Non-Receptor Tyrosine Kinase (Non-RTK) Inhibitors
Non-RTKs are cytosolic TK enzymes that doesn't have a transmembrane domein. Non-RTK's activity is regulated by other factors on cell surface or in the cytoplasm and it transmits signals. Human non-RTK family includes ABL, ACK, CSK, FAK, FES, FRK, JAK, SRC, TEC and SYK. Mutations in a gene for non-RTKs (including BCR-ABL) can result in an aberrant activity of this enzyme; pathologically increased activity of non-RTK may be responsible for growth of malignances, the induction of drug-resistance, and formation of metastasis. Non-RTKs are regarded as important targets in development of anti-tumor agents.
SRC family Kinase Inhibitors
SRC family kinase (SFK) containing c-Scr, Blk, Fgr, Hc,, Lck, Lyk and so on is one of very impor-tant protein group in cancer research. And it is a target of diabetic research because it deeply participates in such processes as secretion of insulin, insulin-resistance and metabolism of glucose. Furthermore, it has been also a object of study in inflammatory research.
JAK Family Kinase Inhibitors
JAK (Janus Kinase) family consists of JAK1, JAK2, JAK3 and TYK2. It has a key role on JAK-STAT (Janus kinase-signal tranducer and of transcription) pathway, and immunosuppression research has been done by inhibiting it since it participates in regulation of immune response.
ABL Family Kinase Inhibitors
ABL kinase (Abelson tyrosine-protein kinase) family includes ABL1 and ARG (ABL2). ABL is said to be deeply involved in chronic myelocytic leukemia (CML) through becoming BCR-ABL fusion gene due to genetic abnormality caused by chromosomal translocation. Imatinib Mesylate [I0936], which inhibits tyrosine kinase activity of BCR-ABL protein has been used as therapeutic agent for CML.
TEC Family Kinase Inhibitors
TEC family kinase includes BTK, BMX, ITK, TEC and TXK. It abounds in blood-forming tissues and it plays a sufficient role in activation of T cell and development/activation of B cell. BTK is especially necessary for development of B cell, so it has been watched as a target of malignant lymphoma therapeutic agent and anti-inflammatory agent.
SYK Family Kinase Inhibitors
SYK (Spleen Tyrosine Kinase) highly expresses in blood immune cells and bone marrow cells and it has been studied for relation with cancer, autoimmune disease and infection disease.