标题
An update on dual Src/Abl inhibitors
作者
关键词
-
出版物
Future Medicinal Chemistry
Volume 4, Issue 6, Pages 799-822
出版商
Future Science, LTD
发表日期
2012-04-25
DOI
10.4155/fmc.12.29
参考文献
相关参考文献
注意:仅列出部分参考文献,下载原文获取全部文献信息。- Dasatinib Treatment for Imatinib Resistant or Intolerant Patients with Chronic Myeloid Leukaemia
- (2013) J Li et al. JOURNAL OF INTERNATIONAL MEDICAL RESEARCH
- Phase II study of single-agent bosutinib, a Src/Abl tyrosine kinase inhibitor, in patients with locally advanced or metastatic breast cancer pretreated with chemotherapy
- (2011) M. Campone et al. ANNALS OF ONCOLOGY
- Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR–ABL including the T315I gatekeeper mutant
- (2011) Mathew Thomas et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Identification of potent c-Src inhibitors strongly affecting the proliferation of human neuroblastoma cells
- (2011) Marco Radi et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Chronic myeloid leukemia stem cells are not dependent on Bcr-Abl kinase activity for their survival
- (2011) A. Hamilton et al. BLOOD
- Development of an Effective Therapy for Chronic Myelogenous Leukemia
- (2011) David W. Woessner et al. CANCER JOURNAL
- Novel Combination Treatments Targeting Chronic Myeloid Leukemia Stem Cells
- (2011) Tareq Al Baghdadi et al. Clinical Lymphoma Myeloma & Leukemia
- Pediatric Phase I Trial and Pharmacokinetic Study of Dasatinib: A Report From the Children's Oncology Group Phase I Consortium
- (2011) Richard Aplenc et al. JOURNAL OF CLINICAL ONCOLOGY
- Design, Synthesis, Biological Activity, and ADME Properties of Pyrazolo[3,4-d]pyrimidines Active in Hypoxic Human Leukemia Cells: A Lead Optimization Study
- (2011) Marco Radi et al. JOURNAL OF MEDICINAL CHEMISTRY
- Potent Activity of Ponatinib (AP24534) in Models of FLT3-Driven Acute Myeloid Leukemia and Other Hematologic Malignancies
- (2011) J. M. Gozgit et al. MOLECULAR CANCER THERAPEUTICS
- Once-daily Dasatinib: Expansion of Phase II Study Evaluating Safety and Efficacy of Dasatinib in Patients With Metastatic Castration-resistant Prostate Cancer
- (2011) Evan Y. Yu et al. UROLOGY
- Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors
- (2010) Diane H. Boschelli et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFR , Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants
- (2010) E. Weisberg et al. BLOOD
- Combined Src and ER blockade impairs human breast cancer proliferation in vitro and in vivo
- (2010) Yi Chen et al. BREAST CANCER RESEARCH AND TREATMENT
- Allosteric inhibition of BCR-ABL
- (2010) A. Quamrul Hassan et al. CELL CYCLE
- Structural Mechanism of the Pan-BCR-ABL Inhibitor Ponatinib (AP24534): Lessons for Overcoming Kinase Inhibitor Resistance
- (2010) Tianjun Zhou et al. Chemical Biology & Drug Design
- Affinity Reagents that Target a Specific Inactive Form of Protein Kinases
- (2010) Pratistha Ranjitkar et al. CHEMISTRY & BIOLOGY
- Src Inhibitors in Lung Cancer: Current Status and Future Directions
- (2010) Sacha I. Rothschild et al. Clinical Lung Cancer
- New Opportunities to Treat the T315I-Bcr-Abl Mutant in Chronic Myeloid Leukaemia: Tyrosine Kinase Inhibitors and Molecules that Act by Alternative Mechanisms
- (2010) S. Schenone et al. CURRENT MEDICINAL CHEMISTRY
- Novel dual Src/Abl inhibitors for hematologic and solid malignancies
- (2010) Silvia Schenone et al. EXPERT OPINION ON INVESTIGATIONAL DRUGS
- New pyrazolo-[3,4-d]-pyrimidine derivative Src kinase inhibitors lead to cell cycle arrest and tumor growth reduction of human medulloblastoma cells
- (2010) Alessandra Rossi et al. FASEB JOURNAL
- Dasatinib Inhibits the Development of Metastases in a Mouse Model of Pancreatic Ductal Adenocarcinoma
- (2010) Jennifer P. Morton et al. GASTROENTEROLOGY
- Curcumin enhances dasatinib-induced inhibition of growth and transformation of colon cancer cells
- (2010) Jyoti Nautiyal et al. INTERNATIONAL JOURNAL OF CANCER
- Human chronic myeloid leukemia stem cells are insensitive to imatinib despite inhibition of BCR-ABL activity
