Bruton's tyrosine kinase as a new therapeutic target.
Targeting Bruton's tyrosine kinase (BTK) with a small molecule inhibitor may be useful in treatment of BTK-expressing malignancies because of the anti-apoptotic function of BTK in cancer cells. Furthermore, BTK inhibitors also exhibit anti-thrombotic properties that may be desirable in the context of the increased risk of thromboembolic complications in cancer patients. This review will focus on the role of BTK in drug resistance in cancer, thromboembolism, and various pathologic immune responses, such as graft versus host disease. The therapeutic potential of targeting BTK is illustrated by discussion of the biologic activity profile of the rationally designed BTK inhibitor LFM-A13.
Uckun
Fatih M
FM
Parker Hughes Cancer Center, 2848 Patton Road, St. Paul, MN 55113, USA. fatih_uckun@ih.org
Tibbles
Heather E
HE
Vassilev
Alexei O
AO
D000077329:Agammaglobulinaemia Tyrosine Kinase; D000577:Amides / Q000737:chemistry* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000737:chemistry* / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D015195:Drug Design; D006801:Humans; D007938:Leukemia / Q000150:complications / Q000188:drug therapy*; D009570:Nitriles / Q000737:chemistry* / Q000494:pharmacology; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000187:drug effects; D013923:Thromboembolism / Q000150:complications / Q000188:drug therapy
D000577:Amides; D000970:Antineoplastic Agents; C118451:LFM A13; D009570:Nitriles; D011505:Protein-Tyrosine Kinases; D000077329:Agammaglobulinaemia Tyrosine Kinase; C000625949:BTK protein, human