Publikacje
- Wszystkie
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- Wszystkie
- Synthetic Lethality
- SEL24
- RVU120
- Wszystkie
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- Wszystkie
- MEN1703 (SEL24)
- Novel Targets
- WRN
- PRMT5
- CDK8/CDK19
- HPK1
- SMARCA
- MNK
- GCN2
- SHMT
- STING
- A2A/A2B
- CDK8
- PIM/FLT3
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American Association for Cancer Research (AACR) Annual Meeting, April 5-10, 2024
Discovery of novel MTA-cooperative PRMT5 inhibitors as targeted therapeutics for MTAP-deleted cancers
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Discovery of WRN inhibitors as targeted therapy in the treatment of microsatellite unstable (MSI-H) tumors
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A Comprehensive Platform for Identification of KRAS-specific Synthetic Lethal Targets using Patient-Derived Cells
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MEN1703/SEL24 exhibits promising antitumoral activity in preclinical models of myelofibrosis both as a single agent and combined with ruxolitinib.
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Combination JAK1/2 and CDK8/19 inhibition demonstrates enhanced efficacy in myeloproliferative neoplasms.
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American Society of Hematology (ASH) Annual Meeting, December 9 –12, 2023
Safety and Efficacy Results from CLI120-001 a Phase 1 Study in RR-AML and HRMDS: Update from Higher Dose Levels
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Preclinical and Clinical Evidence for Erythroid-Stimulating Activity of RVU120 CDK8/19 Inhibitor in AML and MDS
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Novel Clinically Useful Inhibitor of Mediator Complex, RVU120, Relieves Differentiation Block in MDS/AML
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Targeting CDK8/CDK19 to Disrupt Leukemic Stem Cell-like Population in Acute Myeloid Leukemia: Exploring RVU120 As a Promising Frontline Therapy
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Mediator Kinase/CDK8 Inhibition as a Strategy to Improve FLT3 Inhibitor Activity in Acute Myeloid Leukemia
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San Antonio Breast Cancer Symposium (SABCS), December 5-9, 2023
Synergistic Activity of CDK8/19 Inhibitor RVU120 and MEK Inhibitors in Hormone-Negative Breast Cancer: Implications for Targeted Therapy
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European Society for Medical Oncology (ESMO) Congress 2023, October 20-24, 2023
Phase I/II trial of RVU120, a CDK8/CDK19 inhibitor, in patients with relapsed/refractory metastatic or advanced solid tumors
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AACR-NCI-EORTC International Conference (ENA) 2023, October 11-15, 2023
Discovery of Novel MTA-cooperative PRMT5 Inhibitors as Targeted Therapeutics for MTAP-deleted Cancers
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Comprehensive Platform for Unraveling the Molecular Mechanisms and Vulnerabilities of Colorectal Cancer: A Step Forward in Target Discovery
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MEN1703/SEL24, A Potent PIM Inhibitor, Demonstrates Promising Anti-Tumor Activity in Activated B Cell Like DLBCL, Mantle Cell Lymphoma and Marginal Zone Lymphoma Cells
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Congress of the Polish Society of Hematology and Transfusion Medicine, September 14-16, 2023
Safety and Efficacy Update from CLI120–001: a Phase 1b Dose Escalation Study in Relapse-Refractory Acute Myeloid Leukemia and High-Risk Myelodysplasia
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RVU120 CDK8/19 Inhibitor Promotes Erythroid Differentiation in AML and HR-MDS Patients
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European Hematology Association (EHA) Hybrid Congress, June 8-11, 2023
Safety and efficacy update from CLI120-001: a Phase 1b dose-escalation study in relapse/refractory AML and HR-MDS
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Combination JAK1/2 and CDK8/19 inhibition demonstrates enhanced efficacy in myeloproliferative neoplasms
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American Association for Cancer Research (AACR) Annual Meeting, April 14-19, 2023
Discovery of novel MTA-cooperative PRMT5 inhibitors as targeted therapeutics for MTAP-deleted cancers
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American Society of Hematology (ASH) Annual Meeting, December 10 –13, 2022
CDK8/19 Kinase Inhibitor RVU120 in Patients with AML or Higher-Risk MDS: Safety and Efficacy Results from New Dose Escalation Cohorts
