Michelle R. Garnsey
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View article: Design and application of synthetic 17B-HSD13 substrates reveals preserved catalytic activity of protective human variants
Design and application of synthetic 17B-HSD13 substrates reveals preserved catalytic activity of protective human variants Open
View article: Discovery of SARS-CoV-2 papain-like protease (PL <sup>pro</sup> ) inhibitors with efficacy in a murine infection model
Discovery of SARS-CoV-2 papain-like protease (PL <sup>pro</sup> ) inhibitors with efficacy in a murine infection model Open
Vaccines and first-generation antiviral therapeutics have provided important protection against COVID-19 caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). However, there remains a need for additional therapeutic optio…
View article: Discovery of SARS-CoV-2 papain-like protease (PL<sup>pro</sup>) inhibitors with efficacy in a murine infection model
Discovery of SARS-CoV-2 papain-like protease (PL<sup>pro</sup>) inhibitors with efficacy in a murine infection model Open
Vaccines and first-generation antiviral therapeutics have provided important protection against coronavirus disease 2019 (COVID-19) caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). However, there remains a need for a…
View article: Design of Next-Generation DGAT2 Inhibitor PF-07202954 with Longer Predicted Half-Life
Design of Next-Generation DGAT2 Inhibitor PF-07202954 with Longer Predicted Half-Life Open
Diacylglycerol O-acyltransferase 2 (DGAT2) inhibitors have been shown to lower liver triglyceride content and are being explored clinically as a treatment for non-alcoholic steatohepatitis (NASH). This work details efforts to find an exten…
View article: Structural basis of lipid-droplet localization of 17-beta-hydroxysteroid dehydrogenase 13
Structural basis of lipid-droplet localization of 17-beta-hydroxysteroid dehydrogenase 13 Open
Hydroxysteroid 17-beta-dehydrogenase 13 (HSD17B13) is a hepatic lipid droplet-associated enzyme that is upregulated in patients with non-alcoholic fatty liver disease. Recently, there have been several reports that predicted loss of functi…
View article: Crystal structures of 17-beta-hydroxysteroid dehydrogenase 13
Crystal structures of 17-beta-hydroxysteroid dehydrogenase 13 Open
Hydroxysteroid 17-beta-dehydrogenase 13 (HSD17B13) is a hepatic lipid droplet-associated enzyme that is upregulated in patients with non-alcoholic fatty liver disease. Recently, there have been several reports that predicted loss of functi…
View article: CCDC 2237356: Experimental Crystal Structure Determination
CCDC 2237356: 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: Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss
Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss Open
The melanocortin-4 receptor (MC4R) is a centrally expressed, class A GPCR that plays a key role in the regulation of appetite and food intake. Deficiencies in MC4R signaling result in hyperphagia and increased body mass in humans. Antagoni…
View article: Corrigendum: Kinetic Analysis of Catalytic Organic Reactions Using a Temperature Scanning Protocol
Corrigendum: Kinetic Analysis of Catalytic Organic Reactions Using a Temperature Scanning Protocol Open
View article: Kinetic Analysis of Catalytic Organic Reactions Using a Temperature Scanning Protocol
Kinetic Analysis of Catalytic Organic Reactions Using a Temperature Scanning Protocol Open
Experimental and kinetic modelling studies are presented to describe the development of temperature scanning reaction progress protocol for batch reactions. Coupled with graphical manipulations, this approach enables the expansion of in‐si…
View article: Deaminative Reductive Cross-Electrophile Couplings of Alkylpyridinium Salts and Aryl Bromides
Deaminative Reductive Cross-Electrophile Couplings of Alkylpyridinium Salts and Aryl Bromides Open
A nickel-catalyzed reductive cross-coupling of alkylpyridinium salts and aryl bromides has been developed using Mn as the reductant. Both primary and secondary alkylpyridinium salts can be used, and high functional group and heterocycle to…
View article: Transforming Benzylic Amines into Diarylmethanes: Cross-Couplings of Benzylic Pyridinium Salts via C–N Bond Activation
Transforming Benzylic Amines into Diarylmethanes: Cross-Couplings of Benzylic Pyridinium Salts via C–N Bond Activation Open
A nickel-catalyzed cross-coupling of benzylic pyridinium salts with arylboronic acids was developed. Coupled with chemoselective pyridinium formation, this method allows benzyl primary amines to be efficiently converted to di(hetero)arylme…
View article: CCDC 1575706: Experimental Crystal Structure Determination
CCDC 1575706: 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 1575705: Experimental Crystal Structure Determination
CCDC 1575705: 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 1575704: Experimental Crystal Structure Determination
CCDC 1575704: 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: Design and Synthesis of γ- and δ-Lactam M<sub>1</sub> Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M<sub>1</sub>-Selective PAM with Weak Agonist Activity
Design and Synthesis of γ- and δ-Lactam M<sub>1</sub> Positive Allosteric Modulators (PAMs): Convulsion and Cholinergic Toxicity of an M<sub>1</sub>-Selective PAM with Weak Agonist Activity Open
Recent data demonstrated that activation of the muscarinic M1 receptor by a subtype-selective positive allosteric modulator (PAM) contributes to the gastrointestinal (GI) and cardiovascular (CV) cholinergic adverse events (AEs) …
View article: Discovery of the Potent and Selective M1 PAM-Agonist<i>N</i>-[(3<i>R</i>,4<i>S</i>)-3-Hydroxytetrahydro-2<i>H</i>-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects
Discovery of the Potent and Selective M1 PAM-Agonist<i>N</i>-[(3<i>R</i>,4<i>S</i>)-3-Hydroxytetrahydro-2<i>H</i>-pyran-4-yl]-5-methyl-4-[4-(1,3-thiazol-4-yl)benzyl]pyridine-2-carboxamide (PF-06767832): Evaluation of Efficacy and Cholinergic Side Effects Open
It is hypothesized that selective muscarinic M1 subtype activation could be a strategy to provide cognitive benefits to schizophrenia and Alzheimer's disease patients while minimizing the cholinergic side effects observed with nonselective…
View article: Design and optimization of selective azaindole amide M1 positive allosteric modulators
Design and optimization of selective azaindole amide M1 positive allosteric modulators Open