André Alker
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View article: RG7774 (Vicasinabin), an orally bioavailable cannabinoid receptor 2 (CB2R) agonist, decreases retinal vascular permeability, leukocyte adhesion, and ocular inflammation in animal models
RG7774 (Vicasinabin), an orally bioavailable cannabinoid receptor 2 (CB2R) agonist, decreases retinal vascular permeability, leukocyte adhesion, and ocular inflammation in animal models Open
Introduction Preclinical studies suggest that cannabinoid receptor type 2 (CB2R) activation has a therapeutic effect in animal models on chronic inflammation and vascular permeability, which are key pathological features of diabetic retino…
View article: CCDC 2067483: Experimental Crystal Structure Determination
CCDC 2067483: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2067484: Experimental Crystal Structure Determination
CCDC 2067484: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2067485: Experimental Crystal Structure Determination
CCDC 2067485: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Is Smaller Better? Cu<sup>2+</sup>/Cu<sup>+</sup> Coordination Chemistry and Copper-64 Radiochemical Investigation of a 1,4,7-Triazacyclononane-Based Sulfur-Rich Chelator
Is Smaller Better? Cu<sup>2+</sup>/Cu<sup>+</sup> Coordination Chemistry and Copper-64 Radiochemical Investigation of a 1,4,7-Triazacyclononane-Based Sulfur-Rich Chelator Open
The biologically triggered reduction of Cu2+ to Cu+ has been postulated as a possible in vivo decomplexation pathway in 64/67Cu-based radiopharmaceuticals. In an attempt to hinder this phenomenon, we have previously developed a family of S…
View article: CCDC 1981521: Experimental Crystal Structure Determination
CCDC 1981521: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 671179: Experimental Crystal Structure Determination
CCDC 671179: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2124897: Experimental Crystal Structure Determination
CCDC 2124897: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 2124898: Experimental Crystal Structure Determination
CCDC 2124898: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: <i>CELLOPT</i>: improved unit-cell parameters for electron diffraction data of small-molecule crystals
<i>CELLOPT</i>: improved unit-cell parameters for electron diffraction data of small-molecule crystals Open
Electron diffraction enables structure determination of organic small molecules using crystals that are too small for conventional X-ray crystallography. However, because of uncertainties in the experimental parameters, notably the detecto…
View article: Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe
Detection of cannabinoid receptor type 2 in native cells and zebrafish with a highly potent, cell-permeable fluorescent probe Open
Detection and visualization of the cannabinoid receptor type 2 by a cell-permeable high affinity fluorescent probe platform enables tracing receptor trafficking in live cells and in zebrafish.
View article: CCDC 2036253: Experimental Crystal Structure Determination
CCDC 2036253: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: Copper Coordination Chemistry of Sulfur Pendant Cyclen Derivatives: An Attempt to Hinder the Reductive-Induced Demetalation in <sup>64/67</sup>Cu Radiopharmaceuticals
Copper Coordination Chemistry of Sulfur Pendant Cyclen Derivatives: An Attempt to Hinder the Reductive-Induced Demetalation in <sup>64/67</sup>Cu Radiopharmaceuticals Open
The Cu2+ complexes formed by a series of cyclen derivatives bearing sulfur pendant arms, 1,4,7,10-tetrakis[2-(methylsulfanyl)ethyl]-1,4,7,10-tetraazacyclododecane (DO4S), 1,4,7-tris[2-(methylsulfanyl)ethyl]-1,4,7,10-tetraazacyclododecane (…
View article: Cytochrome P450-Mediated Metabolism and CYP Inhibition for the Synthetic Peroxide Antimalarial OZ439
Cytochrome P450-Mediated Metabolism and CYP Inhibition for the Synthetic Peroxide Antimalarial OZ439 Open
OZ439 is a potent synthetic ozonide evaluated for the treatment of uncomplicated malaria. The metabolite profile of OZ439 was characterized in vitro using human liver microsomes combined with LC/MS-MS, chemical derivatization, and metaboli…
View article: Iterative cell optimization in refinement of small molecule electron diffraction data.
Iterative cell optimization in refinement of small molecule electron diffraction data. Open
Electron diffraction data for the MOF Vie-1 and for Oseltamivir. Associated with the manuscript "Iterative cell optimization in refinement of small molecule electron diffraction data." in submission process.
View article: Iterative cell optimization in refinement of small molecule electron diffraction data.
Iterative cell optimization in refinement of small molecule electron diffraction data. Open
Electron diffraction data for the MOF Vie-1 and for Oseltamivir. Associated with the manuscript "Iterative cell optimization in refinement of small molecule electron diffraction data." in submission process.
View article: Discovery of RO7185876, a Highly Potent γ-Secretase Modulator (GSM) as a Potential Treatment for Alzheimer’s Disease
Discovery of RO7185876, a Highly Potent γ-Secretase Modulator (GSM) as a Potential Treatment for Alzheimer’s Disease Open
γ-Secretase (GS) is a key target for the potential treatment of Alzheimer's disease. While inhibiting GS led to serious side effects, its modulation holds a lot of potential to deliver a safe treatment. Herein, we report the discovery of a…
View article: CCDC 1836178: Experimental Crystal Structure Determination
CCDC 1836178: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: CCDC 1922459: Experimental Crystal Structure Determination
CCDC 1922459: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …
View article: A carbohydrate-derived trifunctional scaffold for medicinal chemistry library synthesis
A carbohydrate-derived trifunctional scaffold for medicinal chemistry library synthesis Open
For the generation of compound libraries for drug discovery a central scaffold containing three exit vectors with defined chirality was devised starting from commercially available tri-O-acetyl-glucal. Surprisingly, the reaction of a 4-O-m…
View article: Ligand channel in pharmacologically stabilized rhodopsin
Ligand channel in pharmacologically stabilized rhodopsin Open
Significance A substantial number of known genetic disorders have their origin in mutations that cause misfolding or dysfunction of G protein-coupled receptors (GPCRs). Pharmacological chaperones can rescue such mutant receptors from the e…
View article: CCDC 1819788: Experimental Crystal Structure Determination
CCDC 1819788: Experimental Crystal Structure Determination Open
An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available …