Fragment screening for drug leads by weak affinity chromatography (WAC-MS)

Ohlson, Sten; Duong-Thi, Minh-Dao

doi:10.1016/j.ymeth.2018.01.011

Cited by 22 publications

(11 citation statements)

References 34 publications

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“…However, the common first step for all these approaches is the purification of the target protein, which remains challenging in many cases. On average, only 50-70% soluble protein and 30% membrane proteins from prokaryotes can be expressed in a recombinant form, and among those successfully expressed, only 30-50% can be purified in a homogeneous state (Christendat et al 2000;Norin and Sundström 2002;Dobrovetsky et al 2005). Eukaryotic proteins-including many biomedically interesting targets from humans-seem even more challenging (Banci et al 2006).…”

Section: The Use Of Dsf In Buffer Screening and Optimization Of Protementioning

confidence: 99%

Theory and applications of differential scanning fluorimetry in early-stage drug discovery

2020

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Differential scanning fluorimetry (DSF) is an accessible, rapid, and economical biophysical technique that has seen many applications over the years, ranging from protein folding state detection to the identification of ligands that bind to the target protein. In this review, we discuss the theory, applications, and limitations of DSF, including the latest applications of DSF by ourselves and other researchers. We show that DSF is a powerful high-throughput tool in early drug discovery efforts. We place DSF in the context of other biophysical methods frequently used in drug discovery and highlight their benefits and downsides. We illustrate the uses of DSF in protein buffer optimization for stability, refolding, and crystallization purposes and provide several examples of each. We also show the use of DSF in a more downstream application, where it is used as an in vivo validation tool of ligand-target interaction in cell assays. Although DSF is a potent tool in buffer optimization and large chemical library screens when it comes to ligand-binding validation and optimization, orthogonal techniques are recommended as DSF is prone to false positives and negatives.

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Section: The Use Of Dsf In Buffer Screening and Optimization Of Protementioning

confidence: 99%

Theory and applications of differential scanning fluorimetry in early-stage drug discovery

2020

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“…The corresponding breakthrough time of PGG tended toward that of the neutravidin blank column dead time (0.92 min), thus revealing negligible non-specific interaction during the binding process. 24…”

Section: Resultsmentioning

confidence: 99%

Immobilization of the SARS-CoV-2-receptor binding domain onto methacrylate-based monoliths for nano LC at 30 nL min⁻¹ and application for research of its ligands

Guillaume

André

2022

Anal. Methods

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“…It is also used in genetic engineering, biological compound purification, and vaccine production. For this method, separation is accomplished based on a reversible interaction between analytes and specific ligands such as antibodies and antigens, enzymes and substrates, or enzyme and inhibitor interactions [53,54]. Cao and Liu [55] employed high performance affinity chromatography (HPAC) to determine the binding relations between the structures of plasma proteins and human serum albumin (HAS).…”

Section: Affinity Chromatography (Ac)mentioning

confidence: 99%

Determination of Drugs in Clinical Trials: Current Status and Outlook

Tavana

Chen

2022

Sensors

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All pharmaceutical drugs, vaccines, cosmetic products, and many medical breakthroughs must first be approved through clinical research and trials before advancing to standard practice or entering the marketplace. Clinical trials are sets of tests that are required to determine the safety and efficacy of pharmaceutical compounds, drugs, and treatments. There is one pre-phase and four main clinical phase requirements that every drug must pass to obtain final approval. Analytical techniques play a unique role in clinical trials for measuring the concentrations of pharmaceutical compounds in biological matrices and monitoring the conditions of patients (or volunteers) during various clinical phases. This review focuses on recent analytical methods that are employed to determine the concentrations of drugs and medications in biological matrices, including whole blood, plasma, urine, and breast milk. Four primary analytical techniques (extraction, spectroscopy, chromatography, and electrochemical) are discussed, and their advantages and limitations are assessed. Subsequent to a survey of evidence and results, it is clear that microelectromechanical system (MEMS) based electrochemical sensor and biosensor technologies exhibit several notable advantages over other analytical methods, and their future prospects are discussed.

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Fragment screening for drug leads by weak affinity chromatography (WAC-MS)

Cited by 22 publications

References 34 publications

Theory and applications of differential scanning fluorimetry in early-stage drug discovery

Theory and applications of differential scanning fluorimetry in early-stage drug discovery

Immobilization of the SARS-CoV-2-receptor binding domain onto methacrylate-based monoliths for nano LC at 30 nL min⁻¹ and application for research of its ligands

Determination of Drugs in Clinical Trials: Current Status and Outlook

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Fragment screening for drug leads by weak affinity chromatography (WAC-MS)

Cited by 22 publications

References 34 publications

Theory and applications of differential scanning fluorimetry in early-stage drug discovery

Theory and applications of differential scanning fluorimetry in early-stage drug discovery

Immobilization of the SARS-CoV-2-receptor binding domain onto methacrylate-based monoliths for nano LC at 30 nL min−1 and application for research of its ligands

Determination of Drugs in Clinical Trials: Current Status and Outlook

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Product

Resources

About

Immobilization of the SARS-CoV-2-receptor binding domain onto methacrylate-based monoliths for nano LC at 30 nL min⁻¹ and application for research of its ligands