A method for the simultaneous evaluation of the activities of seven major human drug-metabolizing cytochrome P450s using an in vitro cocktail of probe substrates …

EA Dierks, KR Stams, HK Lim, G Cornelius… - Drug Metabolism and …, 2001 - ASPET
Dierks, Karen R. Stams, Heng-Keang Lim, Georgia Cornelius, Honglu Zhang and Simon E.
… Send reprint requests to: Elizabeth Dierks, Wyeth-Ayerst Research, CN 8000, Princeton, NJ …

Discovery of milvexian, a high-affinity, orally bioavailable inhibitor of factor XIa in clinical studies for antithrombotic therapy

…, MA Galella, T Ziemba, EA Dierks… - Journal of medicinal …, 2021 - ACS Publications
Factor XIa (FXIa) is an enzyme in the coagulation cascade thought to amplify thrombin
generation but has a limited role in hemostasis. From preclinical models and human genetics, an …

Nitric oxide (NO•), the only nitrogen monoxide redox form capable of activating soluble guanylyl cyclase

EA Dierks, JN Burstyn - Biochemical pharmacology, 1996 - Elsevier
In the present study, we determined that of the redox forms of nitrogen monoxide, NO − , NO
• and NO + , only NO . significantly activates soluble guanylyl cyclase (GTP pyrophosphate-…

MGAT2 inhibitor decreases liver fibrosis and inflammation in murine NASH models and reduces body weight in human adults with obesity

…, P Devasthale, RM Lawrence, SA Stryker, EA Dierks… - Cell Metabolism, 2022 - cell.com
Monoacylglycerol acyltransferase 2 (MGAT2) is an important enzyme highly expressed in
the human small intestine and liver for the regulation of triglyceride absorption and …

Studies of the heme coordination and ligand binding properties of soluble guanylyl cyclase (sGC): characterization of Fe (II) sGC and Fe (II) sGC (CO) by electronic …

JN Burstyn, AE Yu, EA Dierks, BK Hawkins… - Biochemistry, 1995 - ACS Publications
Revised Manuscript Received January 23, 1995s abstract: The mechanism of activation of
soluble guanylyl cyclase by NO is poorly understood although it is clear that NO interacts with …

Selective FPR2 agonism promotes a proresolution macrophage phenotype and improves cardiac structure-function post myocardial infarction

…, J Chen, X Ma, DJ Search, EA Dierks… - Basic to Translational …, 2021 - jacc.org
Dysregulated inflammation following myocardial infarction (MI) leads to maladaptive healing
and remodeling. The study characterized and evaluated a selective formyl peptide receptor …

Demonstration of the role of scission of the proximal histidine− iron bond in the activation of soluble guanylyl cyclase through metalloporphyrin substitution studies

EA Dierks, S Hu, KM Vogel, AE Yu… - Journal of the …, 1997 - ACS Publications
Activation of soluble guanylyl cyclase (sGC) by NO correlates with scission of the proximal
iron−histidine bond, as demonstrated by the application of electronic absorption and …

Optimization of a dihydropyrrolopyrazole series of transforming growth factor-β type I receptor kinase domain inhibitors: Discovery of an orally bioavailable …

…, SR Mundla, CHR King, EA Dierks… - Journal of medicinal …, 2008 - ACS Publications
In our continuing effort to expand the SAR of the quinoline domain of dihydropyrrolopyrazole
series, we have discovered compound 15d, which demonstrated the antitumor efficacy with …

1-Aminobenzotriazole, a known cytochrome P450 inhibitor, is a substrate and inhibitor of N-acetyltransferase

Q Sun, TW Harper, EA Dierks, L Zhang, S Chang… - Drug metabolism and …, 2011 - ASPET
1-Aminobenzotriazole (ABT) has been used widely as a nonselective in vitro and in vivo
inhibitor of cytochrome P450 enzymes. To date, however, it has not been evaluated as an …

Optimization of physicochemical properties of pyrrolidine GPR40 AgoPAMs results in a differentiated profile with improved pharmacokinetics and reduced off-target …

…, TM Antrilli, MB Hicks, Q Sun, EA Dierks… - Bioorganic & Medicinal …, 2023 - Elsevier
GPR40 AgoPAMs are highly effective antidiabetic agents that have a dual mechanism of
action, stimulating both glucose-dependent insulin and GLP-1 secretion. The early lipophilic, …