List of works - Layton H. Smith

A Systematic Approach to Identify Biased Agonists of the Apelin Receptor through High-Throughput Screening

scientific article published on 17 March 2017

A chemical biology approach identified PI3K as a potential therapeutic target for neurofibromatosis type 2

scientific article

APJ acts as a dual receptor in cardiac hypertrophy ⬇️

scientific article published on August 16, 2012

Antidiabetic drug metformin (GlucophageR) increases biogenesis of Alzheimer's amyloid peptides via up-regulating BACE1 transcription.

scholarly article

Apelin protects against angiotensin II-induced cardiovascular fibrosis and decreases plasminogen activator inhibitor type-1 production.

scientific article published on April 2011

Assessment of drug-induced arrhythmic risk using limit cycle and autocorrelation analysis of human iPSC-cardiomyocyte contractility

scientific article

Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11.

scientific article published on 28 February 2017

Chemical biology strategy reveals pathway-selective inhibitor of NF-kappaB activation induced by protein kinase C

scientific article

Computational tools and resources for metabolism-related property predictions. 2. Application to prediction of half-life time in human liver microsomes

scientific article

Design, synthesis and evaluation of benzoisothiazolones as selective inhibitors of PHOSPHO1.

scientific article

Development of (E)-2-((1,4-dimethylpiperazin-2-ylidene)amino)-5-nitro-N-phenylbenzamide, ML336: Novel 2-amidinophenylbenzamides as potent inhibitors of venezuelan equine encephalitis virus

scientific article

Differential and opposing regulation of PAI-1 promoter activity by estrogen receptor alpha and estrogen receptor beta in endothelial cells

scientific article

Discovery and validation of a series of aryl sulfonamides as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP).

scientific article

Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor

scientific article

Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.

scientific article

Discovery of ML358, a Selective Small Molecule Inhibitor of the SKN-1 Pathway Involved in Drug Detoxification and Resistance in Nematodes.

scientific article published on 6 May 2015

Discovery of Novel Small-Molecule Inducers of Heme Oxygenase-1 That Protect Human iPSC-Derived Cardiomyocytes from Oxidative Stress

scientific article

Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.

scientific article

Discovery of Sulfonamidebenzamides as Selective Apoptotic CHOP Pathway Activators of the Unfolded Protein Response

scientific article

Downregulation of the Apelinergic Axis Accelerates Aging, whereas Its Systemic Restoration Improves the Mammalian Healthspan

scientific article published in November 2017

Exendin-4 improves cardiac function in mice overexpressing monocyte chemoattractant protein-1 in cardiomyocytes.

scientific article

HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter

scientific article

High-throughput screening for small-molecule inhibitors of plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase

scientific article

Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation ⬇️

scientific article published on August 5, 2011

Image analysis algorithms for immunohistochemical assessment of cell death events and fibrosis in tissue sections

scientific article published on 16 March 2009

Imidazole-derived agonists for the neurotensin 1 receptor.

scientific article

In Vivo Rapid Assessment of Compound Exposure (RACE) for Profiling the Pharmacokinetics of Novel Chemical Probes

scientific article published on December 2012

Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules

scientific article

Pivotal role of PAI-1 in a murine model of hepatic vein thrombosis

scientific article published on 13 September 2005

Plasminogen activator inhibitor-1 antagonist TM5441 attenuates Nω-nitro-L-arginine methyl ester-induced hypertension and vascular senescence

scientific article published on 03 October 2013

Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia.

scientific article published on 3 May 2011

Regulation of the PAI-1 promoter by circadian clock components: differential activation by BMAL1 and BMAL2

scientific article

Repurposing antimalarial aminoquinolines and related compounds for treatment of retinal neovascularization

scientific article published in PLoS ONE

Survivin as a therapeutic target in Sonic hedgehog-driven medulloblastoma

scientific article

Targeting the IRE1α/XBP1 and ATF6 arms of the unfolded protein response enhances VEGF blockade to prevent retinal and choroidal neovascularization.

scientific article

Targeting α-synuclein oligomers by protein-fragment complementation for drug discovery in synucleinopathies

scientific article

The apelin receptor inhibits the angiotensin II type 1 receptor via allosteric trans‐inhibition ⬇️

scientific article published on March 1, 2013

List of works by Layton H. Smith

A Systematic Approach to Identify Biased Agonists of the Apelin Receptor through High-Throughput Screening

A chemical biology approach identified PI3K as a potential therapeutic target for neurofibromatosis type 2

APJ acts as a dual receptor in cardiac hypertrophy ⬇️

Antidiabetic drug metformin (GlucophageR) increases biogenesis of Alzheimer's amyloid peptides via up-regulating BACE1 transcription.

