Lista de obras - Spiros Linardopoulos - Dominio Público Uruguay

7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent

artículo científico publicado en 2015

A cancer-associated aurora A mutant is mislocalized and misregulated due to loss of interaction with TPX2

artículo científico publicado en 2009

A chemical inhibitor of PPM1D that selectively kills cells overexpressing PPM1D.

artículo científico publicado en 2007

APC/C is an essential regulator of centrosome clustering

artículo científico publicado en 2014

Adaptation of the plasma inhibitory activity assay to detect Aurora, ABL and FLT3 kinase inhibition by AT9283 in pediatric leukemia.

artículo científico publicado en 2011

Aurora A kinase regulates mammary epithelial cell fate by determining mitotic spindle orientation in a Notch-dependent manner

artículo científico publicado en 2013

Aurora B expression directly correlates with prostate cancer malignancy and influence prostate cell proliferation

artículo científico publicado en 2006

Aurora B overexpression associates with the thyroid carcinoma undifferentiated phenotype and is required for thyroid carcinoma cell proliferation

artículo científico publicado en 2005

Aurora B prevents premature removal of spindle assembly checkpoint proteins from the kinetochore: A key role for Aurora B in mitosis.

artículo científico publicado en 2016

Aurora Kinase Inhibitors: Current Status and Outlook

artículo científico publicado en 2015

Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells

artículo científico publicado en 2013

Aurora kinase inhibition: a new light in the sky?

artículo científico publicado en 2015

Aurora kinase inhibitors: novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemias.

artículo científico publicado en 2010

Aurora-A expressing tumour cells are deficient for homology-directed DNA double strand-break repair and sensitive to PARP inhibition

artículo científico publicado en 2010

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy

artículo científico publicado en 2017

E-Cadherin/ROS1 Inhibitor Synthetic Lethality in Breast Cancer.

artículo científico publicado en 2018

Functional viability profiles of breast cancer

artículo científico publicado en 2011

High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers

scientific article published on 01 October 2019

High levels of phosphorylated c-Jun, Fra-1, Fra-2 and ATF-2 proteins correlate with malignant phenotypes in the multistage mouse skin carcinogenesis model

artículo científico publicado en 2000

Identification of Stk6/STK15 as a candidate low-penetrance tumor-susceptibility gene in mouse and human

artículo científico publicado en 2003

Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate

artículo científico publicado en 2010

Integrated genomics and functional validation identifies malignant cell specific dependencies in triple negative breast cancer.

artículo científico publicado en 2018

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N-neopentyl

artículo científico publicado en 2018

Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance

artículo científico publicado en 2015

New therapeutic perspectives in CCDC6 deficient lung cancer cells

artículo científico publicado en 2014

Optimization of Imidazo[4,5- b ]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia

artículo científico publicado en 2012

PPM1D gene amplification and overexpression in breast cancer: a qRT-PCR and chromogenic in situ hybridization study

artículo científico publicado en 2010

Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach

artículo científico publicado en 2016

Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns

artículo científico publicado en 2012

Sensitization of (colon) cancer cells to death receptor related therapies: a report from the FP6-ONCODEATH research consortium

artículo científico

Structure-Based Design of Orally Bioavailable 1 H -Pyrrolo[3,2- c ]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)

artículo científico publicado en 2013

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells

artículo científico publicado en 2010

Targeting TAO Kinases Using a New Inhibitor Compound Delays Mitosis and Induces Mitotic Cell Death in Centrosome Amplified Breast Cancer Cells.

artículo científico publicado en 2017

Targeting the PPM1D phenotype; 2,4-bisarylthiazoles cause highly selective apoptosis in PPM1D amplified cell-lines.

artículo científico publicado en 2014

The N-terminal domain of the Aurora-A Phe-31 variant encodes an E3 ubiquitin ligase and mediates ubiquitination of IkappaBalpha

artículo científico publicado en 2006

The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo.

artículo científico publicado en 2011

The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design

artículo científico publicado en 2013

Tumour selective targeting of cell cycle kinases for cancer treatment ⬇️

artículo científico publicado el 15 de abril de 2013

Lista de obras de Spiros Linardopoulos

7-(Pyrazol-4-yl)-3H-imidazo[4,5-b]pyridine-based derivatives for kinase inhibition: Co-crystallisation studies with Aurora-A reveal distinct differences in the orientation of the pyrazole N1-substituent

A cancer-associated aurora A mutant is mislocalized and misregulated due to loss of interaction with TPX2

A chemical inhibitor of PPM1D that selectively kills cells overexpressing PPM1D.

