Lista de obras -

2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase

artículo científico publicado en 2011

A 1536-well quantitative high-throughput screen to identify compounds targeting cancer stem cells.

artículo científico publicado en 2012

A Druggable TCF4- and BRD4-Dependent Transcriptional Network Sustains Malignancy in Blastic Plasmacytoid Dendritic Cell Neoplasm

artículo científico publicado en 2016

A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution

artículo científico publicado en 2009

A comparison of the ability of rilpivirine (TMC278) and selected analogues to inhibit clinically relevant HIV-1 reverse transcriptase mutants

artículo científico publicado en 2012

A high-throughput screen for pre-mRNA splicing modulators ⬇️

artículo científico publicado el 25 de marzo de 2011

A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety

artículo científico publicado en 2010

A multiprotein supercomplex controlling oncogenic signalling in lymphoma

artículo científico publicado en 2018

A novel class of ion displacement ligands as antagonists of the αIIbβ3 receptor that limit conformational reorganization of the receptor

artículo científico publicado en 2014

A small molecule inverse agonist for the human thyroid-stimulating hormone receptor

artículo científico publicado en 2010

A small molecule that inhibits OGT activity in cells

artículo científico publicado en 2015

ATF4 Gene Network Mediates Cellular Response to the Anticancer PAD Inhibitor YW3-56 in Triple-Negative Breast Cancer Cells.

artículo científico publicado en 2015

Alteration of the selectivity of DNA cleavage by a deglycobleomycin analogue containing a trithiazole moiety

artículo científico publicado en 2002

Aurora B kinase is a potent and selective target in MYCN-driven neuroblastoma

artículo científico publicado en 2015

Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors

artículo científico publicado en 2014

Brigatinib causes tumor shrinkage in both NF2-deficient meningioma and schwannoma through inhibition of multiple tyrosine kinases but not ALK

artículo científico publicado en 2021

CD28 and ITK signals regulate autoreactive T cell trafficking.

artículo científico publicado en 2013

CP-690,550, a therapeutic agent, inhibits cytokine-mediated Jak3 activation and proliferation of T cells from patients with ATL and HAM/TSP

artículo científico publicado en 2010

Calcium-sensing receptor is a physiologic multimodal chemosensor regulating gastric G-cell growth and gastrin secretion

artículo científico publicado en 2010

Cancer network activity associated with therapeutic response and synergism

artículo científico publicado en 2016

Chemical Screens Identify Drugs that Enhance or Mitigate Cellular Responses to Antibody-Toxin Fusion Proteins

artículo científico publicado en 2016

Chiral kinase inhibitors

artículo científico publicado en 2011

Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma

artículo científico publicado en 2010

Comparison of bioluminescent kinase assays using substrate depletion and product formation

artículo científico publicado en 2009

Comprehensive Mechanistic Analysis of Hits from High-Throughput and Docking Screens against β-Lactamase

artículo científico publicado en 2008

Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2008.

artículo científico publicado en 2009

Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

artículo científico publicado en 2010

Conformationally constrained analogues of bleomycin A5.

artículo científico publicado en 2003

Cooperative epigenetic modulation by cancer amplicon genes

artículo científico publicado en 2010

Design and synthesis of new bicyclic diketopiperazines as scaffolds for receptor probes of structurally diverse functionality.

artículo científico publicado en 2005

Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria

artículo científico publicado en 2011

Drug repurposing screen identifies lestaurtinib amplifies the ability of the poly (ADP-ribose) polymerase 1 inhibitor AG14361 to kill breast cancer associated gene-1 mutant and wild type breast cancer cells

artículo científico publicado en 2014

Enhanced efficacy of JAK1 inhibitor with mTORC1/C2 targeting in smoldering/chronic adult T cell leukemia

scientific article published on 22 October 2020

Environment Dictates Dependence on Mitochondrial Complex I for NAD+ and Aspartate Production and Determines Cancer Cell Sensitivity to Metformin

