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Ref Type Journal Article
PMID (24387336)
Authors Zhao RX, Xu ZX
Title Targeting the LKB1 tumor suppressor.
Journal Current drug targets
Vol 15
Issue 1
Date 2014 Jan
URL
Abstract Text LKB1 (also known as serine-threonine kinase 11, STK11) is a tumor suppressor, which is mutated or deleted in Peutz-Jeghers syndrome (PJS) and in a variety of cancers. Physiologically, LKB1 possesses multiple cellular functions in the regulation of cell bioenergetics metabolism, cell cycle arrest, embryo development, cell polarity, and apoptosis. New studies demonstrated that LKB1 may also play a role in the maintenance of function and dynamics of hematopoietic stem cells. Over the past years, personalized therapy targeting specific genetic aberrations has attracted intense interests. Within this review, several agents with potential activity against aberrant LKB1 signaling have been discussed. Potential strategies and challenges in targeting LKB1 inactivation are also considered.

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Molecular Profile Treatment Approach
STK11 Q214* mTORC1 Inhibitor
STK11 S240* mTORC1 Inhibitor
STK11 E70* mTORC1 Inhibitor
STK11 Q123* mTORC1 Inhibitor
STK11 K78I mTORC1 Inhibitor
STK11 L67P mTORC1 Inhibitor
STK11 R304W mTORC1 Inhibitor
STK11 E223V mTORC1 Inhibitor
STK11 G163D mTORC1 Inhibitor
STK11 E57Sfs*107 mTORC1 Inhibitor
STK11 L282Afs*3 mTORC1 Inhibitor
STK11 L285Q mTORC1 Inhibitor
STK11 Q170P mTORC1 Inhibitor
STK11 P281Pfs*4 mTORC1 Inhibitor
STK11 G56Tfs*4 mTORC1 Inhibitor
STK11 E65* mTORC1 Inhibitor
STK11 K62Sfs*100 mTORC1 Inhibitor
STK11 L285Lfs*2 mTORC1 Inhibitor
STK11 A205T mTORC1 Inhibitor
STK11 W308C mTORC1 Inhibitor
STK11 E199K mTORC1 Inhibitor
STK11 T250P mTORC1 Inhibitor
STK11 P281L mTORC1 Inhibitor
STK11 K44* mTORC1 Inhibitor
STK11 F157S mTORC1 Inhibitor
STK11 D176Y mTORC1 Inhibitor
STK11 L245R mTORC1 Inhibitor
STK11 E120* mTORC1 Inhibitor
STK11 D207Gfs*59 mTORC1 Inhibitor
STK11 Y60* mTORC1 Inhibitor
STK11 D277Y mTORC1 Inhibitor
STK11 Y118* mTORC1 Inhibitor
STK11 H174R mTORC1 Inhibitor
STK11 D176N mTORC1 Inhibitor
STK11 S216F mTORC1 Inhibitor
STK11 K84* mTORC1 Inhibitor
STK11 Y49D mTORC1 Inhibitor
STK11 P281fs mTORC1 Inhibitor
STK11 G61Afs*3 mTORC1 Inhibitor
STK11 Y272H mTORC1 Inhibitor
STK11 Q170* mTORC1 Inhibitor
STK11 loss mTORC1 Inhibitor
STK11 E57fs mTORC1 Inhibitor
STK11 Q159* mTORC1 Inhibitor
STK11 Q100* mTORC1 Inhibitor
STK11 E121* mTORC1 Inhibitor
STK11 N181E mTORC1 Inhibitor
STK11 D194Y mTORC1 Inhibitor
STK11 E223* mTORC1 Inhibitor
STK11 E165* mTORC1 Inhibitor
STK11 M136R mTORC1 Inhibitor
STK11 G171S mTORC1 Inhibitor
STK11 D53Tfs*11 mTORC1 Inhibitor
STK11 E138* mTORC1 Inhibitor
STK11 K62* mTORC1 Inhibitor
STK11 I35Lfs*127 mTORC1 Inhibitor
STK11 E33* mTORC1 Inhibitor
STK11 D194E mTORC1 Inhibitor
STK11 A218Sfs*42 mTORC1 Inhibitor
STK11 E199* mTORC1 Inhibitor
STK11 I177N mTORC1 Inhibitor
STK11 P281Rfs*6 mTORC1 Inhibitor
STK11 Q37* mTORC1 Inhibitor
STK11 G135R mTORC1 Inhibitor
STK11 K78A mTORC1 Inhibitor
STK11 K48fs mTORC1 Inhibitor
STK11 inact mut mTORC1 Inhibitor
STK11 F354L mTORC1 Inhibitor
STK11 Q220* mTORC1 Inhibitor
STK11 Q137* mTORC1 Inhibitor
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References