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Uda, N.R.* ; Seibert, V.* ; Stenner-Liewen, F.* ; Müller, P.* ; Herzig, P.* ; Gondi, G.* ; Zeidler, R. ; van Dijk, M.* ; Zippelius, A.* ; Renner, C.*

Esterase activity of carbonic anhydrases serves as surrogate for selecting antibodies blocking hydratase activity.

J. Enzyme Inhib. Med. Chem. 30, 955-960 (2015)
DOI PMC
Open Access Gold möglich sobald Verlagsversion bei der ZB eingereicht worden ist.
Carbonic anhydrase 9 (CA9) and carbonic anhydrase 12 (CA12) were proposed as potential targets for cancer therapy more than 20 years ago. However, to date, there are only very few antibodies that have been described to specifically target CA9 and CA12 and also block the enzymatic activity of their targets. One of the early stage bottlenecks in identifying CA9- and CA12-inhibiting antibodies has been the lack of a high-throughput screening system that would allow for rapid assessment of inhibition of the targeted carbon dioxide hydratase activity of carbonic anhydrases. In this study, we show that measuring the esterase activity of carbonic anhydrase offers a robust and inexpensive screening method for identifying antibody candidates that block both hydratase and esterase activities of carbonic anhydrase's. To our knowledge, this is the first implementation of a facile surrogate-screening assay to identify potential therapeutic antibodies that block the clinically relevant hydratase activity of carbonic anhydrases.
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Publikationstyp Artikel: Journalartikel
Dokumenttyp Wissenschaftlicher Artikel
Korrespondenzautor
Schlagwörter Cancer Therapy ; Carbonic Anhydrase 9 & 12 ; Enzyme Inhibition ; High-throughput Screening ; Renal Cell Cancer; Renal-cell Carcinoma; Monoclonal-antibody; Intracellular Ph; Hydrophobic Pocket; Enzymatic-activity; Ix; Protein; Xii; Inhibitors; Hypoxia
ISSN (print) / ISBN 1475-6366
e-ISSN 1475-6374
Zeitschrift Journal of Enzyme Inhibition and Medicinal Chemistry
Quellenangaben Band: 30, Heft: 6, Seiten: 955-960 Artikelnummer: , Supplement: ,
Verlag Informa Healthcare
Verlagsort London
Nichtpatentliteratur Publikationen
Begutachtungsstatus Peer reviewed
Institut(e) Research Unit Gene Vector (AGV)