APC/C is an essential regulator of centrosome clustering

Adaptation of the plasma inhibitory activity assay to detect Aurora, ABL and FLT3 kinase inhibition by AT9283 in pediatric leukemia.

Aurora A kinase regulates mammary epithelial cell fate by determining mitotic spindle orientation in a Notch-dependent manner

Aurora B expression directly correlates with prostate cancer malignancy and influence prostate cell proliferation

Aurora B overexpression associates with the thyroid carcinoma undifferentiated phenotype and is required for thyroid carcinoma cell proliferation

Aurora B prevents premature removal of spindle assembly checkpoint proteins from the kinetochore: A key role for Aurora B in mitosis.

Aurora Kinase Inhibitors: Current Status and Outlook

Aurora isoform selectivity: design and synthesis of imidazo[4,5-b]pyridine derivatives as highly selective inhibitors of Aurora-A kinase in cells

Aurora kinase inhibition: a new light in the sky?

Aurora kinase inhibitors: novel small molecules with promising activity in acute myeloid and Philadelphia-positive leukemias.

Aurora-A expressing tumour cells are deficient for homology-directed DNA double strand-break repair and sensitive to PARP inhibition

Characterisation of CCT271850, a selective, oral and potent MPS1 inhibitor, used to directly measure in vivo MPS1 inhibition vs therapeutic efficacy

E-Cadherin/ROS1 Inhibitor Synthetic Lethality in Breast Cancer.

Functional viability profiles of breast cancer

High Proliferation Rate and a Compromised Spindle Assembly Checkpoint Confers Sensitivity to the MPS1 Inhibitor BOS172722 in Triple-Negative Breast Cancers

High levels of phosphorylated c-Jun, Fra-1, Fra-2 and ATF-2 proteins correlate with malignant phenotypes in the multistage mouse skin carcinogenesis model

Identification of Stk6/STK15 as a candidate low-penetrance tumor-susceptibility gene in mouse and human

Imidazo[4,5-b]pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate

Integrated genomics and functional validation identifies malignant cell specific dependencies in triple negative breast cancer.

Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N-neopentyl

Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance

New therapeutic perspectives in CCDC6 deficient lung cancer cells

Optimization of Imidazo[4,5- b ]pyridine-Based Kinase Inhibitors: Identification of a Dual FLT3/Aurora Kinase Inhibitor as an Orally Bioavailable Preclinical Development Candidate for the Treatment of Acute Myeloid Leukemia

PPM1D gene amplification and overexpression in breast cancer: a qRT-PCR and chromogenic in situ hybridization study

Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach

Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns

Sensitization of (colon) cancer cells to death receptor related therapies: a report from the FP6-ONCODEATH research consortium

Structure-Based Design of Orally Bioavailable 1 H -Pyrrolo[3,2- c ]pyridine Inhibitors of Mitotic Kinase Monopolar Spindle 1 (MPS1)

Structure-based design of imidazo[1,2-a]pyrazine derivatives as selective inhibitors of Aurora-A kinase in cells

Targeting TAO Kinases Using a New Inhibitor Compound Delays Mitosis and Induces Mitotic Cell Death in Centrosome Amplified Breast Cancer Cells.

Targeting the PPM1D phenotype; 2,4-bisarylthiazoles cause highly selective apoptosis in PPM1D amplified cell-lines.

The N-terminal domain of the Aurora-A Phe-31 variant encodes an E3 ubiquitin ligase and mediates ubiquitination of IkappaBalpha

The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo.

The discovery of potent ribosomal S6 kinase inhibitors by high-throughput screening and structure-guided drug design

Tumour selective targeting of cell cycle kinases for cancer treatment ⬇️