T. Smeal

发表

Nek6 Mediates Human Cancer Cell Transformation and Is a Potential Cancer Therapeutic Target

T. Abrams, Lihua Shao, Rounak Nassirpour, 2010, Molecular Cancer Research.

c-Jun N-terminal phosphorylation correlates with activation of the JNK subgroup but not the ERK subgroup of mitogen-activated protein kinases

M. Cobb, R. Davis, B. Dérijard, 1994 .

Activation of protein kinase C decreases phosphorylation of c-Jun at sites that negatively regulate its DNA-binding activity

Tony Hunter, James R. Woodgett, Tod Smeal, 1991, Cell.

Oncoprotein-mediated signalling cascade stimulates c-Jun activity by phosphorylation of serines 63 and 73

M. Karin, D. Mercola, U. Rapp, 1992, Molecular and cellular biology.

The mammalian ultraviolet response is triggered by activation of src tyrosine kinases

M. Karin, R. Gottlieb, T. Smeal, 1992, Cell.

Dihydroxylphenyl amides as inhibitors of the Hsp90 molecular chaperone.

L. Funk, P. Kung, J. Meng, 2008, Bioorganic & medicinal chemistry letters.

The c-fos protein interacts with c-Jun AP-1 to stimulate transcription of AP-1 responsive genes

T. Hunter, M. Karin, W. J. Boyle, 1988, Cell.

A Glycine-Dependent Riboswitch That Uses Cooperative Binding to Control Gene Expression

Dan Mercola, Tod Smeal, Michael Karin, 2004 .

PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models.

Shibing Deng, Hui Wang, Shinji Yamazaki, 2015, Cancer cell.

Targeting 3-Phosphoinoside-Dependent Kinase-1 to Inhibit Insulin-Like Growth Factor-I Induced AKT and p70 S6 Kinase Activation in Breast Cancer Cells

T. Smeal, M. Yin, S. Baxi, 2012, PloS one.

Activation of cAMP and mitogen responsive genes relies on a common nuclear factor

M. Karin, M. Montminy, J. Arias, 1994, Nature.

Mechanisms of cellular senescence.

L. Guarente, T. Smeal, 1997, Current opinion in genetics & development.

Evaluation of Selective γ-Secretase Inhibitor PF-03084014 for Its Antitumor Efficacy and Gastrointestinal Safety to Guide Optimal Clinical Trial Design

P. Wei, T. Smeal, N. Hosea, 2010, Molecular Cancer Therapeutics.

Translational Modeling for An Orally Available Novel Inhibitor of Anaplastic Lymphoma Kinase and c-Ros

S. Yamazaki, H. Zou, P. Vicini, 2014 .

Biomarker and Pharmacologic Evaluation of the γ-Secretase Inhibitor PF-03084014 in Breast Cancer Models

P. Rejto, A. Pavlícek, J. Christensen, 2012, Clinical Cancer Research.

PF-06463922 is a potent and selective next-generation ROS1/ALK inhibitor capable of blocking crizotinib-resistant ROS1 mutations

M. McTigue, Sergei L Timofeevski, Qiuhua Li, 2015, Proceedings of the National Academy of Sciences.

A novel CXCR4 antagonist IgG1 antibody (PF-06747143) for the treatment of hematologic malignancies.

E. Blasi, T. Smeal, M. Spilker, 2014, Blood advances.

Pharmacodynamic Relationships in Nonclinical Tumor Models: A Case Study of Orally Available Novel Inhibitors of Anaplastic Lymphoma Kinase AUTHORS:

S. Yamazaki, H. Zou, P. Vicini, 2014 .

Pharmacodynamic Relationships in Nonclinical Tumor Models: A Case Study of Orally Available Novel Inhibitors of Anaplastic Lymphoma Kinase AUTHORS:

S. Yamazaki, H. Zou, P. Vicini, 2014 .

Jun and v-jun contain multiple regions that participate in transcriptional activation in an interdependent manner.

M. Karin, P. Angel, T. Smeal, 1989, The New biologist.

The c-jun Gene and its Role in Signal Transduction

M. Karin, P. Angel, T. Smeal, 1989 .

Cancer Therapy : Preclinical Biomarker and Pharmacologic Evaluation of the g-Secretase Inhibitor PF-03084014 in Breast Cancer Models

P. Rejto, A. Pavlícek, J. Christensen, 2012 .

Altering the specificity of signal transduction cascades: positive regulation of c‐Jun transcriptional activity by protein kinase A.

M. Karin, M. Hibi, T. Smeal, 1994, The EMBO journal.

The jun proto-oncogene is positively autoregulated by its product, Jun/AP-1

Peter Angel, Kazue Hattori, Tod Smeal, 1988, Cell.

Control of AP-1 activity by signal transduction cascades.

M. Karin, A. Lin, J. Chambard, 1993, Advances in second messenger and phosphoprotein research.

Targeting primary acute myeloid leukemia with a new CXCR4 antagonist IgG1 antibody (PF-06747143)

F. Delhommeau, S. de Botton, D. Trajkovic, 2017, Scientific Reports.

Discovery of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a macrocyclic inhibitor of anaplastic lymphoma kinase (ALK) and c-ros oncogene 1 (ROS1) with preclinical brain expos

Wei Liu, Huichun Zhu, Dac Dinh, 2014, Journal of medicinal chemistry.

