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26 results on '"Vickers, Clare"'

7. Structure-Based Design of MptpB Inhibitors That Reduce Multidrug-Resistant Mycobacterium tuberculosis Survival and Infection Burden in Vivo

Author

Vickers, Clare F., primary, Silva, Ana P. G., additional, Chakraborty, Ajanta, additional, Fernandez, Paulina, additional, Kurepina, Natalia, additional, Saville, Charis, additional, Naranjo, Yandi, additional, Pons, Miquel, additional, Schnettger, Laura S., additional, Gutierrez, Maximiliano G., additional, Park, Steven, additional, Kreiswith, Barry N., additional, Perlin, David S., additional, Thomas, Eric J., additional, Cavet, Jennifer S., additional, and Tabernero, Lydia, additional

Published
2018
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8. NewProt – a protein engineering portal

Author

Schwarte, Andreas, primary, Genz, Maika, additional, Skalden, Lilly, additional, Nobili, Alberto, additional, Vickers, Clare, additional, Melse, Okke, additional, Kuipers, Remko, additional, Joosten, Henk-Jan, additional, Stourac, Jan, additional, Bendl, Jaroslav, additional, Black, Jon, additional, Haase, Peter, additional, Baakman, Coos, additional, Damborsky, Jiri, additional, Bornscheuer, Uwe, additional, Vriend, Gert, additional, and Venselaar, Hanka, additional

Published
2017
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13. Connecting unexplored protein crystal structures to enzymatic function

Author

Steffen-Munsberg, Fabian, Vickers, Clare, Thontowi, Ahmad, Schaetzle, Sebastian, Tumlirsch, Tony, Humble, Maria Svedendahl, Land, Henrik, Berglund, Per, Bornscheuer, Uwe T., Hoehne, Matthias, Steffen-Munsberg, Fabian, Vickers, Clare, Thontowi, Ahmad, Schaetzle, Sebastian, Tumlirsch, Tony, Humble, Maria Svedendahl, Land, Henrik, Berglund, Per, Bornscheuer, Uwe T., and Hoehne, Matthias

Abstract

AuthorCount:10

Published
2013
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14. Revealing the structural basis of promiscuous amine transaminase activity

Author

Steffen-Munsberg, Fabian, Vickers, Clare, Thontowi, Ahmad, Schaetzle, Sebastian, Meinhardt, Tina, Humble, Maria Svedendahl, Land, Henrik, Berglund, Per, Bornscheuer, Uwe T., Hoehne, Matthias, Steffen-Munsberg, Fabian, Vickers, Clare, Thontowi, Ahmad, Schaetzle, Sebastian, Meinhardt, Tina, Humble, Maria Svedendahl, Land, Henrik, Berglund, Per, Bornscheuer, Uwe T., and Hoehne, Matthias

Abstract

AuthorCount:10

Published
2013
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15. Structure-Based Design of MptpB Inhibitors That Reduce Multidrug-Resistant Mycobacterium tuberculosisSurvival and Infection Burden in Vivo

Author

Vickers, Clare F., Silva, Ana P. G., Chakraborty, Ajanta, Fernandez, Paulina, Kurepina, Natalia, Saville, Charis, Naranjo, Yandi, Pons, Miquel, Schnettger, Laura S., Gutierrez, Maximiliano G., Park, Steven, Kreiswith, Barry N., Perlin, David S., Thomas, Eric J., Cavet, Jennifer S., and Tabernero, Lydia

Abstract

Mycobacterium tuberculosisprotein-tyrosine-phosphatase B (MptpB) is a secreted virulence factor that subverts antimicrobial activity in the host. We report here the structure-based design of selective MptpB inhibitors that reduce survival of multidrug-resistant tuberculosis strains in macrophages and enhance killing efficacy by first-line antibiotics. Monotherapy with an orally bioavailable MptpB inhibitor reduces infection burden in acute and chronic guinea pig models and improves the overall pathology. Our findings provide a new paradigm for tuberculosis treatment.

Published
2018
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16. Engineering the Amine Transaminase from Vibrio fluvialis towards Branched-Chain Substrates.

Author

GENz, Maika, Melse, Okke, Schmidt, Sandy, Vickers, Clare, Dörr, Mark, van   dEN   Bergh, Tom, JoostEN, HENk ‐ Jan, and Bornscheuer, Uwe T.