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Multiomics Analysis Confirms Effective Target Engagement for RVU120 – a First-in-class CDK8/19 Kinase Inhibitor in AML and MR-MDS Patients and Reveals the Mechanism of Action
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PIM Inhibition by SEL24 (MEN1703) Combines Synergistically with gilteritinib in FLT3-ITD Preclinical Models of Acute Myeloid Leukemia
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Super-enhancer-driven PIM Kinase Upregulation in Multiple Myeloma Maintains the Plasma Cell-specific Oncogenic and Microenvironmental Circuits and Can Be Efficiently Targeted by the Pan-PIM Inhibitor MEN1703
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PIM Kinases Regulate Super-Enhancer-Dependent Gene Expression In Diffuse Large B-Cell Lymphoma
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MEN1703-mediated PIM kinases inhibition impairs protumoral and immunosuppressive phenotype and functions of macrophages in classical Hodgkin Lymphoma
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EORTC-NCI-AACR Symposium (ENA), October 26-28, 2022
Phase I/II trial of RVU120, a CDK8/CDK19 inhibitor in patients with relapsed/refractory metastatic or advanced solid tumors
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RVU120, a small molecule inhibitor of CDK8/19 kinases, enhances rituximab-driven NK cells-mediated cytotoxicity both in vitro and in vivo
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Discovery of novel MTA-cooperative PRMT5 inhibitors as targeted therapeutics for MTAP deleted cancers
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European Hematology Association (EHA) Hybrid Congress, June 9-17, 2022
CLI120-001 Phase1b Dose Escalation Study of RVU120 in Patients with AML or High-Risk MDS Safety and Efficacy Data Update
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Preclinical and Clinical Signs of RVU120 efficacy, a Specific CDK8/19 Inhibitor in DNMT3A and NPM1 Mutation Positive AML and HR-MDS
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Phase 1/2 Study of SEL24/MEN1703, a First-In-Class Dual PIM/FLT3 Kinase Inhibitor, in Patients with IDH1/2-Mutated Acute Myeloid Leukemia: the DIAMOND-01 Trial
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American Society of Clinical Oncology (ASCO) Annual Meeting, June 3-7, 2022
Phase 1/2 study of SEL24/MEN1703, a first-in-class dual PIM/FLT3 kinase inhibitor, in patients with IDH1/2-mutated acute myeloid leukemia: the DIAMOND-01 trial
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Phase I/II trial of RVU120 (SEL120), a CDK8/CDK19 inhibitor in patients with relapsed/refractory metastatic or advanced solid tumors
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American Association for Cancer Research (AACR) Annual Meeting, April 8-13, 2022
"RVU120, a selective CDK8/CDK19 inhibitor, demonstrates efficacy against hormone-independent breast cancer cells in vitro and in vivo"
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"Discovery of novel MTA-cooperative PRMT5 inhibitors as a targeted therapeutic for MTAP deleted cancers"
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"RVU120 SOL-021: An open-label, single agent, Phase I/II trial of RVU120 (SEL120) in patients with relapsed/refractory metastatic or advanced solid tumors"
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63rd American Society of Hematology (ASH) Annual Meeting & Exposition, December 11 – 14, 2021
"CLI120-001 Phase Ib Study of RVU120 (SEL120) in Patients with AML and High-Risk MDS: Updated Safety/Efficacy Results from Initial Dose Escalation"
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"RVU120 – a CDK8/19 Inhibitor for the Treatment of AML and HR-MDS Can Induce Erythroid Differentiation"
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"Inhibition of Cyclin Dependent Kinase 8 (CDK8): A Novel Approach to Target the Leukemia Initiating Cells (LICs) in T-Cell Acute Lymphoblastic Leukemia (T-ALL)"
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"Preclinical and Clinical Signs of Efficacy of RVU120 (SEL120), a Specific CDK8/19 Inhibitor in DNMT3A-Mutated AML"
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"SEL24(MEN1703) Inhibits PIM/FLT3 Downstream Target in Acute Myeloid Leukemia (AML) Patients: Results of the Pharmacodynamics (PD) Assay and Genomic Profiling in the First-in-Human Diamond-01 Trial"
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44th Annual San Antonio Breast Cancer Symposium (SABCS), December 7-10, 2021
"Selective CDK8/CDK19 inhibitor RVU120 demonstrates efficacy against hormone-independent breast cancer cells in vitro and in vivo"