Villin sequence and peptide map identify six homologous domains.

P. Matsudaira, T. Smeal, R. Jakes, 1988, Proceedings of the National Academy of Sciences of the United States of America.

Identification of an oncoprotein- and UV-responsive protein kinase that binds and potentiates the c-Jun activation domain.

M. Karin, A. Lin, M. Hibi, 1993, Genes & development.

Abstract A277: PF-06463922, a novel ROS1/ALK inhibitor, demonstrates sub-nanomolar potency against oncogenic ROS1 fusions and capable of blocking the resistant ROS1G2032R mutant in preclinical tumor models.

Sergei L Timofeevski, S. Yamazaki, Qiuhua Li, 2013 .

kinases.subgroup of mitogen-activated protein the with activation of the JNK subgroup but not c-Jun N-terminal phosphorylation correlates

M. Cobb, A. Lin, A. Minden, 2013 .

Discovery of (10R)-7-Amino-12-Fluoro-2,10,16-Trimethyl-15-Oxo-10,15,16,17-Tetrahydro-2H-8,4-(Metheno)Pyrazolo[4,3-H][2,5,11]Benzoxadiazacyclotetradecine-3-Carbonitrile (Pf-06463922), a Macrocyclic Inhibitor of Alk/Ros1 with Pre-Clinical Brain Exposure and Broad Spectrum Potency Against Alk-Resistant

Huichun Zhu, Benjamin J. Burke, John Charles Kath, 2014 .

Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F.

G. Getz, A. Iafrate, J. Engelman, 2016, The New England journal of medicine.

Control of transcription factors by signal transduction pathways: the beginning of the end.

M. Karin, T. Smeal, 1992, Trends in biochemical sciences.

Transcriptional interference between c-Jun and the glucocorticoid receptor: Mutual inhibition of DNA binding due to direct protein-protein interaction

M. Karin, J. Drouin, J. Chambard, 1990, Cell.

Targeting the CXCR4 pathway using a novel anti-CXCR4 IgG1 antibody (PF-06747143) in chronic lymphocytic leukemia

L. Rassenti, T. Kipps, T. Smeal, 2017, Journal of Hematology & Oncology.

DNA‐binding activity of jun is increased through its interaction with Fos

B. Spiegelman, M. Karin, P. Angel, 1990, Journal of cellular biochemistry.

Ha-Ras augments c-Jun activity and stimulates phosphorylation of its activation domain

M. Karin, T. Smeal, B. Binétruy, 1991, Nature.

The ALK inhibitor PF-06463922 is effective as a single agent in neuroblastoma driven by expression of ALK and MYCN

S. Robinson, R. Palmer, B. Hallberg, 2016, Disease Models & Mechanisms.

A Phase I Pharmacologic Study of Necitumumab (imc-11f8), a Fully Human Igg1 Monoclonal Antibody the Alk/ros1 Inhibitor Pf-06463922 Overcomes Primary Resistance to Crizotinib in Alk-driven Neuroblastoma

H. Zou, Y. Mossé, M. Lemmon, 2022 .

Sensitivity of Selected Human Tumor Models to PF-04217903, a Novel Selective c-Met Kinase Inhibitor

Shinji Yamazaki, Tod Smeal, J. Christensen, 2012, Molecular Cancer Therapeutics.

Loss of Transcriptional Silencing Causes Sterility in Old Mother Cells of S. cerevisiae

B. Kennedy, L. Guarente, T. Smeal, 1996, Cell.

The ALK / ROS 1 inhibitor PF-06463922 overcomes primary 1 resistance to crizotinib in ALK-driven neuroblastoma 2 3

H. Zou, Y. Mossé, M. Lemmon, 2015 .

Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.

N. Sach, Hong Shen, M. McTigue, 2014, Journal of medicinal chemistry.

Requirement for PAK4 in the Anchorage-independent Growth of Human Cancer Cell Lines*

D. Whyte, J. Bischoff, B. Jallal, 2002, The Journal of Biological Chemistry.

c-Jun N-terminal phosphorylation correlates with activation of the JNK subgroup but not the ERK subgroup of mitogen-activated protein kinases

M. Karin, M. Cobb, R. Davis, 1994, Molecular and cellular biology.

Casein kinase II is a negative regulator of c-Jun DNA binding and AP-1 activity

D. Brenner, J. Frost, T. Hunter, 1992, Cell.

Oncogenic and transcriptional cooperation with Ha-Ras requires phosphorylation of c-Jun on serines 63 and 73

M. Karin, D. Mercola, M. Birrer, 1991, Nature.

Mechanisms of intrinsic and acquired resistance to kinase‐targeted therapies

R. Abraham, S. Bagrodia, T. Smeal, 2012, Pigment cell & melanoma research.

Cancer Therapy : Preclinical Targeting Small Cell Lung Cancer Harboring PIK 3 CA Mutation with a Selective Oral PI 3 K Inhibitor PF-4989216

