Monitoring drug-serum protein interactions for early ADME prediction through Surface Plasmon Resonance technology

Fabini, EdoardoUniv Bologna, Dept Pharm & Biotechnol, Via Belmeloro 6, I-40126 Bologna, Italy. (författare)

Many molecules fail to reach the market due to poor pharmacokinetic (PK) properties, rendering the potential drug virtually unavailable for the primary target despite efficient administration to the body. PK properties of endogenous and exogenous compounds in mammals are dependent, among other factors, on their ability to interact with serum proteins. The extent of binding can greatly influence their ADME (adsorption, distribution, metabolism and execration) profile. Reliable and cost-effective bioavailability studies, early in the drug discovery process, can lead to an improvement of the success rate for compounds entering clinical trials. Optical biosensors based on surface plasmon resonance (SPR) detection emerged as an efficient approach to obtain large amounts of information about the binding of small molecules to serum proteins. Simple, automated and fast assays provide a good throughput, versatility and highly informative data output, rendering the methodology particularly suited for early screening. The ability to provide basic information on PK can be easily coupled to structure-activity relationship analysis. In this review, features of the technology and its employment for the study of serum protein-small molecule interactions are presented and discussed.

NATURVETENSKAP Biologi Biokemi och molekylärbiologi hsv//swe
NATURAL SCIENCES Biological Sciences Biochemistry and Molecular Biology hsv//eng
Optical biosensor
Surface plasmon resonance spectroscopy
Early ADME profiling
Drug-serum proteins interaction
Human serum albumin
Alpha-1-acid glycoprotein

Danielson, U. Helena,1959-Uppsala universitet,Institutionen för kemi - BMC,Science for Life Laboratory, SciLifeLab(Swepub:uu)helenads (författare)
Univ Bologna, Dept Pharm & Biotechnol, Via Belmeloro 6, I-40126 Bologna, Italy.Institutionen för kemi - BMC (creator_code:org_t)

Ingår i:Journal of Pharmaceutical and Biomedical Analysis: Elsevier BV144, s. 188-1940731-70851873-264X

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