Results 101 to 110 of about 7,051 (200)
This review describes how an integrated structural biology platform at Merck Sharp & Dohme LLC, Rahway, New Jersey, USA, combining X‐ray crystallography, cryo‐EM, MicroED and cryo‐ET, enables seamless three‐dimensional insights from molecular to cellular length scales.
Jill E. Chrencik +44 more
wiley +1 more source
Genetic encoding of noncanonical amino acids (ncAA) enables their site‐specific installation in proteins. This work compares the nuclear magnetic resonance (NMR) performance of different ncAAs in a large protein−DNA complex (~ 100 kDa) without isotope labelling. The ncAAs deliver readily detectable NMR signals in the complex between E.
Sreelakshmi Mekkattu Tharayil +7 more
wiley +1 more source
Temozolomide Cocrystals with Carboxamide Coformers
Temozolomide (TMZ) is an antitumor prodrug of broad spectrum antineoplastic activity. TMZ is stable in acidic medium (pH < 4) but starts to decompose at alkaline pH (>7).
Ashwini Nangia (1400761) +2 more
core +3 more sources
Engineering Cocrystals of Poorly Water-Soluble Drugs to Enhance Dissolution in Aqueous Medium
Biopharmaceutics Classification System (BCS) Class II and IV drugs suffer from poor aqueous solubility and hence low bioavailability. Most of these drugs are hydrophobic and cannot be developed into a pharmaceutical formulation due to their poor aqueous ...
Indumathi Sathisaran +1 more
doaj +1 more source
We developed fluorescent molecular rotors (FMRs) that respond sensitively to intracellular viscosity. Based on the dye scaffold of GFP, we systematically investigated molecular rigidity and surface area, and discovered FMRs with remarkably high viscosity sensitivity.
Takashi Kanamori +7 more
wiley +1 more source
Application of Twin Screw Extrusion in the Manufacture of Cocrystals, Part I: Four Case Studies
The application of twin screw extrusion (TSE) as a scalable and green process for the manufacture of cocrystals was investigated. Four model cocrystal forming systems, Caffeine-Oxalic acid, Nicotinamide-trans cinnamic acid, Carbamazepine-Saccharin, and ...
Karthik Nagapudi +4 more
doaj +1 more source
We developed a targeted covalent inhibitor for the p300/CBP‐associated factor (PCAF) bromodomain. Our lead molecule, 10, labeled a unique lysine residue in the PCAF bromodomain, demonstrated potent inhibition in biophysical/biochemical assays, and engaged the PCAF bromodomain in cells.
Richard R. Ede +9 more
wiley +1 more source
Cocrystals: Solution, Mechanochemistry, and Sublimation
A systematic study of the effect of crystallization method on the resulting solid-state form of a series of organic cocrystals has been carried out.
Thalia Carstens (8274975) +2 more
core +1 more source
Daidzein cocrystals: An opportunity to improve its biopharmaceutical parameters
The present study involves the contribution of cocrystallization towards the modification of the biopharmaceutical parameters of poorly watersoluble plant-originated isoflavone, daidzein (DAID). The cocrystals were prepared with GRAS status coformers i.e.
Yashika Bhalla +3 more
doaj +1 more source
Apremilast Cocrystals with Phenolic Coformers
Apremilast (APR) is an anti-inflammatory drug commonly used in the treatment of psoriasis. In efforts to enhance its solubility, several cocrystals with similar structural features have been developed. This study investigates the cocrystallization of APR with four phenolic-type coformers: phenol, catechol, pyrogallol, and hydroxyquinol. These coformers
Yelizaveta Naumkina +3 more
openaire +3 more sources