K. Liu, T. Smeal, M. Yin, 2014 .

Targeting Small Cell Lung Cancer Harboring PIK3CA Mutation with a Selective Oral PI3K Inhibitor PF-4989216

K. Liu, T. Smeal, M. Yin, 2013, Clinical Cancer Research.

Preclinical Development Sensitivity ofSelectedHumanTumorModels toPF-04217903 , a Novel Selective c-Met Kinase Inhibitor

J. Christensen, J. Cui, M. McTigue, 2012 .

Small-molecule p21-activated kinase inhibitor PF-3758309 is a potent inhibitor of oncogenic signaling and tumor growth

D. Knighton, J. Lamerdin, J. Christensen, 2010, Proceedings of the National Academy of Sciences.

The Serine/Threonine Kinase Nek6 Is Required for Cell Cycle Progression through Mitosis*

D. Voehringer, Lihua Shao, B. Jallal, 2003, Journal of Biological Chemistry.

Different requirements for formation of Jun: Jun and Jun: Fos complexes.

M. Karin, P. Angel, T. Smeal, 1989, Genes & development.

Discovery of pyrroloaminopyrazoles as novel PAK inhibitors.

D. Bouzida, J. Christensen, R. Kania, 2012, Journal of medicinal chemistry.

PAK4 mediates morphological changes through the regulation of GEF-H1

M. Gishizky, B. Jallal, T. Smeal, 2005, Journal of Cell Science.

Translational Pharmacokinetic-Pharmacodynamic Modeling for an Orally Available Novel Inhibitor of Anaplastic Lymphoma Kinase and c-Ros Oncogene 1

Paolo Vicini, Hui Wang, Shinji Yamazaki, 2014, The Journal of Pharmacology and Experimental Therapeutics.

Translational Pharmacokinetic-Pharmacodynamic Modeling for An Orally Available Novel Inhibitor of Anaplastic Lymphoma Kinase and c-Ros

S. Yamazaki, H. Zou, P. Vicini, 2014 .

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.

Deepak Dalvie, Michael Zientek, Rose Ann Ferre, 2016, Journal of medicinal chemistry.

Epithelial Tissue Hyperplasia Induced by the RAF Inhibitor PF-04880594 Is Attenuated by a Clinically Well-Tolerated Dose of the MEK Inhibitor PD-0325901

S. Yamazaki, D. Wojciechowicz, S. Bagrodia, 2012, Molecular Cancer Therapeutics.

Targeting Acute Myeloid Leukemia with a New CXCR4 Antagonist IgG1 Antibody (PF-06747143)in NOD/SCID Mice

W. Vainchenker, T. Smeal, O. Legrand, 2015 .

RETRACTED: A novel class of specific Hsp90 small molecule inhibitors demonstrate in vitro and in vivo anti-tumor activity in human melanoma cells.

P. Kung, S. Yamazaki, M. Gehring, 2011, Cancer letters.

Abstract 5245: Identification and characterization of the IDO1 inhibitor LY3381916

J. F. Schindler, M. Kalos, D. Clawson, 2018, Experimental and Molecular Therapeutics.

Casein kinase II is a negative regulator of c-Jun DNA binding and AP-1 activity.

J. Frost, T. Hunter, M. Karin, 1992, Cell.

Mechanisms of intrinsic and acquired resistance to kinase‐targeted therapies

R. Abraham, S. Bagrodia, T. Smeal, 2012, Pigment cell & melanoma research.

Resensitization to Crizotinib by the Lorlatinib ALK Resistance Mutation L1198F.

G. Getz, A. Iafrate, J. Engelman, 2016, The New England journal of medicine.

Abstract PR10: Is CNS availability for oncology a no-brainer? Discovery of PF-06463922, a novel small molecule inhibitor of ALK/ROS1 with preclinical brain availability and broad spectrum potency against ALK-resistant mutations.

N. Sach, M. McTigue, H. Zou, 2013 .

Abstract C253: PF-06463922, a novel brain-penetrating small molecule inhibitor of ALK/ROS1 with potent activity against a broad spectrum of ALK resistant mutations in preclinical models in vitro and in vivo.

Sergei L Timofeevski, S. Yamazaki, Qiuhua Li, 2013 .

K. Gajiwala, N. Sach, Sherry L. Niessen, 2016, Journal of medicinal chemistry.

Sensitivity of Selected Human Tumor Models to PF-04217903, a Novel Selective c-Met Kinase Inhibitor

J. Christensen, J. Cui, M. McTigue, 2012, Molecular Cancer Therapeutics.

Mechanistic Understanding of Translational Pharmacokinetic-Pharmacodynamic Relationships in Nonclinical Tumor Models: A Case Study of Orally Available Novel Inhibitors of Anaplastic Lymphoma Kinase

S. Yamazaki, H. Zou, P. Vicini, 2015, Drug Metabolism and Disposition.

N. Sach, H. Zou, R. Kania, 2014 .