The HECT E3 Ligase E6AP/UBE3A as a Therapeutic Target in Cancer and Neurological Disorders

Fragment-based covalent ligand screening enables rapid discovery of inhibitors for the RBR E3 ubiquitin ligase HOIP

(2019) Henrik Johansson et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Molecular modeling simulation studies reveal new potential inhibitors against HPV E6 protein

(2019) Joel Ricci-López et al.   PLoS One

Covalent Ligand Screening Uncovers a RNF4 E3 Ligase Recruiter for Targeted Protein Degradation Applications

(2019) Carl C. Ward et al.   ACS Chemical Biology

E6AP goes viral: the role of E6AP in viral- and non-viral-related cancers

(2019) Ivona Bandilovska et al.   CARCINOGENESIS

Nano‐LC based proteomic approach identifies that E6AP interacts with ENO1 and targets it for degradation in breast cancer cells

(2019) Mukul Mishra et al.   IUBMB LIFE

Carfilzomib with immunomodulatory drugs for the treatment of newly diagnosed multiple myeloma

(2019) Ola Landgren et al.   LEUKEMIA

Loss of nuclear UBE3A causes electrophysiological and behavioral deficits in mice and is associated with Angelman syndrome

(2019) Rossella Avagliano Trezza et al.   NATURE NEUROSCIENCE

UBE3A-mediated PTPA ubiquitination and degradation regulate PP2A activity and dendritic spine morphology

(2019) Jie Wang et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A novel small-molecule inhibitor of the human papillomavirus E6-p53 interaction that reactivates p53 function and blocks cancer cells growth

(2019) Marta Celegato et al.   CANCER LETTERS

Targeting TRAF6 E3 ligase activity with a small molecule inhibitor combats autoimmunity

(2018) Jara Kerstin Brenke et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

3-Fluoro-4-hydroxyprolines: Synthesis, Conformational Analysis, and Stereoselective Recognition by the VHL E3 Ubiquitin Ligase for Targeted Protein Degradation

(2018) Andrea Testa et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Proteotranscriptomic Measurements of E6-Associated Protein (E6AP) Targets in DU145 Prostate Cancer Cells

(2018) Twishi Gulati et al.   MOLECULAR & CELLULAR PROTEOMICS

Arc ubiquitination in synaptic plasticity

(2018) Angela M. Mabb et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

UBE3A-mediated p18/LAMTOR1 ubiquitination and degradation regulate mTORC1 activity and synaptic plasticity

(2018) Jiandong Sun et al.   eLife

p53 and the Viral Connection: Back into the Future ‡

(2018) Ronit Aloni-Grinstein et al.   Cancers

Discovery of small molecule WWP2 ubiquitin ligase inhibitors

(2018) Andrew Chantry et al.   CHEMISTRY-A EUROPEAN JOURNAL

New Evidence of Mitochondria Dysfunction in the Female Alzheimer's Disease Brain: Deficiency of Estrogen Receptor-β

(2018) Jiangang Long et al.   JOURNAL OF ALZHEIMERS DISEASE

A cell-based high-throughput screening method based on a ubiquitin-reference technique for identifying modulators of E3 ligases

(2018) Maoyuan Tian et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Ube3a reinstatement mitigates epileptogenesis in Angelman syndrome model mice

(2018) Bin Gu et al.   JOURNAL OF CLINICAL INVESTIGATION

Structural dynamics of the E6AP/UBE3A-E6-p53 enzyme-substrate complex

(2018) Carolin Sailer et al.   Nature Communications

The autism-linked UBE3A T485A mutant E3 ubiquitin ligase activates the Wnt/β-catenin pathway by inhibiting the proteasome

(2017) Jason J. Yi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

In VivoKnockdown of Pathogenic Proteins via Specific and Nongenetic Inhibitor of Apoptosis Protein (IAP)-dependent Protein Erasers (SNIPERs)

(2017) Nobumichi Ohoka et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Dual regulation of Stat1 and Stat3 by the tumor suppressor protein PML contributes to interferon α-mediated inhibition of angiogenesis

