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Jennifer Hochscherf     Other 
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Jennifer Hochscherf published an article in July 2018.
Top co-authors See all
Andrew Abell

124 shared publications

ARC Centre of Excellence for Nanoscale Biophotonics, Institute for Photonics and Advanced Sensing, School of Physical Sciences, The University of Adelaide, Adelaide, SA 5005, Australia

Joachim Jose

115 shared publications

Institut für Pharmazeutische und Medizinische Chemie, PharmaCampus, Westfälische Wilhelms-Universität Münster, 48149 Münster, Germany

Marc Le Borgne

94 shared publications

E Faculté de Pharmacie-ISPB, Department of Bioactive Molecules and Medicinal Chemistry , Université de Lyon, Université Claude Bernard Lyon 1 , Lyon , France

Karsten Niefind

75 shared publications

Department für Chemie, Institut für Biochemie, Universität zu Köln, Zülpicher Straße 47, D-50674 Köln, Germany

Zouhair Bouaziz

30 shared publications

Université de Lyon, Université Claude Bernard Lyon 1, Faculté de Pharmacie - ISPB, EA 4446 Bioactive Molecules and Medicinal Chemistry, SFR Santé Lyon-Est CNRS UMS3453-INSERM US7, Lyon, France

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Distribution of Articles published per year 
(2015 - 2018)
Total number of journals
published in
 
4
 
Publications
Article 3 Reads 0 Citations Crystal structure of highly glycosylated human leukocyte elastase in complex with an S2′ site binding inhibitor Jennifer Hochscherf, Markus Pietsch, William Tieu, Kevin Kua... Published: 26 July 2018
Acta Crystallographica Section F Structural Biology Communications, doi: 10.1107/s2053230x1800537x
DOI See at publisher website
Article 0 Reads 0 Citations Unexpected Binding Mode of a Potent Indeno[1,2-b]indole-Type Inhibitor of Protein Kinase CK2 Revealed by Complex Structu... Jennifer Hochscherf, Dirk Lindenblatt, Benedict Witulski, Ro... Published: 13 December 2017
Pharmaceuticals, doi: 10.3390/ph10040098
DOI See at publisher website PubMed View at PubMed ABS Show/hide abstract
Protein kinase CK2, a member of the eukaryotic protein kinase superfamily, is associated with cancer and other human pathologies and thus an attractive drug target. The indeno[1,2-b]indole scaffold is a novel lead structure to develop ATP-competitive CK2 inhibitors. Some indeno[1,2-b]indole-based CK2 inhibitors additionally obstruct ABCG2, an ABC half transporter overexpressed in breast cancer and co-responsible for drug efflux and resistance. Comprehensive derivatization studies revealed substitutions of the indeno[1,2-b]indole framework that boost either the CK2 or the ABCG2 selectivity or even support the dual inhibition potential. The best indeno[1,2-b]indole-based CK2 inhibitor described yet (IC50 = 25 nM) is 5-isopropyl-4-(3-methylbut-2-enyl-oxy)-5,6,7,8-tetrahydroindeno[1,2-b]indole-9,10-dione (4p). Herein, we demonstrate the membrane permeability of 4p and describe co-crystal structures of 4p with CK2α and CK2α′, the paralogs of human CK2 catalytic subunit. As expected, 4p occupies the narrow, hydrophobic ATP site of CK2α/CK2α′, but surprisingly with a unique orientation: its hydrophobic substituents point towards the solvent while its two oxo groups are hydrogen-bonded to a hidden water molecule. An equivalent water molecule was found in many CK2α structures, but never as a critical mediator of ligand binding. This unexpected binding mode is independent of the interdomain hinge/helix αD region conformation and of the salt content in the crystallization medium.
BOOK-CHAPTER 0 Reads 0 Citations Impressions from the Conformational and Configurational Space Captured by Protein Kinase CK2 Jennifer Hochscherf, Alexander Schnitzler, Karsten Niefind Published: 11 February 2015
Protein Kinase CK2 Cellular Function in Normal and Disease States, doi: 10.1007/978-3-319-14544-0_2
DOI See at publisher website
Article 0 Reads 3 Citations Development of a high-throughput screening-compatible assay to identify inhibitors of the CK2α/CK2β interaction Jennifer Hochscherf, Dirk Lindenblatt, Michaela Steinkrüger,... Published: 01 January 2015
Analytical Biochemistry, doi: 10.1016/j.ab.2014.09.003
DOI See at publisher website PubMed View at PubMed
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