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Nat Rev Drug Discov. 2013 Aug;12(8):611-29. doi: 10.1038/nrd4088.

Therapeutic modulators of STAT signalling for human diseases.

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Cancer Biology, and Natural Products and Experimental Therapeutics Programs, University of Hawaii Cancer Center, 701 Ilalo Street, Honolulu, Hawaii 96813, USA.


The signal transducer and activator of transcription (STAT) proteins have important roles in biological processes. The abnormal activation of STAT signalling pathways is also implicated in many human diseases, including cancer, autoimmune diseases, rheumatoid arthritis, asthma and diabetes. Over a decade has passed since the first inhibitor of a STAT protein was reported and efforts to discover modulators of STAT signalling as therapeutics continue. This Review discusses the outcomes of the ongoing drug discovery research endeavours against STAT proteins, provides perspectives on new directions for accelerating the discovery of drug candidates, and highlights the noteworthy candidate therapeutics that have progressed to clinical trials.

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