artículo científico publicado en 2016

Erratum: Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis

article

Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase

artículo científico publicado en 2010

Evaluation of the Activity of Lamivudine and Zidovudine against Ebola Virus

artículo científico publicado en 2016

Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase

artículo científico publicado en 2010

Exploiting synthetic lethality for the therapy of ABC diffuse large B cell lymphoma

artículo científico publicado en 2012

Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors

artículo científico publicado en 2009

Exploratory analysis of kinetic solubility measurements of a small molecule library

artículo científico publicado en 2011

Exploring the cellular activity of camptothecin-triple-helix-forming oligonucleotide conjugates

artículo científico publicado en 2006

Fluorescence spectroscopic profiling of compound libraries

artículo científico publicado en 2008

Functional screening of FGFR4-driven tumorigenesis identifies PI3K/mTOR inhibition as a therapeutic strategy in rhabdomyosarcoma

artículo científico publicado en 2018

Genome-wide Screens Identify Lineage- and Tumor-Specific Genes Modulating MHC-I- and MHC-II-Restricted Immunosurveillance of Human Lymphomas

artículo científico publicado en 2020

High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cells

artículo científico publicado en 2014

High-throughput matrix screening identifies synergistic and antagonistic antimalarial drug combinations

artículo científico publicado en 2015

Hydroxylated tropolones inhibit hepatitis B virus replication by blocking viral ribonuclease H activity

artículo científico publicado en 2014

Identification and Optimization of Inhibitors of Trypanosomal Cysteine Proteases: Cruzain, Rhodesain, and TbCatB

artículo científico publicado en 2010

Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation

artículo científico publicado en 2007

Identification of a potent new chemotype for the selective inhibition of PDE4

artículo científico publicado en 2008

Identification of oxadiazoles as new drug leads for the control of schistosomiasis

artículo científico publicado en 2008

Identification of potent Yes1 kinase inhibitors using a library screening approach

artículo científico publicado en 2013

Inhibition of B Cell Receptor Signaling by Ibrutinib in Primary CNS Lymphoma

artículo científico publicado en 2017

Inhibition of pyruvate kinase M2 by reactive oxygen species contributes to cellular antioxidant responses

artículo científico publicado en 2011

Insulin-dependent diabetes induced by pancreatic beta cell expression of IL-15 and IL-15Rα ⬇️

artículo científico publicado el 31 de julio de 2013

KIF11 and KIF15 mitotic kinesins are potential therapeutic vulnerabilities for malignant peripheral nerve sheath tumors

artículo científico publicado en 2020

Large-scale pharmacological profiling of 3D tumor models of cancer cells.

artículo científico publicado en 2016

Matrix Drug Screen Identifies Synergistic Drug Combinations to Augment SMAC Mimetic Activity in Ovarian Cancer

artículo científico publicado en 2020

Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550).

artículo científico publicado en 2011

Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124

artículo científico publicado en 2010

Multi-Tissue Acceleration of the Mitochondrial Phosphoenolpyruvate Cycle Improves Whole-Body Metabolic Health

artículo científico publicado en 2020

Multiple A2E treatments lead to melanization of rod outer segment-challenged ARPE-19 cells

artículo científico publicado en 2014

Multiplexing high-content flow (HCF) and quantitative high-throughput screening (qHTS) to identify compounds capable of decreasing cell viability, activating caspase 3/7, expressing annexin V, and changing mitochondrial membrane integrity

artículo científico publicado en 2013

N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease

artículo científico publicado en 2007

NMDAR inhibition-independent antidepressant actions of ketamine metabolites.

artículo científico publicado en 2016

Novel Phenotypic Outcomes Identified for a Public Collection of Approved Drugs from a Publicly Accessible Panel of Assays

artículo científico publicado en 2015

Overcoming Acquired Epigenetic Resistance to BTK Inhibitors

artículo científico publicado en 2021

Overcoming adaptive therapy resistance in AML by targeting immune response pathways

scientific article published on 01 September 2019

PfCRT and PfMDR1 modulate interactions of artemisinin derivatives and ion channel blockers

artículo científico publicado en 2016

Phosphodiesterase 4 inhibitors enhance sexual pleasure-seeking activity in rodents

artículo científico publicado en 2011

Playing well with others! Initiating and sustaining successful collaborations between industry, academia and government