Subjects
VIBRIO, AMINOTRANSFERASES, PHARMACEUTICAL industry, KETONES, BACTERIAL mutation, BIOINFORMATICS, ENANTIOMERS
Abstract

Chiral amines are important building blocks, especially for the pharmaceutical industry. Although amine transaminases (ATAs) are versatile enzymes to synthesize chiral amines, the wildtype enzymes do not accept ketones with two large substituents next to the carbonyl functionality. Using bioinformatic tools to design a seven-site mutant library followed by high-throughput screening, we were able to identify variants of the enzyme from Vibrio fluvialis (VF-ATA) with a widened binding pocket, as exemplified for a range of ketones. Three variants allowed the asymmetric synthesis of 2,2-dimethyl-1-phenylpropan-1-amine-not accessible by any wildtype ATA described so far. The best variant containing four mutations (L56V, W57C, F85V, V153A) gave 100 % conversion of the ketone to yield the amine with an enantiomeric excess value >99 %, notably with preference for the ( R)-enantiomer. In silico modeling enabled the reconstruction of the substrate binding mode to the newly evolved pocket and, hence, allowed explanation of the experimental results. [ABSTRACT FROM AUTHOR]

Published
2016
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17. Connecting Unexplored Protein Crystal Structures to Enzymatic Function

Author

Steffen-Munsberg, Fabian, primary, Vickers, Clare, additional, Thontowi, Ahmad, additional, Schätzle, Sebastian, additional, Tumlirsch, Tony, additional, Svedendahl Humble, Maria, additional, Land, Henrik, additional, Berglund, Per, additional, Bornscheuer, Uwe T., additional, and Höhne, Matthias, additional

Published
2012
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19. Synthesis of Unprotected Carboxy Indazoles via Pd-Catalyzed Carbonylation

Author

Wainwright, Philip, primary, Perni, Remedios, additional, Vickers, Clare, additional, Coffey, Steven B., additional, Buzon, Leanne, additional, DiRico, Kenneth, additional, Nelson, Kendra L., additional, Zhao, Zhengrong, additional, Limberakis, Chris, additional, Freeman-Cook, Kevin D., additional, and Corbett, Jeffrey W., additional

Published
2012
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21. Laws in the Making.

Author

Vickers, Clare

Subjects
Laws in the Making (Book) -- Book reviews, Books -- Book reviews
Published
1995

22. Revealing the Structural Basis of Promiscuous Amine Transaminase Activity.

Author

Steffen‐Munsberg, Fabian, Vickers, Clare, Thontowi, Ahmad, Schätzle, Sebastian, Meinhardt, Tina, Svedendahl Humble, Maria, Land, Henrik, Berglund, Per, Bornscheuer, Uwe T., and Höhne, Matthias

Subjects
*SUBSTRATES (Materials science), *ENZYME activation, *AMINO acids, *AMINOTRANSFERASES, *PROMISCUITY
Abstract

One lock for different keys: A flexible arginine in the active site allows γ‐aminobutyrate:pyruvate transaminases to bind the chemically different substrates L‐alanine and γ‐aminobutyric acid. Moreover, a flexible arginine residue facilitates the promiscuous conversion of (S)‐amines and ketones. The degree of promiscuity can be related to distinct key amino acids lying at the surface of the active site. [ABSTRACT FROM AUTHOR]

Published
2013
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23. Connecting Unexplored Protein Crystal Structures to Enzymatic Function.

Author

Steffen‐Munsberg, Fabian, Vickers, Clare, Thontowi, Ahmad, Schätzle, Sebastian, Tumlirsch, Tony, Svedendahl Humble, Maria, Land, Henrik, Berglund, Per, Bornscheuer, Uwe T., and Höhne, Matthias

Subjects
*CHEMICALS, *ENZYME analysis, *SITAGLIPTIN, *X-ray crystallography, *AMINES
Abstract

Digging in the database: Four synthetically useful transaminases for which no function was known were studied by evaluating a set of eight amino donors and seven acceptors (see figure). The four enzymes differ substantially in their catalytic properties and substrate preferences. We also used the enzymes in the asymmetric synthesis of a range of chiral amines and observed excellent enantioselectivities and conversions. [ABSTRACT FROM AUTHOR]

Published
2013
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25. Why I volunteer.

Author

Vickers, Clare

Subjects
VOLUNTEERS, MUSEUMS
Abstract

A personal narrative is presented which explores the author's experience as a volunteer at Wrexham County Borough Museum and Archives.

Published
2016

26. Enzymatic Late-Stage Oxidation of Lead Compounds with Solubilizing Biomimetic Docking/Protecting groups.

Author

Vickers C, Backfisch G, Oellien F, Piel I, and Lange UEW

Abstract

Late-stage functionalization of lead compounds is of high interest in drug discovery since it offers an easy access to metabolites and derivatives of a lead compound without the need to redesign an often long multistep synthesis. Owing to their high degree of chemoselectivity, biocatalytic transformations, enzymatic oxidations in particular, are potentially very powerful because they could allow the synthesis of less lipophilic derivatives of a lead compound. In the majority of cases, enzymatic oxidations have been used in an empirical way as their regioselectivity is difficult to predict. In this publication, the concept of using docking/protecting groups in a biomimetic fashion was investigated, which could help steer the regioselectivity of a P450 BM3 -mediated oxidation. A novel set of docking/protecting groups was designed that can be cleaved under very mild conditions and address the often problematic aqueous solubility of the substrates. Vabicaserin was used as tool compound containing typical groups such as basic, aliphatic, and aromatic moieties. The results were rationalized with the help of in silico docking and molecular dynamic studies., (© 2018 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.)

Published
2018
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