Apelin protects against angiotensin II-induced cardiovascular fibrosis and decreases plasminogen activator inhibitor type-1 production.

Assessment of drug-induced arrhythmic risk using limit cycle and autocorrelation analysis of human iPSC-cardiomyocyte contractility

Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11.

Chemical biology strategy reveals pathway-selective inhibitor of NF-kappaB activation induced by protein kinase C

Computational tools and resources for metabolism-related property predictions. 2. Application to prediction of half-life time in human liver microsomes

Design, synthesis and evaluation of benzoisothiazolones as selective inhibitors of PHOSPHO1.

Development of (E)-2-((1,4-dimethylpiperazin-2-ylidene)amino)-5-nitro-N-phenylbenzamide, ML336: Novel 2-amidinophenylbenzamides as potent inhibitors of venezuelan equine encephalitis virus

Differential and opposing regulation of PAI-1 promoter activity by estrogen receptor alpha and estrogen receptor beta in endothelial cells

Discovery and validation of a series of aryl sulfonamides as selective inhibitors of tissue-nonspecific alkaline phosphatase (TNAP).

Discovery of 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate (ML221) as a functional antagonist of the apelin (APJ) receptor

Discovery of ML314, a Brain Penetrant Non-Peptidic β-Arrestin Biased Agonist of the Neurotensin NTR1 Receptor.

Discovery of ML358, a Selective Small Molecule Inhibitor of the SKN-1 Pathway Involved in Drug Detoxification and Resistance in Nematodes.

Discovery of Novel Small-Molecule Inducers of Heme Oxygenase-1 That Protect Human iPSC-Derived Cardiomyocytes from Oxidative Stress

Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy.

Discovery of Sulfonamidebenzamides as Selective Apoptotic CHOP Pathway Activators of the Unfolded Protein Response

Downregulation of the Apelinergic Axis Accelerates Aging, whereas Its Systemic Restoration Improves the Mammalian Healthspan

Exendin-4 improves cardiac function in mice overexpressing monocyte chemoattractant protein-1 in cardiomyocytes.

HNF4α antagonists discovered by a high-throughput screen for modulators of the human insulin promoter

High-throughput screening for small-molecule inhibitors of plasmodium falciparum glucose-6-phosphate dehydrogenase 6-phosphogluconolactonase

Identification of Inhibitors of NOD1-Induced Nuclear Factor-κB Activation ⬇️

Image analysis algorithms for immunohistochemical assessment of cell death events and fibrosis in tissue sections

Imidazole-derived agonists for the neurotensin 1 receptor.

In Vivo Rapid Assessment of Compound Exposure (RACE) for Profiling the Pharmacokinetics of Novel Chemical Probes

Inhibition of protein kinase C-driven nuclear factor-kappaB activation: synthesis, structure-activity relationship, and pharmacological profiling of pathway specific benzimidazole probe molecules

Pivotal role of PAI-1 in a murine model of hepatic vein thrombosis

Plasminogen activator inhibitor-1 antagonist TM5441 attenuates Nω-nitro-L-arginine methyl ester-induced hypertension and vascular senescence

Potent, selective, and orally available benzoisothiazolone phosphomannose isomerase inhibitors as probes for congenital disorder of glycosylation Ia.

Regulation of the PAI-1 promoter by circadian clock components: differential activation by BMAL1 and BMAL2

Repurposing antimalarial aminoquinolines and related compounds for treatment of retinal neovascularization

Survivin as a therapeutic target in Sonic hedgehog-driven medulloblastoma

Targeting the IRE1α/XBP1 and ATF6 arms of the unfolded protein response enhances VEGF blockade to prevent retinal and choroidal neovascularization.

Targeting α-synuclein oligomers by protein-fragment complementation for drug discovery in synucleinopathies

The apelin receptor inhibits the angiotensin II type 1 receptor via allosteric trans‐inhibition ⬇️