Search results for: Sten Ohlson

Items from 1 to 20 out of 31 results

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

Sten Ohlson, Minh-Dao Duong-Thi

Methods > 2018 > 146 > C > 26-38

Fragment-based drug discovery is an important tool for design of small molecule hit-to-lead compounds against various biological targets. Several approved drugs have been derived from an initial fragment screen and many such candidates are in various stages of clinical trials. Finding fragment hits, that are suitable for optimisation by medicinal chemists, is still a challenge as the binding between...

article

Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6)

Lianbin Yao, Pondy Murugappan Ramanujulu, Anders Poulsen, Sten Ohlson, more

Bioorganic & Medicinal Chemistry Letters > 2018 > 28 > 15 > 2636-2640

Inhibition of more than one pathway in a cancer cell with a single molecule could result in better therapies with less complex dosing regimens. In this work multi-component ligands have been prepared by joining together key pharmacophores of two different enzyme inhibitors in a way which increases potency against the individual pathways. Selective JAK1/2 inhibitor, ruxolitinib (3), and pan-HDAC inhibitor...

article

Direct analysis – no sample preparation – of bioavailable cortisol in human plasma by weak affinity chromatography (WAC)

Sten Ohlson, Jagjit Kaur, Manfred Raida, Ulf Niss, more

Journal of Chromatography B > 2017 > 1061-1062 > C > 438-444

Pre-analytical treatment of blood plasma is a time consuming and often rate limiting step in the workflow of LC/MS analysis. We present in this pilot study a new approach for quantitative LC/MS based on weak affinity chromatography (WAC) of crude plasma. The steroid hormone cortisol was selected as a clinically relevant biomarker, as it currently requires extensive pre-analytical preparation. A WAC...

article

Comparison of weak affinity chromatography and surface plasmon resonance in determining affinity of small molecules

Minh-Dao Duong-Thi, Gunnar Bergström, Carl-Fredrik Mandenius, Maria Bergström, more

Analytical Biochemistry > 2014 > 461 > Complete > 57-59

In this study, we compared affinity data from surface plasmon resonance (SPR) and weak affinity chromatography (WAC), two established techniques for determination of weak affinity (mM–μM) small molecule–protein interactions. In the current comparison, thrombin was used as target protein. In WAC the affinity constant (K _D ) was determined from retention times, and in SPR it was determined by...

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Synthesis, Biological Evaluation, WAC and NMR Studies of S‐Galactosides and Non‐Carbohydrate Ligands of Cholera Toxin Based on Polyhydroxyalkylfuroate Moieties

Javier Ramos‐Soriano, Ulf Niss, Jesús Angulo, Manuel Angulo, more

Chemistry – A European Journal > 19 > 52 > 17989 - 18003

The synthesis of several non‐carbohydrate ligands of cholera toxin based on polyhydroxyalkylfuroate moieties is reported. Some of them have been linked to D‐galactose through a stable and well‐tolerated S‐glycosidic bond. They represent a novel type of non‐hydrolyzable bidentate ligand featuring galactose and polyhydroxyalkylfuroic esters as pharmacophoric residues, thus mimicking the GM1 ganglioside...

article

Immobilized lipodisks as model membranes in high-throughput HPLC-MS analysis

Elinor Meiby, Malin Morin Zetterberg, Sten Ohlson, Víctor Agmo Hernández, more

Analytical and Bioanalytical Chemistry > 2013 > 405 > 14 > 4859-4869

Lipodisks, also referred to as polyethylene glycol (PEG)-stabilized bilayer disks, have previously been demonstrated to hold great potential as model membranes in drug partition studies. In this study, an HPLC-MS system with stably immobilized lipodisks is presented. Functionalized lipodisks were immobilized on two different HPLC support materials either covalently by reductive amination or by streptavidin–biotin...

article

Elucidating the selectivity of recombinant forms of Aleuria aurantia lectin using weak affinity chromatography

Maria Bergström, Eva Åström, Peter Påhlsson, Sten Ohlson

Journal of Chromatography B > 2012 > 885-886 > Complete > 66-72

Aberrant glycosylation is connected to several pathological conditions and lectins are useful tools to characterize glycosylated biomarkers. The Aleuria aurantia lectin (AAL) is of special interest since it interacts with all types of fucosylated saccharides. AAL has been expressed in Escherichia coli as a fully functional recombinant protein. Engineered variants of AAL have been developed with the...