- (2010) Amie S. Corbin et al. JOURNAL OF CLINICAL INVESTIGATION
- Phase I/II Study of the Src Inhibitor Dasatinib in Combination With Erlotinib in Advanced Non–Small-Cell Lung Cancer
- (2010) Eric B. Haura et al. JOURNAL OF CLINICAL ONCOLOGY
- Phase II Study of Dasatinib in Patients With Advanced Non–Small-Cell Lung Cancer
- (2010) Faye M. Johnson et al. JOURNAL OF CLINICAL ONCOLOGY
- Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant
- (2010) Wei-Sheng Huang et al. JOURNAL OF MEDICINAL CHEMISTRY
- The Src Inhibitor AZD0530 Blocks Invasion and May Act as a Radiosensitizer in Lung Cancer Cells
- (2010) Phillip R. Purnell et al. Journal of Thoracic Oncology
- A Phase II Study of Dasatinib in Patients with Chemosensitive Relapsed Small Cell Lung Cancer (Cancer and Leukemia Group B 30602)
- (2010) Antonius A. Miller et al. Journal of Thoracic Oncology
- Beneficial effects of combining a type II ATP competitive inhibitor with an allosteric competitive inhibitor of BCR-ABL for the treatment of imatinib-sensitive and imatinib-resistant CML
- (2010) E Weisberg et al. LEUKEMIA
- Activity of the potent dual Abl/Src tyrosine kinase inhibitor FB2 against Bcr–Abl positive cell lines in vitro and in vivo
- (2010) Xia Yuan et al. LEUKEMIA RESEARCH
- Src family kinase inhibitor PP2 efficiently inhibits cervical cancer cell proliferation through down-regulating phospho-Src-Y416 and phospho-EGFR-Y1173
- (2010) Lu Kong et al. MOLECULAR AND CELLULAR BIOCHEMISTRY
- Bivalent inhibitors of the tyrosine kinases ABL and SRC: determinants of potency and selectivity
- (2010) Zachary B. Hill et al. Molecular BioSystems
- Discovery and Characterization of Novel Mutant FLT3 Kinase Inhibitors
- (2010) E. Weisberg et al. MOLECULAR CANCER THERAPEUTICS
- SKI-606 (Bosutinib) Blocks Prostate Cancer Invasion, Growth, and Metastasis In vitro and In vivo through Regulation of Genes Involved in Cancer Growth and Skeletal Metastasis
- (2010) S. A. Rabbani et al. MOLECULAR CANCER THERAPEUTICS
- Dasatinib versus Imatinib in Newly Diagnosed Chronic-Phase Chronic Myeloid Leukemia
- (2010) Hagop Kantarjian et al. NEW ENGLAND JOURNAL OF MEDICINE
- Control of mammary tumor differentiation by SKI-606 (bosutinib)
- (2010) L Hebbard et al. ONCOGENE
- Structure–activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: Toward selective Abl inhibitors
- (2009) Christophe Antczak et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- The effect of the dual Src/Abl kinase inhibitor AZD0530 on Philadelphia positive leukaemia cell lines
- (2009) Patricia Mambou Gwanmesia et al. BMC CANCER
- Dasatinib synergizes with doxorubicin to block growth, migration and invasion of breast cancer cells
- (2009) C S Pichot et al. BRITISH JOURNAL OF CANCER
- AP24534, a Pan-BCR-ABL Inhibitor for Chronic Myeloid Leukemia, Potently Inhibits the T315I Mutant and Overcomes Mutation-Based Resistance
- (2009) Thomas O'Hare et al. CANCER CELL
- Equally Potent Inhibition of c-Src and Abl by Compounds that Recognize Inactive Kinase Conformations
- (2009) M. A. Seeliger et al. CANCER RESEARCH
- Structural Analysis of DFG-in and DFG-out Dual Src-Abl Inhibitors Sharing a Common Vinyl Purine Template
- (2009) Tianjun Zhou et al. Chemical Biology & Drug Design
- AP24163 Inhibits the Gatekeeper Mutant of BCR-ABL and SuppressesIn vitroResistance
- (2009) Mohammad Azam et al. Chemical Biology & Drug Design
- 3D QSAR Models Built on Structure-Based Alignments of Abl Tyrosine Kinase Inhibitors
- (2009) Federico Falchi et al. ChemMedChem
- Antitumor Effects and Biomarkers of Activity of AZD0530, a Src Inhibitor, in Pancreatic Cancer
- (2009) N.V. Rajeshkumar et al. CLINICAL CANCER RESEARCH
- New SRC/ABL inhibitors for chronic myeloid leukemia therapy show selectivity for T315I ABL mutant CD34+ cells
- (2009) Maria Alessandra Santucci et al. INVESTIGATIONAL NEW DRUGS
- Effects of the Src kinase inhibitor saracatinib (AZD0530) on bone turnover in healthy men: A randomized, double-blind, placebo-controlled, multiple-ascending-dose phase I trial
