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Journal of medicinal chemistry, ISSN 0022-2623, 08/2012, Volume 55, Issue 16, pp. 7193 - 7207
Journal Article
PloS one, ISSN 1932-6203, 06/2014, Volume 9, Issue 6, pp. e100880 - e100880
.... GSK2110183 and GSK2141795 are orally bioavailable, potent inhibitors of the AKT kinases that have progressed to human clinical studies... 
Science & Technology - Other Topics | Multidisciplinary Sciences | Science & Technology | Ribosomal Protein S6 Kinases - metabolism | Pyrazoles - chemical synthesis | Antineoplastic Agents - chemical synthesis | Humans | Gene Expression Regulation, Neoplastic | Phosphatidylinositol 3-Kinases - metabolism | Phosphatidylinositol 3-Kinases - antagonists & inhibitors | Proto-Oncogene Proteins c-akt - genetics | Pancreatic Neoplasms - drug therapy | PTEN Phosphohydrolase - antagonists & inhibitors | Female | Antineoplastic Agents - pharmacology | Drug Evaluation, Preclinical | MAP Kinase Kinase Kinases - antagonists & inhibitors | Proto-Oncogene Proteins c-akt - metabolism | Pyrazoles - pharmacology | PTEN Phosphohydrolase - genetics | Protein Kinase Inhibitors - chemical synthesis | Signal Transduction | Administration, Oral | MAP Kinase Kinase Kinases - genetics | Pancreatic Neoplasms - pathology | Pancreatic Neoplasms - enzymology | PTEN Phosphohydrolase - metabolism | Pancreatic Neoplasms - genetics | MAP Kinase Kinase Kinases - metabolism | Mice, SCID | Drug Synergism | Phosphatidylinositol 3-Kinases - genetics | Xenograft Model Antitumor Assays | Animals | Tumor Burden - drug effects | Cell Line, Tumor | Diamines - pharmacology | Mice | Protein Kinase Inhibitors - pharmacology | Blood Glucose - metabolism | Diamines - chemical synthesis | Ribosomal Protein S6 Kinases - antagonists & inhibitors | Ribosomal Protein S6 Kinases - genetics | Proto-Oncogene Proteins c-akt - antagonists & inhibitors | Cellular signal transduction | Glucose | Phosphotransferases | Dextrose | Tumors | Biotechnology | Phosphorylation | Animal models | Leukemia | Homeostasis | Oncology | AKT protein | Kinases | K-Ras protein | Anticancer properties | Feedback | Polyethylene glycol | Inhibition | Enzymes | Tumor cells | MAP kinase | Breast cancer | Bioavailability | Substrates | 1-Phosphatidylinositol 3-kinase | Studies | Signaling | Inhibitors | Pancreatic cancer | Mutation | Laboratory animals | ATP | PTEN protein | Cancer | Apoptosis | Index Medicus
Journal Article
Journal Article
Journal Article
Journal Article
Journal Article
Molecules (Basel, Switzerland), ISSN 1420-3049, 08/2018, Volume 23, Issue 9, p. 2181
Journal Article
Chemical biology & drug design, ISSN 1747-0277, 01/2011, Volume 77, Issue 1, pp. 1 - 11
The BCR‐ABL inhibitor imatinib has revolutionized the treatment of chronic myeloid leukemia... 
kinase | ponatinib | AP24534 | drug discovery | X‐ray crystallography | structure‐based drug design | X-ray crystallography | Structure-based drug design | Drug discovery | Ponatinib | Kinase | Pharmacology & Pharmacy | Biochemistry & Molecular Biology | Life Sciences & Biomedicine | Chemistry, Medicinal | Science & Technology | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - drug therapy | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - genetics | Crystallography, X-Ray | Piperazines - chemistry | Structure-Activity Relationship | Pyridazines - pharmacology | Pyridazines - chemical synthesis | Pyrimidines - chemistry | Protein Kinase Inhibitors - chemistry | Protein Binding - drug effects | Imidazoles - chemical synthesis | Imidazoles - therapeutic use | Pyridazines - therapeutic use | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - enzymology | Imidazoles - pharmacology | Piperazines - therapeutic use | Pyrimidines - pharmacology | Imatinib Mesylate | Piperazines - pharmacology | Drug Resistance, Neoplasm - genetics | Fusion Proteins, bcr-abl - genetics | Animals | Mutation - drug effects | Protein Kinase Inhibitors - therapeutic use | Pyrimidines - therapeutic use | Fusion Proteins, bcr-abl - antagonists & inhibitors | Cell Line, Tumor | Mice | Protein Kinase Inhibitors - pharmacology | Benzamides | Fluoroimmunoassay | Fusion Proteins, bcr-abl - metabolism | Drug Resistance, Neoplasm - drug effects | Drug resistance | Analysis | Leukemia | Index Medicus | STRUCTURE-ACTIVITY RELATIONSHIPS | MUTANTS | BASIC BIOLOGICAL SCIENCES | ENZYME INHIBITORS | TYROSINE | GENE MUTATIONS | PHOSPHOTRANSFERASES | MYELOID LEUKEMIA | MUTATIONS | ANTINEOPLASTIC DRUGS | 60 APPLIED LIFE SCIENCES | RESIDUES
Journal Article
Journal of medicinal chemistry, ISSN 0022-2623, 02/2013, Volume 56, Issue 3, pp. 640 - 659
.... This work, together with crystal structures of selected inhibitors in complex with both enzymes described in a companion paper, provides a rationale for the observed SAR. 12u demonstrates potent anticancer activity against primary chronic lymphocytic leukemia cells with a therapeutic window 31- and 107-fold over those of normal B- and T-cells. 
Protein Kinase Inhibitors - chemical synthesis | Magnetic Resonance Spectroscopy | Pyrimidines - chemical synthesis | Antineoplastic Agents - chemical synthesis | Humans | Models, Molecular | Crystallography, X-Ray | Cyclin-Dependent Kinase 9 - antagonists & inhibitors | Structure-Activity Relationship | Pyrimidines - pharmacology | Antineoplastic Agents - chemistry | Pyrimidines - chemistry | Protein Kinase Inhibitors - chemistry | Spectrometry, Mass, Electrospray Ionization | Cell Line, Tumor | Antineoplastic Agents - pharmacology | Molecular Structure | Protein Kinase Inhibitors - pharmacology | Drug Screening Assays, Antitumor | Index Medicus | Antitumor activity
Journal Article
Journal Article