitors prime neuroblastoma cells for chemotherapy by shifting the balance towards pro-apoptotic Bcl-2 proteins and enhanced mitochondrial apoptosis

S. Fulda, L. Friedman, K. Debatin, 2011, Oncogene.

Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents

I. Ellis, S. Chin, C. Caldas, 2015, Breast Cancer Research.

Abstract P4-15-02: The PI3K inhibitor GDC-0032 enhances the efficacy of standard of care therapeutics in PI3K alpha mutant breast cancer models

M. Belvin, L. Friedman, D. Sampath, 2013 .

Doubling Down on the PI 3 K-AKT-mTOR Pathway Enhances the Antitumor Efficacy of PARP Inhibitor in Triple Negative Breast Cancer Model beyond BRCA-ness 1 , 2

B. Leyland-Jones, L. Friedman, P. De, 2014 .

Phosphoproteomic characterization of DNA damage response in melanoma cells following MEK/PI3K dual inhibition

M. Belvin, K. Hoeflich, L. Friedman, 2013, Proceedings of the National Academy of Sciences.

Therapeutic Ligands Antagonize Estrogen Receptor Function by Impairing Its Mobility

Mamie Yu, A. Daemen, R. Houtman, 2019, Cell.

Phosphoinositide 3-Kinase (PI3K) Pathway Alterations Are Associated with Histologic Subtypes and Are Predictive of Sensitivity to PI3K Inhibitors in Lung Cancer Preclinical Models

G. Hampton, J. Fridlyand, J. Spoerke, 2012, Clinical Cancer Research.

Abstract 5250: PI3K inhibitors prime neuroblastoma cells for chemotherapy-induced apoptosis apoptosis in vitro and in vivo by shifting the balance towards pro-apoptotic Bcl-2 proteins and increased mitochondrial perturbations

S. Fulda, L. Friedman, K. Debatin, 2010 .