A small-molecule mimic of a peptide docking motif inhibits the protein kinase PDK1

Proceedings of the National Academy of Sciences of the United States of America

Volumn 111, Issue 52, 2014, Pages 18590-18595

  Rettenmaier, T Justin ^a   Sadowsky, Jack D ^a,c   Thomsen, Nathan D ^a,d   Chen, Steven C ^a   Doak, Allison K ^a   Arkin, Michelle R ^a   Wells, James A ^a,b  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b UNIVERSITY OF CALIFORNIA   (United States)

^c GENENTECH INC   (United States)

^d GILEAD SCIENCES   (United States)

Author keywords

Allostery; Drug discovery; Peptide mimicry; Protein protein interaction

Indexed keywords

ADENOSINE TRIPHOSPHATE; LIGAND; PDK1 INTERACTING FRAGMENT PEPTIDE; PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE 1; PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE 1 INHIBITOR; PROTEIN KINASE INHIBITOR; SULFONAMIDE; UNCLASSIFIED DRUG; 3 PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE; ANTINEOPLASTIC AGENT; PDPK1 PROTEIN, HUMAN; PEPTIDE; TUMOR PROTEIN;

ALLOSTERISM; ANTINEOPLASTIC ACTIVITY; ARTICLE; BINDING AFFINITY; BINDING SITE; CONTROLLED STUDY; CRYSTAL STRUCTURE; ENZYME ACTIVATION; HEK293 CELL LINE; HUMAN; HUMAN CELL; IC50; IN VITRO STUDY; MOLECULAR DOCKING; MOLECULAR MIMICRY; MUTATIONAL ANALYSIS; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN EXPRESSION; PROTEIN MOTIF; PROTEIN PROTEIN INTERACTION; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG EFFECTS; ENZYMOLOGY; GENETICS; METABOLISM; NEOPLASMS; PATHOLOGY; PROTEIN SECONDARY STRUCTURE; X RAY CRYSTALLOGRAPHY;

RUMEX;

3-PHOSPHOINOSITIDE-DEPENDENT PROTEIN KINASES; ALLOSTERIC REGULATION; ALLOSTERIC SITE; AMINO ACID MOTIFS; ANTINEOPLASTIC AGENTS; CRYSTALLOGRAPHY, X-RAY; HEK293 CELLS; HUMANS; MOLECULAR DOCKING SIMULATION; NEOPLASM PROTEINS; NEOPLASMS; PEPTIDES; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, SECONDARY;

EID: 84924384879     PISSN: 00278424     EISSN: 10916490     Source Type: Journal    
DOI: 10.1073/pnas.1415365112     Document Type: Article

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