(2017) Kuo-Sheng Hsu et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

The Autism Protein Ube3A/E6AP Remodels Neuronal Dendritic Arborization via Caspase-Dependent Microtubule Destabilization

(2017) Natasha Khatri et al.   JOURNAL OF NEUROSCIENCE

Reduced abundance of the E3 ubiquitin ligase E6AP contributes to decreased expression of theINK4/ARFlocus in non–small cell lung cancer

(2017) Cristina Gamell et al.   Science Signaling

Identifying the ubiquitination targets of E6AP by orthogonal ubiquitin transfer

(2017) Yiyang Wang et al.   Nature Communications

E6AP promotes prostate cancer by reducing p27 expression

(2017) Dinesh Raghu et al.   Oncotarget

Novel neurobiological roles of UBE3A

(2017) Jiandong Sun et al.   Oncotarget

Reduced abundance of the E3 ubiquitin ligase E6AP contributes to decreased expression of theINK4/ARFlocus in non–small cell lung cancer

(2017) Cristina Gamell et al.   Science Signaling

Hepatitis C virus core protein inhibits E6AP expression via DNA methylation to escape from ubiquitin-dependent proteasomal degradation

(2016) Juri Kwak et al.   CANCER LETTERS

mTOR, a Potential Target to Treat Autism Spectrum Disorder

(2016) Atsushi Sato   CNS & Neurological Disorders-Drug Targets

Daratumumab monotherapy in patients with treatment-refractory multiple myeloma (SIRIUS): an open-label, randomised, phase 2 trial

(2016) Sagar Lonial et al.   LANCET

Protein Delivery of an Artificial Transcription Factor Restores Widespread Ube3a Expression in an Angelman Syndrome Mouse Brain

(2016) Barbara J Bailus et al.   MOLECULAR THERAPY

Structure of the E6/E6AP/p53 complex required for HPV-mediated degradation of p53

(2016) Denise Martinez-Zapien et al.   NATURE

Restoration of tumor suppression in prostate cancer by targeting the E3 ligase E6AP

(2016) P J Paul et al.   ONCOGENE

An Autism-Linked Mutation Disables Phosphorylation Control of UBE3A

(2015) Jason J. Yi et al.   CELL

Ube3a Imprinting Impairs Circadian Robustness in Angelman Syndrome Models

(2015) Shu-qun Shi et al.   CURRENT BIOLOGY

Imbalanced Mechanistic Target of Rapamycin C1 and C2 Activity in the Cerebellum of Angelman Syndrome Mice Impairs Motor Function

(2015) J. Sun et al.   JOURNAL OF NEUROSCIENCE

Excitatory/Inhibitory Balance and Circuit Homeostasis in Autism Spectrum Disorders

(2015) Sacha B. Nelson et al.   NEURON

Bortezomib-Based Therapy for Newly Diagnosed Mantle-Cell Lymphoma

(2015) Tadeusz Robak et al.   NEW ENGLAND JOURNAL OF MEDICINE

Seizure-like activity in a juvenile Angelman syndrome mouse model is attenuated by reducingArcexpression

(2015) Caleigh Mandel-Brehm et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

UBE3A Regulates Synaptic Plasticity and Learning and Memory by Controlling SK2 Channel Endocytosis

(2015) Jiandong Sun et al.   Cell Reports

Uncovering a Role for SK2 in Angelman Syndrome

(2015) Sofia B. Lizarraga et al.   Cell Reports

Complete senescence: RB and PML share the task

(2014) Mathieu Vernier et al.   CELL CYCLE

Small-Molecule Inhibitors of Protein-Protein Interactions: Progressing toward the Reality

(2014) Michelle R. Arkin et al.   CHEMISTRY & BIOLOGY

Mutation Update for UBE3A Variants in Angelman Syndrome

(2014) Bekim Sadikovic et al.   HUMAN MUTATION

Oxidative stress–induced assembly of PML nuclear bodies controls sumoylation of partner proteins