article

Fragment screening of cyclin G-associated kinase by weak affinity chromatography

Elinor Meiby, Stefan Knapp, Jonathan M. Elkins, Sten Ohlson

Analytical and Bioanalytical Chemistry > 2012 > 404 > 8 > 2417-2425

Fragment-based drug discovery (FBDD) has become a new strategy for drug discovery where lead compounds are evolved from small molecules. These fragments form low affinity interactions (dissociation constant (K _D) = mM − μM) with protein targets, which require fragment screening methods of sufficient sensitivity. Weak affinity chromatography (WAC) is a promising new technology for fragment screening...

article

Weak affinity chromatography as a new approach for fragment screening in drug discovery

Minh-Dao Duong-Thi, Elinor Meiby, Maria Bergström, Tomas Fex, more

Analytical Biochemistry > 2011 > 414 > 1 > 138-146

Fragment-based drug design (FBDD) is currently being implemented in drug discovery, creating a demand for developing efficient techniques for fragment screening. Due to the intrinsic weak or transient binding of fragments (mM–μM in dissociation constant (K _D )) to targets, methods must be sensitive enough to accurately detect and quantify an interaction. This study presents weak affinity chromatography...

article

Toward high‐throughput drug screening on a chip‐based parallel affinity separation platform

Sten Ohlson, Minh‐Dao Duong‐Thi, Maria Bergström, Tomas Fex, more

Journal of Separation Science > 33 > 17‐18 > 2575 - 2581

High‐throughput screening of compound libraries, including the study of fragments, has become one of the cornerstones in modern drug discovery research. During this process hits are defined that may be developed into valuable leads and eventually into possible drug candidates. In this paper, we have demonstrated that parallel zonal weak affinity chromatography in microcolumns on a chip offers a possible...

article

Monitoring of influenza virus hemagglutinin in process samples using weak affinity ligands and surface plasmon resonance

Carl-Fredrik Mandenius, Ronghui Wang, Anna Aldén, Gunnar Bergström, more

Analytica Chimica Acta > 2008 > 623 > 1 > 66-75

Surface plasmon resonance (SPR) was used to screen the interaction between a variety of affinity ligands and hemagglutinin (HA) from human influenza virus, with the aim of identifying low affinity ligands useful for the development of a rapid bioanalytical sensor. Three sialic acid-based structures and four lectins were evaluated as sensor ligands. The sialic acid-based ligands included a natural...

article

Designing transient binding drugs: A new concept for drug discovery

Sten Ohlson

Drug Discovery Today > 2008 > 13 > 9-10 > 433-439

A multitude of weak, or transient, biological interactions (dissociation constant: K _d >μM), either working alone or in concert, occur frequently throughout biological systems. We are starting to appreciate their importance in complex biological networks. This realization has important implications to drug discovery as we can question the current paradigm of drug design to find the highest...

article

Towards a FRET-based immunosensor for continuous carbohydrate monitoring

Henrik A. Engström, Per Ola Andersson, Klaus Gregorius, Sten Ohlson

Journal of Immunological Methods > 2008 > 333 > 1-2 > 107-114

In this report we have evaluated the potential of using fluorescence/Förster resonance energy transfer (FRET) in a competitive immunosensor for continuous monitoring of the carbohydrate hapten maltose. The cyanine dyes Cy5 and Cy5.5 were used as a donor–acceptor pair by conjugation to maltose-labeled bovine serum albumin (BSA) and the monoclonal antibody IgG 39.5, giving Cy5–BSA–maltotriitol (3.1/1/18)...

article

Porcine platelet lysate as a supplement for animal cell culture

Anna Aldén, Lorena Gonzalez, Anna Persson, Kerstin Christensson, more

Cytotechnology > 2007 > 55 > 1 > 3-8

A novel supplementation of cell growth media based on a porcine platelet lysate was developed for culture of animal-derived cells. The platelet lysate was produced from porcine blood and contained lysate of platelets and plasma components. It showed satisfactory microbiological integrity and it carried only low amount of endotoxins (<10 EU/mL). The porcine platelet lysate supported well proliferation...

article

Screening for transient biological interactions as applied to albumin ligands: A new concept for drug discovery

Sten Ohlson, Siamak Shoravi, Tomas Fex, Roland Isaksson

Analytical Biochemistry > 2006 > 359 > 1 > 120-123

The notion that many biological interactions are based on transient binding (dissociation constants (K _d ) in the range of 10–0.01mM) is familiar, yet the implications for biological sciences have been realized only recently. An important area of biological sciences is drug design, where the traditional “lock and key” view of binding has prevailed and drug candidates are usually selected on...

article

A label-free continuous total-internal-reflection-fluorescence-based immunosensor

