DT2216—a Bcl-xL-specific degrader is highly active against Bcl-xL-dependent T cell lymphomas

Background Patients with advanced T cell lymphomas (TCLs) have limited therapeutic options and poor outcomes in part because their TCLs evade apoptosis through upregulation of anti-apoptotic Bcl-2 proteins. Subsets of TCL cell lines, patient-derived xenografts (PDXs), and primary patient samples dep...

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Bibliographic Details
Published in:	Journal of hematology and oncology Vol. 13; no. 1; pp. 95 - 13
Main Authors:	He, Yonghan, Koch, Raphael, Budamagunta, Vivekananda, Zhang, Peiyi, Zhang, Xuan, Khan, Sajid, Thummuri, Dinesh, Ortiz, Yuma T., Zhang, Xin, Lv, Dongwen, Wiegand, Janet S., Li, Wen, Palmer, Adam C., Zheng, Guangrong, Weinstock, David M., Zhou, Daohong
Format:	Journal Article
Language:	English
Published:	London BioMed Central 16.07.2020 BioMed Central Ltd Springer Nature B.V BMC
Subjects:	Aniline Compounds - therapeutic use Aniline Compounds - toxicity Animals Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Antineoplastic Agents - toxicity Antineoplastic Combined Chemotherapy Protocols - therapeutic use Antitumor agents Apoptosis Bcl-2 protein Bcl-x protein bcl-X Protein - antagonists & inhibitors bcl-X Protein - metabolism Bcl-xL Biotechnology Blood Platelets - drug effects Bridged Bicyclo Compounds, Heterocyclic - therapeutic use Cancer Research Cell Line, Tumor Comparative analysis Drug Design Drug Screening Assays, Antitumor Drug Synergism Female Flow cytometry Graft Survival Hematology Humans Immunoblotting Ligases Liver - pathology Lymphocytes T Lymphoma Lymphoma, T-Cell - drug therapy Lymphoma, T-Cell - metabolism Medical prognosis Medicine Medicine & Public Health Mice Mice, Inbred NOD Mice, SCID Neoplasia Neoplasm Proteins - antagonists & inhibitors Neoplasm Proteins - metabolism Neoplasm Transplantation Non-Hodgkin's lymphomas Oncology Patient-derived xenograft Patients Piperazines PROTAC Proteins Proteolysis Proto-Oncogene Proteins c-bcl-2 - antagonists & inhibitors Random Allocation Spleen - pathology Sulfonamides - therapeutic use Sulfonamides - toxicity T cell lymphoma T cells Thrombocytopenia Toxicity Tumors Ubiquitin-protein ligase Ubiquitin-Protein Ligases - chemistry VHL VHL protein Vincristine Xenograft Model Antitumor Assays Xenografts St Louis Missouri United States > US Bcl-xL VHL PROTAC T cell lymphoma Patient-derived xenograft
ISSN:	1756-8722, 1756-8722
Online Access:	Get full text
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