(2014) Umut Sahin et al.   JOURNAL OF CELL BIOLOGY

Autoregulation of the 26S proteasome by in situ ubiquitination

(2014) Andrew D. Jacobson et al.   MOLECULAR BIOLOGY OF THE CELL

Synaptic, transcriptional and chromatin genes disrupted in autism

(2014) Silvia De Rubeis et al.   NATURE

Towards a therapy for Angelman syndrome by targeting a long non-coding RNA

(2014) Linyan Meng et al.   NATURE

The E3 ubiquitin ligase UBE3A is an integral component of the molecular circadian clock through regulating the BMAL1 transcription factor

(2014) Nicole C. Gossan et al.   NUCLEIC ACIDS RESEARCH

Topoisomerase 1 inhibition reversibly impairs synaptic function

(2014) Angela M. Mabb et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A de novo convergence of autism genetics and molecular neuroscience

(2014) Niklas Krumm et al.   TRENDS IN NEUROSCIENCES

Rapamycin improves sociability in the BTBR T+Itpr3tf/J mouse model of autism spectrum disorders

(2013) Jessica A. Burket et al.   BRAIN RESEARCH BULLETIN

XIAP inhibits autophagy via XIAP-Mdm2-p53 signalling

(2013) Xing Huang et al.   EMBO JOURNAL

The Angelman Syndrome Protein Ube3a Is Required for Polarized Dendrite Morphogenesis in Pyramidal Neurons

(2013) S. Miao et al.   JOURNAL OF NEUROSCIENCE

Topoisomerases facilitate transcription of long genes linked to autism

(2013) Ian F. King et al.   NATURE

The nuclear coactivator amplified in breast cancer 1 maintains tumor-initiating cells during development of ductal carcinoma in situ

(2013) V Ory et al.   ONCOGENE

Peroxiredoxin 1 is a tumor-associated antigen in esophageal squamous cell carcinoma

(2013) PENGFEI REN et al.   ONCOLOGY REPORTS

Surface α-Enolase Promotes Extracellular Matrix Degradation and Tumor Metastasis and Represents a New Therapeutic Target

(2013) Kuan-Chung Hsiao et al.   PLoS One

Structure Based Identification and Characterization of Flavonoids That Disrupt Human Papillomavirus-16 E6 Function

(2013) Jonathan J. Cherry et al.   PLoS One

Role of the ubiquitin ligase E6AP/UBE3A in controlling levels of the synaptic protein Arc

(2013) S. Kuhnle et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Structural Basis for Hijacking of Cellular LxxLL Motifs by Papillomavirus E6 Oncoproteins

(2013) K. Zanier et al.   SCIENCE

E6AP ubiquitin ligase regulates PML-induced senescence in Myc-driven lymphomagenesis

(2012) K. Wolyniec et al.   BLOOD

Carfilzomib and ONX 0912 Inhibit Cell Survival and Tumor Growth of Head and Neck Cancer and Their Activities Are Enhanced by Suppression of Mcl-1 or Autophagy

(2012) Y. Zang et al.   CLINICAL CANCER RESEARCH

Mutation of HERC2 causes developmental delay with Angelman-like features

(2012) Gaurav V Harlalka et al.   JOURNAL OF MEDICAL GENETICS

Mechanisms of CaMKII action in long-term potentiation

(2012) John Lisman et al.   NATURE REVIEWS NEUROSCIENCE

Maternal Loss of Ube3a Produces an Excitatory/Inhibitory Imbalance through Neuron Type-Specific Synaptic Defects

(2012) Michael L. Wallace et al.   NEURON

Decreased Tonic Inhibition in Cerebellar Granule Cells Causes Motor Dysfunction in a Mouse Model of Angelman Syndrome

(2012) K. Egawa et al.   Science Translational Medicine

A therapeutic trial of pro-methylation dietary supplements in Angelman syndrome

(2011) Lynne M. Bird et al.   AMERICAN JOURNAL OF MEDICAL GENETICS PART A

Overexpression of ligase defective E6-associated protein, E6-AP, results in mammary tumorigenesis

