Abstract
Papain-like cysteine proteases bear an enormous potential as drug discovery targets for both infectious and systemic human diseases. The considerable progress in this field over the last two decades has also raised interest in the visualization of these enzymes in their native context, especially with regard to tumor imaging. After a short introduction to structure and general functions of human cysteine cathepsins, we highlight their importance for drug discovery and development and provide a critical update on the current state of knowledge toward their involvement in tumor progression, with a special emphasis on their role in therapy response. In accordance with a radiopharmaceutical point of view, the main focus of this review article will be the discussion of recently developed fluorescence and radiotracer-based imaging agents together with related molecular probes.
Highlights
Structural and Biochemical ConsiderationsThe term cathepsins was introduced by the famous chemist Richard Willstätter (1872–1942) and his PhD student Eugen Bamann (1900–1981) for the entirety of the intracellular proteases referring to their protein-degrading activity in the first half of the last century (Figure 1) (Willstätter and Bamann, 1929)
Because they share a high degree of homology to the plant enzyme papain, the cysteine cathepsins are included in the C1 family of clan CA according to the MEROPS protease classification system (Rawlings et al, 2014
Inhibitors based on small molecules that target papainlike cysteine proteases have contributed substantially to the understanding of the catalytic mechanisms, enzyme-substrate recognition and the biological functions of this class of proteolytic enzymes
Summary
The term cathepsins was introduced by the famous chemist Richard Willstätter (1872–1942) and his PhD student Eugen Bamann (1900–1981) for the entirety of the intracellular proteases referring to their protein-degrading activity (greek καθεψειν = to digest, to boil) in the first half of the last century (Figure 1) (Willstätter and Bamann, 1929). In this sense, their physiological functions were for long time considered to be restricted to cellular protein catabolism.
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