artículo científico publicado en 2014

Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis

artículo científico publicado en 2012

Pyruvate kinase M2 regulates Hif-1α activity and IL-1β induction and is a critical determinant of the warburg effect in LPS-activated macrophages

scientific article published on January 2015

Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease

artículo científico publicado en 2010

Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade

artículo científico publicado en 2008

Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death

artículo científico publicado en 2009

Quantitative high-throughput screening using a live-cell cAMP assay identifies small-molecule agonists of the TSH receptor

artículo científico publicado en 2008

RNA Polymerase II Regulates Topoisomerase 1 Activity to Favor Efficient Transcription

artículo científico publicado en 2016

RUC-4: a novel αIIbβ3 antagonist for prehospital therapy of myocardial infarction

artículo científico publicado en 2014

Rigosertib induces mitotic arrest and apoptosis in RAS-driven rhabdomyosarcoma and neuroblastoma

artículo científico publicado en 2020

Rilpivirine analogs potently inhibit drug-resistant HIV-1 mutants

artículo científico publicado en 2016

Selective small molecule inhibitor of the Mycobacterium tuberculosis fumarate hydratase reveals an allosteric regulatory site

scientific journal article

Selective targeting of JAK/STAT signaling is potentiated by Bcl-xL blockade in IL-2-dependent adult T-cell leukemia

artículo científico publicado en 2015

Small-molecule agonists for the thyrotropin receptor stimulate thyroid function in human thyrocytes and mice

artículo científico publicado en 2009

Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: Development of chemical probe ML315 ⬇️

artículo científico publicado el 30 de marzo de 2013

Solid-phase synthesis of bleomycin A(5) and three monosaccharide analogues: exploring the role of the carbohydrate moiety in RNA cleavage

artículo científico publicado en 2002

Solid-phase synthesis of bleomycin group antibiotics. Construction of a 108-member deglycobleomycin library

artículo científico publicado en 2003

Structure-Guided Design of a High-Affinity Platelet Integrin IIb 3 Receptor Antagonist That Disrupts Mg2+ Binding to the MIDAS

artículo científico publicado en 2012

Synthesis and biological evaluation of analogues of the kinase inhibitor nilotinib as Abl and Kit inhibitors ⬇️

artículo científico publicado el 10 de diciembre de 2012

Synthesis and characterization of a BODIPY conjugate of the BCR-ABL kinase inhibitor Tasigna (nilotinib): evidence for transport of Tasigna and its fluorescent derivative by ABC drug transporters

artículo científico publicado en 2011

Synthesis, Activity, and Structural Analysis of Novel α-Hydroxytropolone Inhibitors of Human Immunodeficiency Virus Reverse Transcriptase-Associated Ribonuclease H

artículo científico publicado en 2011

TCR signaling via Tec kinase ITK and interferon regulatory factor 4 (IRF4) regulates CD8 + T-cell differentiation ⬇️

artículo científico publicado el 24 de septiembre de 2012

The Synthesis and Evaluation of Dihydroquinazolin-4-ones and Quinazolin-4-ones as Thyroid Stimulating Hormone Receptor Agonists

artículo científico publicado en 2011

The extracellular calcium-sensing receptor is required for cholecystokinin secretion in response to L-phenylalanine in acutely isolated intestinal I cells

artículo científico publicado en 2011

The inhibition and treatment of breast cancer with poly (ADP-ribose) polymerase (PARP-1) inhibitors

artículo científico publicado en 2006

The phosphatidylinositol-3-phosphate 5-kinase inhibitor apilimod blocks filoviral entry and infection

artículo científico publicado en 2017

The pilot phase of the NIH Chemical Genomics Center

artículo científico publicado en 2009

Therapeutic strategies for diffuse midline glioma from high-throughput combination drug screening

artículo científico publicado en 2019

Total synthesis of LL-Z1640-2 utilizing a late-stage intramolecular Nozaki–Hiyama–Kishi reaction ⬇️

artículo científico publicado el 29 de diciembre de 2010

Transcriptomic profiling and quantitative high-throughput (qHTS) drug screening of CDH1 deficient hereditary diffuse gastric cancer (HDGC) cells identify treatment leads for familial gastric cancer.

artículo científico publicado en 2017

Lista de obras de

2-Oxo-N-aryl-1,2,3,4-tetrahydroquinoline-6-sulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase

A 1536-well quantitative high-throughput screen to identify compounds targeting cancer stem cells.