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Society for Immunotherapy of Cancer’s (SITC) 36th Anniversary Annual Meeting, November 11-14, 2021
"Novel, orally administered HPK1 inhibitors demonstrate anti-tumor efficacy and enhanced immune response"
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"Characterization of RVU-27065 a novel small-molecule STING agonist suitable for systemic administration"
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Discovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology
Heinrich T, Sala-Hojman A, Ferretti R, Petersson C, Minguzzi S, Gondela A, Ramaswamy S, Bartosik A et al. Discovery of 5-{2-[5-Chloro-2-(5-ethoxyquinoline-8-sulfonamido)phenyl]ethynyl}-4-methoxypyridine-2-carboxylic Acid, a Highly Selective in Vivo Useable Chemical Probe to Dissect MCT4 Biology. Journal of Medicinal Chemistry, August 2021
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Virtual 26th Annual European Hematology Association (EHA) Congress, June 9-17, 2021
"RVU120/SEL120 CDK8/19 inhibitor - a drug candidate for the treatment of MDS can induce erythroid differentiation in transformed CD34+ hematopoietic progenitor cells"
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"CLI120-001 Phase 1b Study of SEL120/RVU120 in patients with AML or High Risk MDS: Preliminary clinical and PK results from initial dose escalation cohorts"
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“Results from DIAMOND-01 (CLI24-001) TRIAL: First in Human Study of SEL24/MEN1703, a Dual PIM/FLT3 Kinase Inhibitor, in Patients with Acute Myeloid Leukemia”
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AACR Virtual Annual Meeting 2021, April 10-15 and May 17-21, 2021
"RVU120 (SEL120), a CDK8/CDK19 inhibitor, possesses strong multilineage differentiation potential in leukemic cells"
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"Development and characterization of small molecule HPK1 inhibitors"
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"New generation of STING agonists: development and characterization of a novel series of systemic immunomodulators with improved potency"
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62nd American Society of Hematology (ASH) Annual Meeting and Exposition, December 5-8, 2020
"SEL24/MEN1703 provides PIM/FLT3 Downstream Pathway Inhibition in Acute Myeloid Leukemia (AML) Blast Cells: Results of the Pharmacodynamic (PD) Assay in the Dose Escalation Part of First-in-Human DIAMOND-01 Trial"
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"PIM Kinase Inhibition Decreases the Proangiogenic Properties of Multiple Myeloma Cells and Affects the Metabolic State of the Vascular Endothelium"
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Society for Immunotherapy of Cancer’s (SITC) 35th Anniversary Annual Meeting, November 11-14, 2020
"Development of improved small molecule STING agonists suitable for systemic administration"
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AACR Virtual Annual Meeting II, June 22-24, 2020
"Synergistic effect of CDK8 and BCL-2 inhibition in AML through regulation of MCL-1 and BIM balance"
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"In vivo and in vitro characterization of RVU330 best-in-class dual A2A/A2B adenosine receptor antagonist"
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"Development of selective small molecule STING agonists suitable for systemic administration"
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"Development and characterization of small molecule HPK1 inhibitors"
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"Development of novel, selective SMARCA2 (BRM) degraders for treatment of SMARCA4 (BRG1) mutated tumors"
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Virtual 25th Annual European Hematology Association (EHA) Congress, June 11-21, 2020
“A First-in-human study of SEL120, a novel oral selective CDK8/19 inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome”
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"Results of the dose escalation part of DIAMOND trial (CLI24-001): first in human study of SEL24/MEN1703, a dual PIM/FLT3 kinase inhibitor, in Patients with Acute Myeloid Leukemia"
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Synthetically Lethal Interactions of Heme Oxygenase-1 and Fumarate Hydratase Genes
Podkalicka, P.; Mucha, O.; Kruczek, S.; Biela, A.; Andrysiak, K.; Stępniewski, J.; Mikulski, M.; Gałęzowski, M.; Sitarz, K.; Brzózka, K.; Józkowicz, A.; Dulak, J.; Łoboda, A. Synthetically Lethal Interactions of Heme Oxygenase-1 and Fumarate Hydratase Genes. Biomolecules 2020, 10, 143.
