Niklas Dienstbier
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View article: Identification of non-charged 7.44 analogs interacting with the NHR2 domain of RUNX1-ETO with improved antiproliferative effect in RUNX-ETO positive cells
Identification of non-charged 7.44 analogs interacting with the NHR2 domain of RUNX1-ETO with improved antiproliferative effect in RUNX-ETO positive cells Open
View article: Small-molecule inhibitor of C-terminal HSP90 dimerization modulates autophagy and functions synergistically with mTOR inhibition to kill cisplatin-resistant cancer cells
Small-molecule inhibitor of C-terminal HSP90 dimerization modulates autophagy and functions synergistically with mTOR inhibition to kill cisplatin-resistant cancer cells Open
Background A major obstacle for the successful treatment of cancer is the primary presence or development of resistance mechanisms toward therapeutic intervention. In urothelial cancer, cisplatin-based regimens are still routinely employed…
View article: Identification of non-charged 7.44 analogs interacting with the NHR2 domain of RUNX1-ETO and exhibiting an improved, selective antiproliferative effect in RUNX-ETO positive cells
Identification of non-charged 7.44 analogs interacting with the NHR2 domain of RUNX1-ETO and exhibiting an improved, selective antiproliferative effect in RUNX-ETO positive cells Open
The RUNX1/ETO fusion protein is a chimeric transcription factor in acute myeloid leukemia (AML) created by chromosomal translocation t(8;21)(q22;q22). t(8;21) abnormality is associated with 12% of de novo AML cases and up to 40% in the AML…
View article: Co-targeting HSP90 alpha and CDK7 overcomes resistance against HSP90 inhibitors in BCR-ABL1+ leukemia cells
Co-targeting HSP90 alpha and CDK7 overcomes resistance against HSP90 inhibitors in BCR-ABL1+ leukemia cells Open
View article: Development of the first geldanamycin-based HSP90 degraders
Development of the first geldanamycin-based HSP90 degraders Open
Despite the early clinical promise, adverse events such as acquired resistance and dose-limiting toxicities have barred the widespread use of HSP90 inhibitors as anticancer drugs. A new approach involving proteolysis-targeting chimeras (PR…
View article: Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity
Solid-Phase Synthesis of Cereblon-Recruiting Selective Histone Deacetylase 6 Degraders (HDAC6 PROTACs) with Antileukemic Activity Open
In this work, we utilized the proteolysis targeting chimera (PROTAC) technology to achieve the chemical knock-down of histone deacetylase 6 (HDAC6). Two series of cereblon-recruiting PROTACs were synthesized via a solid-phase parallel synt…
View article: Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activity
Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activity Open
In this work, we utilized the proteolysis targeting chimera (PROTAC) technology to achieve the chemical knock-down of histone deacetylase 6 (HDAC6). Two series of cereblon-recruiting PROTACs were synthesized via a solid-phase parallel synt…
View article: Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activity
Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activity Open
In this work, we utilized the proteolysis targeting chimera (PROTAC) technology to achieve the chemical knock-down of histone deacetylase 6 (HDAC6). Two series of cereblon-recruiting PROTACs were synthesized via a solid-phase parallel synt…
View article: S153: DECRYPTING THE ROLE OF HSP90Α AND Β ISOFORMS TO OVERCOME RESISTANCE IN BCR-ABL1 LEUKEMIA
S153: DECRYPTING THE ROLE OF HSP90Α AND Β ISOFORMS TO OVERCOME RESISTANCE IN BCR-ABL1 LEUKEMIA Open
Background: The BCR-ABL1 fusion protein, which results from the chromosomal translocation t(9;22)(q34;q11) is detected in over 95% of CML, 25% of adult BCP-ALL and 3-5% of childhood BCP-ALL patients. The development of tyrosine kinase inhi…
View article: Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activity
Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activity Open
Selective histone deacetylase 6 (HDAC6) inhibitors are useful tools to study the function of the second catalytic domain of HDAC6, but they cannot interfere with (non)-enzymatic functions of HDAC6, which are mediated via the first catalyti…
View article: Development of a First-in-Class Small-Molecule Inhibitor of the C-Terminal Hsp90 Dimerization
Development of a First-in-Class Small-Molecule Inhibitor of the C-Terminal Hsp90 Dimerization Open
Heat shock proteins 90 (Hsp90) are promising therapeutic targets due to their involvement in stabilizing several aberrantly expressed oncoproteins. In cancerous cells, Hsp90 expression is elevated, thereby exerting antiapoptotic effects, w…
View article: Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activity
Solid-phase synthesis of cereblon-recruiting selective histone deacetylase 6 degraders (HDAC6 PROTACs) with anti-leukemic activity Open
Selective histone deacetylase 6 (HDAC6) inhibitors are useful tools to study the function of the second catalytic domain of HDAC6, but they cannot interfere with (non)-enzymatic functions of HDAC6, which are mediated via the first catalyti…
View article: Development of a First-in-Class Small Molecule Inhibitor of the C-terminal Hsp90 Dimerization
Development of a First-in-Class Small Molecule Inhibitor of the C-terminal Hsp90 Dimerization Open
Heat shock protein 90 (Hsp90) is a promising therapeutic target due to its involvement in stabilizing several aberrantly expressed oncoproteins. In cancerous cells, Hsp90 expression is elevated, thereby contributing in exerting anti-apopto…
View article: PB1648 THE CLINICAL RELEVANCE OF INDIRECT MYC INHIBITORS FOR PERSONALIZED T‐ALL TREATMENT
PB1648 THE CLINICAL RELEVANCE OF INDIRECT MYC INHIBITORS FOR PERSONALIZED T‐ALL TREATMENT Open
Background: Therapy refractory and relapsed T cell lymphoblastic leukemia (T‐ALL) is still one of the most common reasons for cancer related death in children. The current therapy option is stem cell transplantation, which is associated wi…