Kinetics of phloretin binding to phosphatidylcholine vesicle membranes. [PDF]
The submillisecond kinetics for phloretin binding to unilamellar phosphatidylcholine (PC) vesicles was investigated using the temperature-jump technique.
Solomon, AK, Verkman, AS
core
Amphiphilic blockers punch through a mutant CLC-0 pore. [PDF]
Intracellularly applied amphiphilic molecules, such as p-chlorophenoxy acetate (CPA) and octanoate, block various pore-open mutants of CLC-0. The voltage-dependent block of a particular pore-open mutant, E166G, was found to be multiphasic. In symmetrical
Chen, Tsung-Yu, Zhang, Xiao-Dong
core +2 more sources
A Sequence-Specific Threading Tetraintercalator with an Extremely Slow Dissociation Rate Constant
A long-lived and sequence specific ligand-DNA complex would make possible the modulation of biological processes for extended periods. We have been investigating the threading polyintercalation approach to DNA recognition in which chains of aromatic ...
G. Holman +4 more
semanticscholar +1 more source
The role and implications of mammalian cellular circadian entrainment
At their most fundamental level, mammalian circadian rhythms occur inside every individual cell. To tell the correct time, cells must align (or ‘entrain’) their circadian rhythm to the external environment. In this review, we highlight how cells entrain to the major circadian cues of light, feeding and temperature, and the implications this has for our
Priya Crosby
wiley +1 more source
Computer programs for calculating pKa: a comparative study for 3-(3-(2-nitrophenyl)prop-2-enoyl)-2H-1-benzopyran-2-one [PDF]
Coumarin-based compounds containing a chalcone moiety exhibit antimicrobial activity. These substances are potential drugs and it is important to determine their pKa values. However, they are almost insoluble in water.
SELMA ŠPIRTOVIĆ-HALILOVIĆ +1 more
doaj
Peptide‐based ligand antagonists block a Vibrio cholerae adhesin
The structure of a peptide‐binding domain of the Vibrio cholerae adhesin FrhA was solved by X‐ray crystallography, revealing how the inhibitory peptide AGYTD binds tightly at its Ca2+‐coordinated pocket. Structure‐guided design incorporating D‐amino acids enhanced binding affinity, providing a foundation for developing anti‐adhesion therapeutics ...
Mingyu Wang +9 more
wiley +1 more source
A ligand when bound to a macromolecule (protein, DNA, RNA) will influence the biochemical function of that macromolecule. This observation is empirical and attributable to the association of the ligand with the amino acids/nucleotides that comprise the ...
Siddhartha Kundu
doaj +1 more source
A mechanistic modelling approach for the determination of the mechanisms of inhibition by cyclosporine on the uptake and metabolism of atorvastatin in rat hepatocytes using a high throughput uptake method [PDF]
Determine the inhibition mechanism through which cyclosporine inhibits the uptake and metabolism of atorvastatin in fresh rat hepatocytes using mechanistic models applied to data generated using a high throughput oil spin method.
Carter, Simon J. +5 more
core +2 more sources
Disordered but rhythmic—the role of intrinsic protein disorder in eukaryotic circadian timing
Unstructured domains known as intrinsically disordered regions (IDRs) are present in nearly every part of the eukaryotic core circadian oscillator. IDRs enable many diverse inter‐ and intramolecular interactions that support clock function. IDR conformations are highly tunable by post‐translational modifications and environmental conditions, which ...
Emery T. Usher, Jacqueline F. Pelham
wiley +1 more source
How to measure and evaluate binding affinities
Quantitative measurements of biomolecule associations are central to biological understanding and are needed to build and test predictive and mechanistic models.
Inga Jarmoskaite +3 more
doaj +1 more source

