Chirality and asymmetry increase the potency of candidate ADRM1/RPN13 inhibitors

Bortezomib and the other licensed 20S proteasome inhibitors show robust activity against liquid tumors like multiple myeloma, but have disappointed against solid tumors including ovarian cancer. Consequently, interest is mounting in alternative non-peptide based drugs targeting the proteasome's...

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Veröffentlicht in:	PloS one 2021-09, Vol.16 (9), p.e0256937-e0256937
Hauptverfasser:	Anchoori, Ravi K, George, Logan, Tseng, Ssu-Hsueh, Lam, Brandon, Polkampally, Srinidhi, Amiano, Anjali D, Foran, Palmer, Tsingine, Hannah, Samanapally, Harideep, Carrizo Velasquez, Fernanda, Das, Samarjit, Xing, Deyin, Bin Salam, Ahmad, Karanam, Balasubramanyam, Hung, Chien-Fu, Roden, Richard B S
Format:	Artikel
Sprache:	eng
Schlagworte:	Analogs Analysis Anesthesiology Animals Annexin V Antibodies Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Apoptosis Apoptosis - drug effects Asymmetry Benzylidene Compounds - chemistry Benzylidene Compounds - pharmacology Binding Biology and Life Sciences Bioluminescence Biomarkers Bortezomib BRCA2 protein Breast cancer Cancer Cell Line, Tumor Cell Proliferation - drug effects Chemical bonds Chirality Cisplatin Clustering Critical care Cytotoxicity Deoxyribonucleic acid Depletion Depolarization DNA DNA damage DNA repair Doxorubicin Drug delivery Drug dosages Female Gene expression Glutathione Glycolysis Gynecological cancer Health aspects Humans Inhibitors Intracellular Signaling Peptides and Proteins - antagonists & inhibitors Lysates Medical research Medicine and Health Sciences Metabolism Mice Mice, Inbred C57BL Mice, Nude Mitochondria Molecular weight Multiple myeloma NMR Nuclear magnetic resonance Ovarian cancer Ovarian carcinoma Ovarian Neoplasms - drug therapy Oxidative stress Pathology Peptides Physical Sciences Proteasome inhibitors Proteins Research and Analysis Methods Solid tumors Toxicity Tumor cell lines Tumors Ubiquitin Ubiquitination Ubiquitination - drug effects
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