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- W2794011199 abstract "It is well known that small molecule colloidal aggregation is a leading cause of false positives in early drug discovery. Colloid-formers are diverse and well represented among corporate and academic screening decks, and even among approved drugs. Less appreciated is how colloid formation by drug-like compounds fits into the wider understanding of colloid physical chemistry. Here we introduce the impact that colloidal aggregation has had on early drug discovery, and then turn to the physical and thermodynamic driving forces for small molecule colloidal aggregation, including the particulate nature of the colloids, their critical aggregation concentration-governed formation, their mechanism of protein adsorption and subsequent inhibition, and their sensitivity to detergent. We describe methods that have been used extensively to both identify aggregate-formers and to study and control their physical chemistry. While colloidal aggregation is widely recognized as a problem in early drug discovery, we highlight the opportunities for exploiting this phenomenon in biological milieus and for drug formulation." @default.
- W2794011199 created "2018-03-29" @default.
- W2794011199 creator A5007222348 @default.
- W2794011199 creator A5009419179 @default.
- W2794011199 creator A5014223813 @default.
- W2794011199 creator A5045900479 @default.
- W2794011199 date "2018-04-01" @default.
- W2794011199 modified "2023-10-17" @default.
- W2794011199 title "Colloidal aggregation: From screening nuisance to formulation nuance" @default.
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- W2794011199 doi "https://doi.org/10.1016/j.nantod.2018.02.011" @default.