Henrik A. Engström, Per Ola Andersson, Sten Ohlson

Analytical Biochemistry > 2006 > 357 > 2 > 159-166

In this study, we continuously monitored, second-by-second, concentration changes of two different carbohydrates (maltose and panose) by using monoclonal antibodies in an optical immunosensor based on total internal reflection fluorescence. Earlier studies have demonstrated that these antibodies increase their intrinsic tryptophan fluorescence upon binding of carbohydrate antigens. Using the four...

article

Transiently binding antibody fragments against Lewis x and sialyl-Lewis x

Reine Johansson, Mats Ohlin, Bo Jansson, Sten Ohlson

Journal of Immunological Methods > 2006 > 312 > 1-2 > 20-26

Biomolecular recognition is often characterised by low affinity where many weak interactions work either alone or in concert, resulting in an inherent dynamic situation. For example the well-studied weak binding of cell–cell interactions is predominantly based on a range of carbohydrates that interact with numerous (protein) ligands. Finding appropriate binders to these carbohydrate structures may...

article

HPLC analysis of carbohydrate deficient transferrin isoforms isolated by the Axis-Shield %CDT method

Anna Aldén, Sten Ohlson, Peter Påhlsson, Ingvar Rydén

Clinica Chimica Acta > 2005 > 356 > 1-2 > 143-146

Carbohydrate-deficient transferrin (CDT) is elevated during prolonged overconsumption of alcohol and CDT is considered to be the most specific biochemical marker for alcohol overconsumption. However, an accurate method for analysing CDT is necessary because the test is frequently used for example in legal matters.Patient serum samples were analysed with the Axis-Shield %CDT and eluates were pooled...

article

Analysis of the specificity and thermodynamics of the interaction between low affinity antibodies and carbohydrate antigens using fluorescence spectroscopy

Henrik A. Engström, Per Ola Andersson, Sten Ohlson

Journal of Immunological Methods > 2005 > 297 > 1-2 > 203-211

The purpose of this work has been to examine whether fluorescence spectroscopy can be used to investigate weak or transient binding between monoclonal antibodies and carbohydrate antigens. In earlier studies we have demonstrated that the three monoclonal antibodies 39.4 (IgG2b), 39.5 (IgG2b) and 61.1(IgG3) bind weakly to the glycosidic α(1–4) bond present in e.g. maltose and panose. In this study...

article

Lectin affinity capillary electrophoresis in glycoform analysis applying the partial filling technique

Maria Bergström, Mikael Nilsson, Roland Isaksson, Ingvar Rydén, more

Journal of Chromatography B > 2004 > 809 > 2 > 323-329

The study of protein glycosylation and its significance in biological interactions is a field of growing interest. This work demonstrates a lectin-based separation of protein glycoforms of α ₁ -acid glycoprotein (AGP or orosomucoid) with capillary electrophoresis. Glycoform analysis was performed with a “partial filling technique” with the lectin Concanavalin A (Con A) as affinity ligand....

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Search results for: Sten Ohlson

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

Merging of ruxolitinib and vorinostat leads to highly potent inhibitors of JAK2 and histone deacetylase 6 (HDAC6)

Direct analysis – no sample preparation – of bioavailable cortisol in human plasma by weak affinity chromatography (WAC)

Comparison of weak affinity chromatography and surface plasmon resonance in determining affinity of small molecules

Synthesis, Biological Evaluation, WAC and NMR Studies of S‐Galactosides and Non‐Carbohydrate Ligands of Cholera Toxin Based on Polyhydroxyalkylfuroate Moieties

Immobilized lipodisks as model membranes in high-throughput HPLC-MS analysis

Elucidating the selectivity of recombinant forms of Aleuria aurantia lectin using weak affinity chromatography

Fragment screening of cyclin G-associated kinase by weak affinity chromatography

Weak affinity chromatography as a new approach for fragment screening in drug discovery

Toward high‐throughput drug screening on a chip‐based parallel affinity separation platform

Monitoring of influenza virus hemagglutinin in process samples using weak affinity ligands and surface plasmon resonance

Designing transient binding drugs: A new concept for drug discovery

Towards a FRET-based immunosensor for continuous carbohydrate monitoring

Porcine platelet lysate as a supplement for animal cell culture

Screening for transient biological interactions as applied to albumin ligands: A new concept for drug discovery

A label-free continuous total-internal-reflection-fluorescence-based immunosensor

Transiently binding antibody fragments against Lewis x and sialyl-Lewis x

HPLC analysis of carbohydrate deficient transferrin isoforms isolated by the Axis-Shield %CDT method

Analysis of the specificity and thermodynamics of the interaction between low affinity antibodies and carbohydrate antigens using fluorescence spectroscopy

Lectin affinity capillary electrophoresis in glycoform analysis applying the partial filling technique

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