Rational Alteration of Pharmacokinetics of Chiral Fluorinated and Deuterated Derivatives of Emixustat for Retinal Therapy

Shedding new light on the generation of the visual chromophore

(2020) Krzysztof Palczewski et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Effects of emixustat hydrochloride in patients with proliferative diabetic retinopathy: a randomized, placebo-controlled phase 2 study

(2020) Ryo Kubota et al.   GRAEFES ARCHIVE FOR CLINICAL AND EXPERIMENTAL OPHTHALMOLOGY

Randomised study evaluating the pharmacodynamics of emixustat hydrochloride in subjects with macular atrophy secondary to Stargardt disease

(2020) Ryo Kubota et al.   BRITISH JOURNAL OF OPHTHALMOLOGY

Oxidative Deamination of Emixustat by Human Vascular Adhesion Protein-1/Semicarbazide-Sensitive Amine Oxidase

(2019) Michael J. Reid et al.   DRUG METABOLISM AND DISPOSITION

Stereoselective Synthesis of syn-γ-Hydroxynorvaline and Related α-Amino Acids

(2019) Dominika Valachová et al.   SYNTHESIS-STUTTGART

Pharmacotherapy for metabolic and cellular stress in degenerative retinal diseases

(2019) Ryo Kubota et al.   DRUG DISCOVERY TODAY

An Expedient Synthesis of CMF-019: (S)-5-Methyl-3-{1-(pentan-3-yl)-2-(thiophen-2-ylmethyl)-1H-benzo[d]imidazole-5-carboxamido}hexanoic acid, a Potent Apelin Receptor (APJ) Agonist

(2018) Lena Trifonov et al.   Medicinal Chemistry

Emixustat Hydrochloride for Geographic Atrophy Secondary to Age-Related Macular Degeneration

(2018) Philip J. Rosenfeld et al.   OPHTHALMOLOGY

Validation and reproducibility of an LC–MS/MS method for emixustat and its three deaminated metabolites in human plasma

(2018) Terry Podoll et al.   Bioanalysis

Rational Tuning of Visual Cycle Modulator Pharmacodynamics

(2017) Philip D. Kiser et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

MolProbity: More and better reference data for improved all-atom structure validation

(2017) Christopher J. Williams et al.   PROTEIN SCIENCE

Disposition, profiling and identification of emixustat and its metabolites in humans

(2017) Michael E. Fitzsimmons et al.   XENOBIOTICA

Decomposition of Intermolecular Interaction Energies within the Local Pair Natural Orbital Coupled Cluster Framework

(2016) Wolfgang B. Schneider et al.   Journal of Chemical Theory and Computation

Asymmetric Hydrogenation of β-Secondary Amino Ketones Catalyzed by a Ruthenocenyl Phosphino-oxazoline-ruthenium Complex (RuPHOX-Ru): the Synthesis of γ-Secondary Amino Alcohols

(2015) Jianxia Wang et al.   ADVANCED SYNTHESIS & CATALYSIS

Molecular pharmacodynamics of emixustat in protection against retinal degeneration

(2015) Jianye Zhang et al.   JOURNAL OF CLINICAL INVESTIGATION

Applications of Fluorine in Medicinal Chemistry

(2015) Eric P. Gillis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Catalytic mechanism of a retinoid isomerase essential for vertebrate vision

(2015) Philip D Kiser et al.   Nature Chemical Biology

PHASE II, RANDOMIZED, PLACEBO-CONTROLLED, 90-DAY STUDY OF EMIXUSTAT HYDROCHLORIDE IN GEOGRAPHIC ATROPHY ASSOCIATED WITH DRY AGE-RELATED MACULAR DEGENERATION

(2015) Pravin U. Dugel et al.   RETINA-THE JOURNAL OF RETINAL AND VITREOUS DISEASES

Bioanalysis of emixustat (ACU-4429) in whole blood collected with volumetric absorptive microsampling by LC–MS/MS

(2015) Zhixin Miao et al.   Bioanalysis

Visual Cycle Modulation as an Approach toward Preservation of Retinal Integrity

(2015) Claes Bavik et al.   PLoS One

Analysis of Carotenoid Isomerase Activity in a Prototypical Carotenoid Cleavage Enzyme, Apocarotenoid Oxygenase (ACO)

(2014) Xuewu Sui et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Natural triple excitations in local coupled cluster calculations with pair natural orbitals

(2013) Christoph Riplinger et al.   JOURNAL OF CHEMICAL PHYSICS

An efficient and near linear scaling pair natural orbital based local coupled cluster method

(2013) Christoph Riplinger et al.   JOURNAL OF CHEMICAL PHYSICS

Using Deuterium in Drug Discovery: Leaving the Label in the Drug

(2013) Thomas G. Gant   JOURNAL OF MEDICINAL CHEMISTRY

An evaluation of substituent effects on aromatic edge-to-face interactions and CF–π versus CH–π interactions using an imino torsion balance model

(2013) W. Brian Jennings et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

PHASE 1, DOSE-RANGING STUDY OF EMIXUSTAT HYDROCHLORIDE (ACU-4429), A NOVEL VISUAL CYCLE MODULATOR, IN HEALTHY VOLUNTEERS

(2013) Ryo Kubota et al.   RETINA-THE JOURNAL OF RETINAL AND VITREOUS DISEASES

Long-Range Corrected Hybrid Density Functionals with Improved Dispersion Corrections

(2012) You-Sheng Lin et al.   Journal of Chemical Theory and Computation

Structure of RPE65 isomerase in a lipidic matrix reveals roles for phospholipids and iron in catalysis

(2012) P. D. Kiser et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

REFMAC5 for the refinement of macromolecular crystal structures

(2011) Garib N. Murshudov et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Reaction of Vascular Adhesion Protein-1 (VAP-1) with Primary Amines

(2011) Dominic P. H. M. Heuts et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Sponge Transgenic Mouse Model Reveals Important Roles for the MicroRNA-183 (miR-183)/96/182 Cluster in Postmitotic Photoreceptors of the Retina

(2011) Qubo Zhu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Effect of the damping function in dispersion corrected density functional theory

(2011) Stefan Grimme et al.   JOURNAL OF COMPUTATIONAL CHEMISTRY

Primary amines protect against retinal degeneration in mouse models of retinopathies

(2011) Akiko Maeda et al.   Nature Chemical Biology

The bisretinoids of retinal pigment epithelium

(2011) Janet R. Sparrow et al.   PROGRESS IN RETINAL AND EYE RESEARCH

SAFETY AND EFFECT ON ROD FUNCTION OF ACU-4429, A NOVEL SMALL-MOLECULE VISUAL CYCLE MODULATOR

(2011) Ryo Kubota et al.   RETINA-THE JOURNAL OF RETINAL AND VITREOUS DISEASES

A New Generation of Crystallographic Validation Tools for the Protein Data Bank

(2011) Randy J. Read et al.   STRUCTURE

Integration, scaling, space-group assignment and post-refinement

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Importance of Membrane Structural Integrity for RPE65 Retinoid Isomerization Activity

(2010) Marcin Golczak et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Revealing Noncovalent Interactions

(2010) Erin R. Johnson et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

The first example of a crystallization-induced asymmetric transformation (CIAT) in the Mannich reaction

(2010) Pavol Jakubec et al.   TETRAHEDRON-ASYMMETRY

RPE65, Visual Cycle Retinol Isomerase, Is Not Inherently 11-cis-specific

(2009) T. Michael Redmond et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Cl-π interactions in protein-ligand complexes

(2008) Yumi N. Imai et al.   PROTEIN SCIENCE