Target family classification

Naumann, T. and Matter, H. (2002) Structural classification of protein kinases using 3d molecular interaction field analysis of their ligand binding sites Target family landscapes../. Med. Chem. 45, 2366-2378. 

Based on their sequence homology, disulfide connectivity, and cysteine location within the sequence and chemistry of the reactive site. Pis can be assigned to distinct families, as classified by Laskowski and Kato. Kunitz-type, Bowman—Birk-type, Potato type I and type II, and squash inhibitors are members of these families shown in Table 3. For inhibitors not falling into these classifications more families have been proposed. Pis can also be classified by their target/mode of action. Plants have been found to express Pis that target serine proteinases, cysteine proteinases, aspartic proteinases, and metallo-proteinases. Serine and cysteine protease inhibitors are the best-studied PIs. ... 

Table 1 Classification and Description of the Different Targets included in the In vitro Pharmacological BioPrint Profile. The number of assays per each family is detailed. Among the receptors there are 91 G-protein coupled receptors.

The emphasis in this contribution is laid on an emerging paradigm in drug discovery, notably the systematic classification of therapeutically relevant target classes according to structure and function. These are subsequently correlated with family-wide recognition motifs that can be translated into lead-like low-molecular-... 

The classification of ion channels by their topology is exemplified for potassium channels in Figure 8.1 [1], Potassium channels can be classified into 2TM/P channels, which contain two transmembrane helices (TM) with one P loop (P) between them, 6TM/P channels, 7TM/P channels, 8TM/2P channels, and 4TM/2P channels. The 4TM/2P family is called leakage channels and is targeted by numerous anesthetics [8],... 

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