Membrane proteins, such as G protein-coupled
receptors (GPCRs) and ion channels play diverse physiological functions by
converting extracellular stimuli into intracellular signals. Hence, membrane
proteins are the major category of drugs targets. In this review, the author summarizes
recent findings on the physiological functions of GPCR, which senses medium-
and long-chain free fatty acids, in the regulation of systemic energy
metabolism and the physiological role of ion channels, which involved in the
regulation of intracellular calcium, in bone formation. The author further
describes the importance of these membrane proteins in future clinical
applications.
Modeling and
simulation have major advantages in dosing regimen selection. Severe infections
caused by antimicrobial-resistant strains have higher morbidity and fatality
rates than other drug-susceptible infections. The author has attempted to
identify the variability in efficacy and side effects using a population
pharmacokinetics and pharmacodynamics analysis with
anti-anti-methicillin-resistant Staphylococcus
aureus (MRSA) agents. In this review presents the details of our recent
research on the optimal dosing design of antimicrobial agents for the treatment
of MRSA infection based on hospital pharmacometrics.
Peroxisome proliferator-activated
receptor-α (PPARα), PPARɤ, and PPARσ/β are nuclear receptor-type transcription factors
that regulate expression of multiple genes involved in metabolism. They are
activated by endogenous lipids as well as synthetic ligands that include
fibrate (PPARα agonists)- and glitazone (PPARɤ agonists)-class drugs. The Current Topics include
single review and three original articles that argue about the PPAR–ligand
physical interactions revealed by X-ray crystallography. These studies may
contribute to the development of novel PPAR specific,
dual, or pan agonists for therapeutics against various metabolic diseases.
The efficacy of
infliximab in treating rheumatoid arthritis depends on its serum trough
concentration.
However, serum infliximab
concentration-detecting reagent performance as a biosimilar remains unclear. This
study aimed to investigate whether the serum infliximab concentration-detecting
reagent qualitative assay yields comparable results for biosimilar infliximab
and the originator product. Prepared samples were quantitatively assessed using
an enzyme-linked immunosorbent assay and qualitatively using serum infliximab
concentration-detecting reagent, and the results obtained for the originator
and biosimilar product were compared. Serum infliximab concentration-detecting
reagent yields comparable results for biosimilar infliximab and the originator
product on being used as a qualitative assay for trough serum levels.
Matoba & Noda have determined the
crystal structure of plant ATG12-ATG3, a complex that mediates Atg8 lipidation during
autophagy, and elucidated their interaction manner. By comparison with human
ATG12-ATG3 complex, the authors have identified the consensus sequence for
ATG12-binding and defined it as Atg12-interacting motif (AIM12), the first
identified binding motif for Atg12-family proteins.