WO WO2018129533A1
· 2018
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Yang et al., “Development of the first small molecular histone deacetylase 6 degraders”, Bioorg Med Chem Lett, Aug. 1, 2018 (Year: 2018).
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Yang et al., “Development of the first small molecular histone deacetylase 6 degraders”, Bioorg Med Chem Lett, May 30, 2018 (Year: 218).
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An et al. “Developing Potent PROTACs Tools for Selective Degradation of HDAC6 Protein”
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Bassi et al. “Modulating PCAF/GCN5 Immune Cell Function through a PROTAC Approach”
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Batchu et al. “The Therapeutic Hope for Hdac6 Inhibitors in Malignancy and Chronic Disease”
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Bergman et al. “Selective Histone Deacetylase 6 Inhibitors Bearing Substituted Urea Linkers Inhibit Melanoma Cell Growth”
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Bondeson et al. “Catalytic in Vivo Protein Knockdown by Small-Molecule Protacs”
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Bondeson et al. “Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead”
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Bradbury et al. “Histone Deacetylases in Acute Myeloid Leukaemia Show a Distinctive Pattern of Expression That Changes Selectively in Response to Deacetylase Inhibitors”
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Bradner et al. “Chemical Phylogenetics of Histone Deacetylases”
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Buckley et al. Small-Molecule Control of Intracellular Protein Levels through Modulation of the Ubiquitin Proteasome System. Angew. Chemie—Int. Ed. 2014, 53 (9), 2312-2330.
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Burslem et al. “The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study”
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Chamberlain et al. “Structure of the Human Cereblon-DDB1-Lenalidomide Complex Reveals Basis for Responsiveness to Thalidomide Analogs”
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Cosenza et al. “Ricolinostate (Acy-1215), a Selective HDAC6 Inhibitor, Alone and in Combination with Bendamustine Is Effective in Preclinical Studies in Lymphoma Cell Lines”
[cited by applicant]
Cosenza et al., Ricolinostate, a selective HGAC6 inhibitor, shows anti-lymphoma cell activity alone and in combination with bendamustine,
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De Vreese et al. “Synthesis and SAR Assessment of Novel Tubathian Analogs in the Pursuit of Potent and Selective Hdac6 Inhibitors”
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De Vreese et al. “Synthesis of Potent and Selective HDAC6 Inhibitors Bearing a Cyclohexane- or Cycloheptane-Annulated 1,5-Benzothiazepine Scaffold”
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Demizu et al. “Design and Synthesis of Estrogen Receptor Degradation Inducer Based on a Protein Knockdown Strategy”
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Douglass et al.. “A Comprehensive Mathematical Model for Three-Body Binding Equilibria”
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Erb et al. “Transcription Control by the ENL Yeats Domain in Acute Leukaemia”
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Falkenberg et al. “Histone Deacetylases and Their Inhibitors in Cancer, Neurological Diseases and Immune Disorders”
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Fass et al. “Crebinostat: A Novel Cognitive Enhancer That Inhibits Histone Deacetylase Activity and Modulates Chromatin-Mediated Neuroplasticity”
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Fischer et al. “Structure of the DDB1-CRBN E3 Ubiquitin Ligase in Complex with Thalidomide”
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Gadd et al. “Structural Basis of PROTAC Cooperative Recognition for Selective Protein Degradation”
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Goracci et al. “A Rational Approach for the Identification of Non-Hydroxamate HDAC6-Selective Inhibitors”
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Handbook of Pharmaceutical Manufacturing Formulations, 2
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P. Heinrich Stahl and Camille G. Wermuth, Eds. “Handbook of Pharmaceutical Salts: Properties, Selection, and Use; 2nd Revised Edition,” © 2011, Wiley-VCH (Hoboken, NJ), ISBN 978-3906390512.
