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Acta Crystallographica Section A Foundations and Advances, ISSN 2053-2733, 08/2016, Volume 72, Issue a1, pp. s4 - s5
Journal Article
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 04/2016, Volume 26, Issue 8, pp. 2065 - 2067
We report structure-guided modifications of the benzyloxy substituent of the Insulin-like Growth Factor-1 Receptor (IGF-1R) inhibitor NVP-AEW541. This chemical... 
Journal Article
British Journal of Pharmacology, ISSN 0007-1188, 06/2015, Volume 172, Issue 11, pp. 2675 - 2700
Journal Article
British Journal of Pharmacology, ISSN 0007-1188, 06/2015, Volume 172, Issue 11, pp. 2675 - 2700
Journal Article
Nature, ISSN 0028-0836, 03/2017, Volume 543, Issue 7647, pp. 733 - 737
Journal Article
Blood, ISSN 0006-4971, 11/2011, Volume 118, Issue 21, pp. 2746 - 2746
Abstract Abstract 2746 Background: The tyrosine kinase (TK) activity of the ABL protein is normally tightly regulated, with the N-terminal cap (NCap) region (≈... 
Journal Article
Current topics in medicinal chemistry, 2017, Volume 17, Issue 1, p. 59
The need for novel approaches for targeting well-known protein families in drug discovery has been discussed for several years. There is a huge amount of... 
Protein Kinases - metabolism | Allosteric Regulation | Humans | Protein Kinase Inhibitors - pharmacology | Binding Sites
Journal Article
Nature, ISSN 0028-0836, 01/2010, Volume 463, Issue 7280, pp. 501 - 506
In an effort to find new pharmacological modalities to overcome resistance to ATP-binding-site inhibitors of Bcr-Abl, we recently reported the discovery of... 
CELL LUNG-CANCER | KINASE-INHIBITOR | SELECTIVE INHIBITOR | C-ABL | TYROSINE KINASE | MULTIDISCIPLINARY SCIENCES | DYNAMICS | MUTATIONS | LYMPHOBLASTIC-LEUKEMIA | IMATINIB RESISTANCE | CHRONIC MYELOID-LEUKEMIA | Humans | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - drug therapy | Male | Transplantation, Heterologous | Piperazines - chemistry | Pyrimidines - chemistry | Pyrimidines - metabolism | Antineoplastic Agents - metabolism | Mass Spectrometry | Bone Marrow Transplantation | Inhibitory Concentration 50 | Female | Antineoplastic Agents - pharmacology | Binding Sites | Disease Models, Animal | Fusion Proteins, bcr-abl - chemistry | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - enzymology | Protein Structure, Tertiary | Crystallization | Antineoplastic Combined Chemotherapy Protocols | Models, Molecular | Pyrimidines - pharmacology | Antineoplastic Agents - chemistry | Mutation - genetics | Imatinib Mesylate | Piperazines - pharmacology | Fusion Proteins, bcr-abl - genetics | Animals | Cell Line, Tumor | Leukemia, Myelogenous, Chronic, BCR-ABL Positive - metabolism | Mice | Benzamides | Fusion Proteins, bcr-abl - metabolism | Drug Resistance, Neoplasm - drug effects | Nilotinib | Dasatinib | Drug resistance in microorganisms | Usage | Nuclear magnetic resonance spectroscopy | Research | Chronic myeloid leukemia | X-ray crystallography | Chromosome abnormalities | Gene mutations | Analysis | Genetic aspects | Diagnosis | Binding proteins | Drug therapy | Health aspects | Proteins | Studies | Competition | Enzymes | E coli | Kinases | Drug resistance | Crystal structure | Index Medicus
Journal Article
Blood, ISSN 0006-4971, 11/2011, Volume 118, Issue 21, pp. 1674 - 1674
Abstract Abstract 1674 Background: Imatinib, nilotinib and dasatinib are effective therapies for chronic myeloid leukemia, as a consequence of their inhibiting... 
Journal Article
Current topics in medicinal chemistry, ISSN 1568-0266, 2017, Volume 17, Issue 1, pp. 59 - 70
The need for novel approaches for targeting well-known protein families in drug discovery has been discussed for several years. There is a huge amount of... 
Allosteric | Activator | Kinase | Binding mode | Inhibitor | Structure-Based Drug Discovery | Target Space | CATALYTIC SUBUNIT | CHEMISTRY, MEDICINAL | C-ABL | PROTEIN-KINASE | TYROSINE KINASE | BCR-ABL | PSEUDOKINASE DOMAIN | CRYSTAL-STRUCTURES | P21-ACTIVATED KINASES | SMALL-MOLECULE INHIBITOR | STRUCTURAL BASIS
Journal Article