Reversible Covalent Inhibition─ Desired Covalent Adduct Formation by Mass Action
Covalent inhibition has seen a resurgence in the last several years. Although long-plagued
by concerns of off-target effects due to nonspecific reactions leading to covalent adducts …
by concerns of off-target effects due to nonspecific reactions leading to covalent adducts …
Ligand-free signaling of G-protein-coupled receptors: physiology, pharmacology, and genetics
W Sadee - Molecules, 2023 - mdpi.com
G-protein-coupled receptors (GPCRs) are ubiquitous sensors and regulators of cellular
functions. Each GPCR exists in complex aggregates with multiple resting and active …
functions. Each GPCR exists in complex aggregates with multiple resting and active …
Pharmacodynamic models of indirect effects and irreversible inactivation with turnover: applicability to mechanism-based modeling of gene silencing and targeted …
AF Wang, VS Ayyar - Journal of Pharmaceutical Sciences, 2024 - Elsevier
Indirect response (IDR) and turnover with inactivation (TI) comprise two arrays of mechanism-
based pharmacodynamic (PD) models widely used to describe delayed drug effects. IDR …
based pharmacodynamic (PD) models widely used to describe delayed drug effects. IDR …
Pharmacological characterization of the zebrafish (Danio rerio) histamine H1 receptor reveals the involvement of the second extracellular loop in the binding of …
DA McNaught-Flores, AJ Kooistra, YC Chen… - Molecular …, 2024 - ASPET
The zebrafish (Danio rerio) histamine H1 receptor gene (zfH1R) was cloned in 2007 and
reported to be involved in fish locomotion. Yet, no detailed characterization of its …
reported to be involved in fish locomotion. Yet, no detailed characterization of its …
Bispecific FpFs: a versatile tool for preclinical antibody development
M Collins, N Ibeanu, WR Grabowska, S Awwad… - RSC Chemical …, 2024 - pubs.rsc.org
We previously described FpFs (Fab–PEG–Fab) as binding mimetics of IgGs. FpFs are
prepared with di (bis-sulfone) conjugation reagents that undergo disulfide rebridging …
prepared with di (bis-sulfone) conjugation reagents that undergo disulfide rebridging …
Contributions of William Jusko to Development of Pharmacokinetic and Pharmacodynamic Models and Methods
DE Mager, RM Straubinger - Journal of Pharmaceutical Sciences, 2024 - Elsevier
William J. Jusko, PhD,(Fig. 1) graduated from the University of Buffalo (UB) in 1965 with a
BS degree in Pharmacy, and went on at UB to obtain a PhD degree working with Gerhard …
BS degree in Pharmacy, and went on at UB to obtain a PhD degree working with Gerhard …