A Druggable TCF4- and BRD4-Dependent Transcriptional Network Sustains Malignancy in Blastic Plasmacytoid Dendritic Cell Neoplasm

A basis for reduced chemical library inhibition of firefly luciferase obtained from directed evolution

A comparison of the ability of rilpivirine (TMC278) and selected analogues to inhibit clinically relevant HIV-1 reverse transcriptase mutants

A high-throughput screen for pre-mRNA splicing modulators ⬇️

A highly potent and selective caspase 1 inhibitor that utilizes a key 3-cyanopropanoic acid moiety

A multiprotein supercomplex controlling oncogenic signalling in lymphoma

A novel class of ion displacement ligands as antagonists of the αIIbβ3 receptor that limit conformational reorganization of the receptor

A small molecule inverse agonist for the human thyroid-stimulating hormone receptor

A small molecule that inhibits OGT activity in cells

ATF4 Gene Network Mediates Cellular Response to the Anticancer PAD Inhibitor YW3-56 in Triple-Negative Breast Cancer Cells.

Alteration of the selectivity of DNA cleavage by a deglycobleomycin analogue containing a trithiazole moiety

Aurora B kinase is a potent and selective target in MYCN-driven neuroblastoma

Blockade of oncogenic IκB kinase activity in diffuse large B-cell lymphoma by bromodomain and extraterminal domain protein inhibitors

Brigatinib causes tumor shrinkage in both NF2-deficient meningioma and schwannoma through inhibition of multiple tyrosine kinases but not ALK

CD28 and ITK signals regulate autoreactive T cell trafficking.

CP-690,550, a therapeutic agent, inhibits cytokine-mediated Jak3 activation and proliferation of T cells from patients with ATL and HAM/TSP

Calcium-sensing receptor is a physiologic multimodal chemosensor regulating gastric G-cell growth and gastrin secretion

Cancer network activity associated with therapeutic response and synergism

Chemical Screens Identify Drugs that Enhance or Mitigate Cellular Responses to Antibody-Toxin Fusion Proteins

Chiral kinase inhibitors

Chronic active B-cell-receptor signalling in diffuse large B-cell lymphoma

Comparison of bioluminescent kinase assays using substrate depletion and product formation

Comprehensive Mechanistic Analysis of Hits from High-Throughput and Docking Screens against β-Lactamase

Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2008.

Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Conformationally constrained analogues of bleomycin A5.

Cooperative epigenetic modulation by cancer amplicon genes

Design and synthesis of new bicyclic diketopiperazines as scaffolds for receptor probes of structurally diverse functionality.

Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria

Drug repurposing screen identifies lestaurtinib amplifies the ability of the poly (ADP-ribose) polymerase 1 inhibitor AG14361 to kill breast cancer associated gene-1 mutant and wild type breast cancer cells

Enhanced efficacy of JAK1 inhibitor with mTORC1/C2 targeting in smoldering/chronic adult T cell leukemia

Environment Dictates Dependence on Mitochondrial Complex I for NAD+ and Aspartate Production and Determines Cancer Cell Sensitivity to Metformin

Erratum: Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis

Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase

Evaluation of the Activity of Lamivudine and Zidovudine against Ebola Virus

Evaluation of thieno[3,2-b]pyrrole[3,2-d]pyridazinones as activators of the tumor cell specific M2 isoform of pyruvate kinase

Exploiting synthetic lethality for the therapy of ABC diffuse large B cell lymphoma

Exploration and optimization of substituted triazolothiadiazines and triazolopyridazines as PDE4 inhibitors

Exploratory analysis of kinetic solubility measurements of a small molecule library

Exploring the cellular activity of camptothecin-triple-helix-forming oligonucleotide conjugates