- (2009) Rosemary A Hannon et al. JOURNAL OF BONE AND MINERAL RESEARCH
- Inhibition of Src with AZD0530 Reveals the Src-Focal Adhesion Kinase Complex as a Novel Therapeutic Target in Papillary and Anaplastic Thyroid Cancer
- (2009) Rebecca E. Schweppe et al. JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM
- Dasatinib in the Treatment of Chronic Myeloid Leukemia in Accelerated Phase After Imatinib Failure: The START A Trial
- (2009) Jane F. Apperley et al. JOURNAL OF CLINICAL ONCOLOGY
- Results of Dasatinib Therapy in Patients With Early Chronic-Phase Chronic Myeloid Leukemia
- (2009) Jorge E. Cortes et al. JOURNAL OF CLINICAL ONCOLOGY
- 9-(Arenethenyl)purines as Dual Src/Abl Kinase Inhibitors Targeting the Inactive Conformation: Design, Synthesis, and Biological Evaluation
- (2009) Wei-Sheng Huang et al. JOURNAL OF MEDICINAL CHEMISTRY
- Through the “Gatekeeper Door”: Exploiting the Active Kinase Conformation
- (2009) Fabio Zuccotto et al. JOURNAL OF MEDICINAL CHEMISTRY
- A Chemical Genetic Method for Generating Bivalent Inhibitors of Protein Kinases
- (2009) Zachary B. Hill et al. JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
- Activity of FB2, a novel dual Abl/Src tyrosine kinase inhibitor, against imatinib-resistant chronic myeloid leukemiain vivoandin vitro
- (2009) He Liu et al. LEUKEMIA & LYMPHOMA
- New insights into small-molecule inhibitors of Bcr-Abl
- (2009) S. Schenone et al. MEDICINAL RESEARCH REVIEWS
- The Src Inhibitor AZD0530 Reversibly Inhibits the Formation and Activity of Human Osteoclasts
- (2009) T. J. de Vries et al. MOLECULAR CANCER RESEARCH
- A Conserved Salt Bridge in the G Loop of Multiple Protein Kinases Is Important for Catalysis and for In Vivo Lyn Function
- (2009) Rina Barouch-Bentov et al. MOLECULAR CELL
- Preclinical anticancer activity of the potent, oral Src inhibitor AZD0530
- (2009) Tim P. Green et al. Molecular Oncology
- Novel N9-arenethenyl purines as potent dual Src/Abl tyrosine kinase inhibitors
- (2008) Yihan Wang et al. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
- Src as a therapeutic target in men with prostate cancer and bone metastases
- (2008) Fred Saad BJU INTERNATIONAL
- Dasatinib crosses the blood-brain barrier and is an efficient therapy for central nervous system Philadelphia chromosome-positive leukemia
- (2008) K. Porkka et al. BLOOD
- Dual targeting of Src and ER prevents acquired antihormone resistance in breast cancer cells
- (2008) S. Hiscox et al. BREAST CANCER RESEARCH AND TREATMENT
- Effects of Dasatinib on Src Kinase Activity and Downstream Intracellular Signaling in Primitive Chronic Myelogenous Leukemia Hematopoietic Cells
- (2008) H. Konig et al. CANCER RESEARCH
- C6-Unsubstituted Pyrazolo[3,4-d]pyrimidines Are Dual Src/Abl Inhibitors Effective against Imatinib Mesylate Resistant Chronic Myeloid Leukemia Cell Lines
- (2008) Maria Alessandra Santucci et al. ChemMedChem
- Small Molecules ATP-Competitive Inhibitors of FLT3: A Chemical Overview
- (2008) S. Schenone et al. CURRENT MEDICINAL CHEMISTRY
- Intermittent Target Inhibition With Dasatinib 100 mg Once Daily Preserves Efficacy and Improves Tolerability in Imatinib-Resistant and -Intolerant Chronic-Phase Chronic Myeloid Leukemia
- (2008) Neil P. Shah et al. JOURNAL OF CLINICAL ONCOLOGY
- Structure-Based Optimization of Pyrazolo[3,4-d]pyrimidines as Abl Inhibitors and Antiproliferative Agents toward Human Leukemia Cell Lines
- (2008) Fabrizio Manetti et al. JOURNAL OF MEDICINAL CHEMISTRY
- Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530
- (2008) Y-M Chang et al. ONCOGENE
Publish scientific posters with Peeref
Peeref publishes scientific posters from all research disciplines. Our Diamond Open Access policy means free access to content and no publication fees for authors.
Learn MoreBecome a Peeref-certified reviewer
The Peeref Institute provides free reviewer training that teaches the core competencies of the academic peer review process.
Get Started