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Anticalins in Drug Development

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Abstract

Anticalins are a novel class of engineered ligand-binding proteins that are prepared from lipocalins — conventional plasma proteins in humans —via targeted random mutagenesis and selection against prescribed haptens or antigens. The first anticalins were selected to bind to small ligands, such as the cardioactive drug digoxin. Recently, libraries that also permit the generation of anticalins with high affinities and specificities for protein targets, especially disease-related cell-surface receptors, have been constructed. Anticalins are much smaller than antibodies or their antigen-binding fragments, lack glycosylation as well as immunological effector functions, and consist of a single, stably folded polypeptide chain. Thus, they offer benefits as biopharmaceuticals in several areas of medical therapy, for example as receptor antagonists or as effective antidotes against toxic compounds.

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  1. The use of trade names is for product identification purposes only and does not imply endorsement

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Acknowledgments

The authors are associated with PIERIS Proteolab AG, a biopharmaceutical company focused on the development and commercialization of ANTICALINS® for therapeutic use. No sources of funding were used to assist in the preparation of this review.

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  1. PIERIS Proteolab AG, Freising-Weihenstephan, Germany

    Steffen Schlehuber

  2. Lehrstuhl für Bio-logische Chemie, Technische Universität München, 85350, Freising-Weihenstephan, Germany

    Arne Skerra

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Correspondence to Arne Skerra.

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Schlehuber, S., Skerra, A. Anticalins in Drug Development. BioDrugs 19, 279–288 (2005). https://doi.org/10.2165/00063030-200519050-00001

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