Fluorescence spectroscopic profiling of compound libraries

Functional screening of FGFR4-driven tumorigenesis identifies PI3K/mTOR inhibition as a therapeutic strategy in rhabdomyosarcoma

Genome-wide Screens Identify Lineage- and Tumor-Specific Genes Modulating MHC-I- and MHC-II-Restricted Immunosurveillance of Human Lymphomas

High-throughput combinatorial screening identifies drugs that cooperate with ibrutinib to kill activated B-cell-like diffuse large B-cell lymphoma cells

High-throughput matrix screening identifies synergistic and antagonistic antimalarial drug combinations

Hydroxylated tropolones inhibit hepatitis B virus replication by blocking viral ribonuclease H activity

Identification and Optimization of Inhibitors of Trypanosomal Cysteine Proteases: Cruzain, Rhodesain, and TbCatB

Identification of N-(quinolin-8-yl)benzenesulfonamides as agents capable of down-regulating NFkappaB activity within two separate high-throughput screens of NFkappaB activation

Identification of a potent new chemotype for the selective inhibition of PDE4

Identification of oxadiazoles as new drug leads for the control of schistosomiasis

Identification of potent Yes1 kinase inhibitors using a library screening approach

Inhibition of B Cell Receptor Signaling by Ibrutinib in Primary CNS Lymphoma

Inhibition of pyruvate kinase M2 by reactive oxygen species contributes to cellular antioxidant responses

Insulin-dependent diabetes induced by pancreatic beta cell expression of IL-15 and IL-15Rα ⬇️

KIF11 and KIF15 mitotic kinesins are potential therapeutic vulnerabilities for malignant peripheral nerve sheath tumors

Large-scale pharmacological profiling of 3D tumor models of cancer cells.

Matrix Drug Screen Identifies Synergistic Drug Combinations to Augment SMAC Mimetic Activity in Ovarian Cancer

Modulation of innate and adaptive immune responses by tofacitinib (CP-690,550).

Molecular basis for the high-affinity binding and stabilization of firefly luciferase by PTC124

Multi-Tissue Acceleration of the Mitochondrial Phosphoenolpyruvate Cycle Improves Whole-Body Metabolic Health

Multiple A2E treatments lead to melanization of rod outer segment-challenged ARPE-19 cells

Multiplexing high-content flow (HCF) and quantitative high-throughput screening (qHTS) to identify compounds capable of decreasing cell viability, activating caspase 3/7, expressing annexin V, and changing mitochondrial membrane integrity

N4-phenyl modifications of N2-(2-hydroxyl)ethyl-6-(pyrrolidin-1-yl)-1,3,5-triazine-2,4-diamines enhance glucocerebrosidase inhibition by small molecules with potential as chemical chaperones for Gaucher disease

NMDAR inhibition-independent antidepressant actions of ketamine metabolites.

Novel Phenotypic Outcomes Identified for a Public Collection of Approved Drugs from a Publicly Accessible Panel of Assays

Overcoming Acquired Epigenetic Resistance to BTK Inhibitors

Overcoming adaptive therapy resistance in AML by targeting immune response pathways

PfCRT and PfMDR1 modulate interactions of artemisinin derivatives and ion channel blockers

Phosphodiesterase 4 inhibitors enhance sexual pleasure-seeking activity in rodents

Playing well with others! Initiating and sustaining successful collaborations between industry, academia and government

Pyruvate kinase M2 activators promote tetramer formation and suppress tumorigenesis

Pyruvate kinase M2 regulates Hif-1α activity and IL-1β induction and is a critical determinant of the warburg effect in LPS-activated macrophages

Quantitative analyses of aggregation, autofluorescence, and reactivity artifacts in a screen for inhibitors of a thiol protease

Quantitative high-throughput screen identifies inhibitors of the Schistosoma mansoni redox cascade

Quantitative high-throughput screening identifies inhibitors of anthrax-induced cell death

Quantitative high-throughput screening using a live-cell cAMP assay identifies small-molecule agonists of the TSH receptor

RNA Polymerase II Regulates Topoisomerase 1 Activity to Favor Efficient Transcription