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61st American Society of Hematology (ASH) Annual Meeting, December 7-10, 2019, Orlando, FL, USA
"SEL120 – a First-in-Class CDK8/19 Inhibitor As a Novel Option for the Treatment of Acute Myeloid Leukemia and High-Risk Myelodysplastic Syndrome – Data from Preclinical Studies and Introduction to a Phase Ib Clinical Trial"
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"CDK8 Inhibitors Induce Transcriptional Reprogramming of AML Cells Associated with Differentiation"
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Society for Immunotherapy of Cancer 34th Annual Meeting (SITC 2019), November 6–10, National Harbor, MD, USA
"Novel dual A2A /A2B adenosine receptor antagonists for cancer immunotherapy in vitro characterization"
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"Development and characterization of next generation small molecule STING agonists"
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CICON 2019 – Translating Science into Survival – September 25-28, 2019, Paris, France
“Characterization of novel potent dual A2A/A2B adenosine receptor antagonists for cancer immunotherapy”
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24th Congress of EHA, June 13-16, 2019 Amsterdam, Netherlands
"CLI24-001: First-in-human study of SEL24/MEN1703, an oral dual PIM/FLT3 kinase inhibitor, in patients with acute myeloid leukemia"
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ASCO Annual Meeting 2019, May 31-June 4, Chicago, IL, USA
"CLI24-001: First-in-human study of SEL24/MEN1703, an oral dual PIM/FLT3 kinase inhibitor, in patients with acute myeloid leukemia"
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AACR Annual Meeting 2019, March 29- April 3, 2019, Atlanta, GA, USA
"SEL120, a Potent and Specific Inhibitor of CDK8 Induces Complete Remission in Human Patient Derived Xenograft Models of Acute Myeloid Leukemia (AML)"
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"Novel dual A2A /A2B adenosine receptor antagonists for cancer immunotherapy in vitro and in vivo characterization"
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"Discovery and characterization of next-generation small molecule direct STING agonists"
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American Society of Hematology (ASH) Annual Meeting, 1-4 December 2018, San Diego, CA, USA
"CDK8 Inhibitor SEL120-34A Has Therapeutic Efficacy in Murine and Human AML Models"
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EORTC-NCI-AACR Molecular Targets and Cancer Therapeutics Symposium, 13-16 November 2018, Dublin, Ireland
“SEL120−34A, a potent and specific inhibitor of CDK8, as a potential treatment of acute myeloid and lymphoblastic leukemias”
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Annual Meeting & Pre-Conference Programs of the Society for Immunotherapy of Cancer (SITC), 7-11 November 2018, Washington, DC, USA
"Novel class of small molecule direct STING agonists as a potential cancer immunotherapy"
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“Characterization of novel dual A2A/B adenosine receptor antagonists for cancer immunotherapy”
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Mechanisms to Therapies: Innovations in Cancer Metabolism, 9-11 October 2018, Bilbao, Spain
"Discovery of novel SHMT1/2 small molecule inhibitors for cancer treatment"
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Leukemia and Lymphoma – Europe and the USA Linking Knowledge and Practice, 3-5 October 2018, Dubrovnik, Croatia
“CDK8 inhibitor SEL120 targets AML by regulation of transcriptional programs involved in the maintenance of leukemia stem cells”
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Annual Immuno-Oncology Summit, 27-31 August 2018, Boston, MA, USA
"Discovery of novel small molecule STING agonists as a new cancer immunotherapy"
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“Characterization of novel dual A2A/B adenosine receptor antagonists for cancer immunotherapy”
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AACR Annual Meeting 2018, 14-18 April 2018, Chicago, IL, USA
"Characterization of novel dual A2A/A2B adenosine receptor antagonists for cancer immunotherapy"
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"CDK8 inhibitor SEL120-34A targets CD34 positive AML cells by regulation of transcriptional programs involved in the maintenance of leukemia stem cells"
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"Discovery of novel SHMT small molecule inhibitors for cancer treatment"
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AACR Annual Meeting 2017, 1 - 5 April 2017, Washington, DC, USA
"Development of small molecule selective inhibitors of GCN2 as an immunotherapy aimed at preventing immune escape of tumor cells"
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"Differential activity on lung adenocarcinoma cells with loss-of-function mutations of SWI/SNF protein SMARCA4"
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"Small molecule inhibitors of SHMT1/2 validate serine metabolism as a target in the treatment of c-Myc positive solid tumors"
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"Inhibition of CDK8 kinase with SEL120-34A allows for a personalized approach in AML"
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"Development of a potent, dual pan-PIM/FLT3 inhibitor for the treatment of heme malignancies"
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AACR Annual Meeting 2015, 18 – 22 April 2015 in Philadelphia, PA, USA:
“First-in-class dual PIM/FLT3 inhibitor SEL24-B489 for the treatment of hematological malignancies”
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“Selective CDK8 inhibitor SEL120-34A alters expression of interferon-related DNA damage resistance signature genes in colorectal cancer”
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AACR Annual Meeting 2014, 5-9 April 2014, San Diego, USA:
“Preclinical characterization of SEL24-B489, a dual PIM/FLT3 inhibitor for the treatment of hematological malignancies”
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“Repression of tumor survival pathways by novel, selective inhibitors of MNK1 and MNK2 kinases”
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