[cited by applicant]
Hideshima et al. “Rational Combination Treatment with Histone Deacetylase Inhibitors and Immunomodulatory Drugs in Multiple Myeloma”
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Hideshima et al. “Discovery of Selective Small-Molecule HDAC6 Inhibitor for Overcoming Proteasome Inhibitor Resistance in Multiple Myeloma”
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Ito et al. “Identification of a Primary Target of Thalidomide Teratogenicity”
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Jang et al. “Novel Analogs Targeting Histone Deacetylase Suppress Aggressive Thyroid Cancer Cell Growth and Induce Re-Differentiation”
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Jaskula-Sztul et al. “Tumor-Suppressor Role of Notch3 in Medullary Thyroid Carcinoma Revealed by Genetic and Pharmacological Induction”
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Johnstone, R. W. “Histone-Deacetylase Inhibitors: Novel Drugs for the Treatment of Cancer”
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Kalin et al. “Development and Therapeutic Implications of Selective Histone Deacetylase 6 Inhibitors”
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Kronke et al. “Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells”
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Lai et al. “Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL”
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Lai et al. “Induced Protein Degradation: An Emerging Drug Discovery Paradigm”
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Li et al., Histone deacetylase 6 in cancer,
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Li et al. “Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression”
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Lin et al. “Design and Synthesis of Orally Bioavailable Aminopyrrolidinone Histone Deacetylase 6 Inhibitors”
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Livak et al. “Analysis of Relative Gene Expression Data Using Real-Time Quantitative PCR and the 2-
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Lu et al. “The Myeloma Drug Lenalidomide Promotes the Cereblon-Dependent Destruction of Ikaros Proteins”
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Lu et al. “Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4”
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Matyskiela et al. “A Novel Cereblon Modulator Recruits GSPT1 to the CRL4
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Miyake et al. “Structural Insights into HDAC6 Tubulin Deacetylation and Its Selective Inhibition”
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Nabet et al. “The dTAG System for Immediate and Target-Specific Protein Degradation”
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Niesvizky et al. “Selective HDAC6 Inhibitor ACY-241, an Oral Tablet, Combined with Pomalidomide and Dexamethasone: Safety and Efficacy of Escalation and Expansion Cohorts in Patients with Relapsed or Relapsed-and-Refrac…
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Olson et al. “Pharmacological Perturbation of CDK9 Using Selective CDK9 Inhibition or Degradation”
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Ottis et al. “Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy”
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Papadas A., Asimakopoulos F. (2017) “Mechanisms of Resistance in Multiple Myeloma.” In: Mandalà M., Romano E. (eds) Mechanisms of Drug Resistance in Cancer Therapy. Handbook of Experimental Pharmacology, vol. 249. © 201…
[cited by applicant]
Qin et al. “Discovery of QCA570 as an Exceptionally Potent and Efficacious Proteolysis Targeting Chimera (PROTAC) Degrader of the Bromodomain and Extra-Terminal (BET) Proteins Capable of Inducing Complete and Durable Tu…
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Raina et al. “Protac-Induced Bet Protein Degradation as a Therapy for Castration-Resistant Prostate Cancer”
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Ray et al. “Combination of a Novel HDAC6 Inhibitor ACY-241 and Anti-PD-L1 Antibody Enhances Anti-Tumor Immunity and Cytotoxicity in Multiple Myeloma”
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Remillard et al. “Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands”
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Sakamoto et al. “Protacs: Chimeric Molecules That Target Proteins to the Skp1-Cullin-F Box Complex for Ubiquitination and Degradation”
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Santo et al. “Preclinical Activity, Pharmacodynamic, and Pharmacokinetic Properties of a Selective HDAC6 Inhibitor, ACY-1215, in Combination with Bortezomib in Multiple Myeloma”
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Schiedel et al. “Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals)”
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Senger et al. “Synthesis and Biological Investigation of Oxazole Hydroxamates as Highly Selective Histone Deacetylase 6 (Hdac6) Inhibitors”
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Shen, et al. “Bicyclic-Capped Histone Deacetylase 6 Inhibitors with Improved Activity in a Model of Axonal Charcot-Marie-Tooth Disease”
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Tahtouh et al. “Selectivity Cocrystal Structures, and Neuroprotective Properties of Leucettines, a Family of Protein Kinase Inhibitors Derived from the Marine Sponge Alkaloid Leucettamine” B,
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Tang et al. “Discovery of Histone Deacetylase 8 Selective Inhibitors”
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Wang et al. “Boiling Water-Catalyzed Neutral and Selective N-Boc Deprotection”
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Winter et al. “Phthalimide Conjugation as a Strategy for in Vivo Target Protein Degradation”
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Wu et al., Development of Multifunctional Histone Deacetylase 6 Degraders with Potent Antimyeloma Activity,
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Yang et al. “Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer”
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Yang et al. “Development of the First Small Molecule Histone Deacetylase 6 (HDAC6) Degraders”
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Yee et al. “Ricolinostat (Acy-1215), the First Selective HDAC6 Inhibitor, in Combination with Lenalidomide and Dexamethasone in Patients with Relapsed and Relapsed -and Refractory Multiple Myeloma: Phase 1b Results (Ace…
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Zengerle et al. “Selective Small Molecule Induced Degradation of the Bet Bromodomain Protein BRD4”
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Zhang et al. “Degradation of Target Protein in Living Cells by Small-Molecule Proteolysis Inducer”
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Zhang et al. “Mice Lacking Histone Deacetylase 6 Have Hyperacetylated Tubulin but Are Viable and Develop Normally”
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Zhou et al. “Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression”
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