A5000154659- Ubiquitin and proteasome pathways
- ATP Synthase and ATPases Research
- Lysosomal Storage Disorders Research
- Glycosylation and Glycoproteins Research
- Cytokine Signaling Pathways and Interactions
- Carbohydrate Chemistry and Synthesis
- Biochemical and Molecular Research
- Chronic Myeloid Leukemia Treatments
- Chronic Lymphocytic Leukemia Research
- Protein Degradation and Inhibitors
- Multiple Myeloma Research and Treatments
- interferon and immune responses
- Synthesis and biological activity
- Eosinophilic Disorders and Syndromes
- RNA and protein synthesis mechanisms
- HER2/EGFR in Cancer Research
- Quinazolinone synthesis and applications
- Cancer, Hypoxia, and Metabolism
- Histone Deacetylase Inhibitors Research
- Immune Cell Function and Interaction
- Galectins and Cancer Biology
- Myeloproliferative Neoplasms: Diagnosis and Treatment
- Cancer Mechanisms and Therapy
- 14-3-3 protein interactions
- Endoplasmic Reticulum Stress and Disease
University of Lausanne
2011-2018
University of Michigan
2008-2014
The University of Texas Health Science Center at Houston
2011
The University of Texas MD Anderson Cancer Center
2005-2009
All India Institute of Medical Sciences
2006-2009
Department of Biotechnology
2009
TherapeuticsMD (United States)
2005-2006
Abstract Recent evidence suggests that several deubiquitinases (DUB) are overexpressed or activated in tumor cells and many contribute to the transformed phenotype. Agents with DUB inhibitory activity may therefore have therapeutic value. In this study, we describe mechanism of action WP1130, a small molecule derived from compound Janus-activated kinase 2 (JAK2) activity. WP1130 induces rapid accumulation polyubiquitinated (K48/K63-linked) proteins into juxtanuclear aggresomes, without...
Dual-Duty Active Site O-linked N-acetylglucosamine transferase (OGT) catalyzes the addition of (GlcNac) to serine or threonine residues, influencing localization and function proteins. Because its activity is sensitive nutrient uridine diphosphate (UDP)–GlcNac, OGT has been proposed regulate cellular responses status. Recently, in presence UDP-GlcNac was shown cleave host cell factor–1 (HCF-1), a transcriptional coregulator human cell-cycle progression. This cleavage required for HCF-1...
O-linked N -acetylglucosamine (O-GlcNAc) is an essential and dynamic post-translational modification found on hundreds of nucleocytoplasmic proteins in metazoa. Although a single enzyme, O-GlcNAc transferase (OGT), generates the entire cytosolic proteome, it not understood how recognizes its protein substrates, targeting only fraction serines/threonines metazoan proteome for glycosylation. We describe trapped complex human OGT with C-terminal domain TAB1, key innate immunity-signalling...
In complex with the cosubstrate UDP- N -acetylglucosamine (UDP-GlcNAc), O- linked-GlcNAc transferase (OGT) catalyzes Ser/Thr O -GlcNAcylation of many cellular proteins and proteolysis transcriptional coregulator HCF-1. Such a dual glycosyltransferase–protease activity, which occurs in same active site, is unprecedented integrates both reversible irreversible forms protein post-translational modification within one enzyme. Although occurring we show here that glycosylation occur through...
Human HCF-1 (also referred to as HCFC-1) is a transcriptional co-regulator that undergoes complex maturation process involving extensive O-GlcNAcylation and site-specific proteolysis. proteolysis results in two active, noncovalently associated HCF-1N HCF-1C subunits regulate distinct phases of the cell-division cycle. are both catalyzed by O-GlcNAc transferase (OGT), which thus displays an unusual dual enzymatic activity. OGT cleaves at six highly conserved 26 amino acid repeat sequences...
Polymorphisms in the TNF-α and TNF receptor type 2 (TNFR2) genes Asian Indians are not well understood. We investigated single nucleotide polymorphisms 5′-flanking promoter/enhancer region exons 6, 9 10 of TNFR2 gene by PCR-restriction length polymorphism (PCR-RFLP) PCR-sequence specific primer (SSP) techniques, respectively. The results showed bi-allelic (−308G > A) 6 (676 T G) (1176 G A). Additionally, three (1663 A, 1668G 1690C T) were observed exon gene. distribution polymorphic alleles...
Macrophages are key mediators of antimicrobial defense and innate immunity. Innate intracellular mechanisms can be rapidly regulated at the posttranslational level by coordinated addition removal ubiquitin ligases deubiquitinases (DUBs). While have been extensively studied, contribution DUBs to macrophage immune function is incompletely defined. We therefore employed a small molecule DUB inhibitor, WP1130, probe role in response bacterial infection. Treatment activated bone marrow-derived...
Supplementary Figure 4 from Deubiquitinase Inhibition by Small-Molecule WP1130 Triggers Aggresome Formation and Tumor Cell Apoptosis
Supplementary Figure 7 from Deubiquitinase Inhibition by Small-Molecule WP1130 Triggers Aggresome Formation and Tumor Cell Apoptosis