(2011) Sivapriya Ramamoorthy et al.   BREAST CANCER RESEARCH AND TREATMENT

Peroxiredoxin 1 Controls Prostate Cancer Growth through Toll-Like Receptor 4-Dependent Regulation of Tumor Vasculature

(2011) J. R. Riddell et al.   CANCER RESEARCH

Specific degradation of CRABP-II via cIAP1-mediated ubiquitylation induced by hybrid molecules that crosslink cIAP1 and the target protein

(2011) Keiichiro Okuhira et al.   FEBS LETTERS

Physical and Functional Interaction of the HECT Ubiquitin-protein Ligases E6AP and HERC2

(2011) Simone Kühnle et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Zn-binding AZUL domain of human ubiquitin protein ligase Ube3A

(2011) Alexander Lemak et al.   JOURNAL OF BIOMOLECULAR NMR

Topoisomerase inhibitors unsilence the dormant allele of Ube3a in neurons

(2011) Hsien-Sung Huang et al.   NATURE

Expression of AIB1 protein as a prognostic factor in breast cancer

(2011) Kyungji Lee et al.   World Journal of Surgical Oncology

Double-blind therapeutic trial in Angelman syndrome using betaine and folic acid

(2010) Sarika U. Peters et al.   AMERICAN JOURNAL OF MEDICAL GENETICS PART A

E3 ubiquitin protein ligase, E6-associated protein (E6-AP) regulates PI3K-Akt signaling and prostate cell growth

(2010) Sathish Srinivasan et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

IAP Regulation of Metastasis

(2010) Swarna Mehrotra et al.   CANCER CELL

EphB-Mediated Degradation of the RhoA GEF Ephexin5 Relieves a Developmental Brake on Excitatory Synapse Formation

(2010) Seth S. Margolis et al.   CELL

Will the Ubiquitin System Furnish as Many Drug Targets as Protein Kinases?

(2010) Philip Cohen et al.   CELL

The Angelman Syndrome Protein Ube3A Regulates Synapse Development by Ubiquitinating Arc

(2010) Paul L. Greer et al.   CELL

Promyelocytic Leukemia Protein Controls Cell Migration in Response to Hydrogen Peroxide and Insulin-like Growth Factor-1

(2010) Erin L. Reineke et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

E6AP ubiquitin ligase mediates ubiquitin-dependent degradation of peroxiredoxin 1

(2010) Junichi Nasu et al.   JOURNAL OF CELLULAR BIOCHEMISTRY

Progesterone inhibits estrogen-mediated neuroprotection against excitotoxicity by down-regulating estrogen receptor-β

(2010) Claudia Aguirre et al.   JOURNAL OF NEUROCHEMISTRY

Genomic imprinting of experience-dependent cortical plasticity by the ubiquitin ligase gene Ube3a

(2010) M. Sato et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Regulation of the polycomb protein Ring1B by self-ubiquitination or by E6-AP may have implications to the pathogenesis of Angelman syndrome

(2010) D. Zaaroor-Regev et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

PML Regulates Apoptosis at Endoplasmic Reticulum by Modulating Calcium Release

(2010) C. Giorgi et al.   SCIENCE

Increased expression of enolase α in human breast cancer confers tamoxifen resistance in human breast cancer cells

(2009) Shih-Hsin Tu et al.   BREAST CANCER RESEARCH AND TREATMENT

E6AP promotes the degradation of the PML tumor suppressor

(2009) I Louria-Hayon et al.   CELL DEATH AND DIFFERENTIATION

PML-IV functions as a negative regulator of telomerase by interacting with TERT

(2009) W. Oh et al.   JOURNAL OF CELL SCIENCE

Ube3a is required for experience-dependent maturation of the neocortex

(2009) Koji Yashiro et al.   NATURE NEUROSCIENCE

Physiological functions of the HECT family of ubiquitin ligases

(2009) Daniela Rotin et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

E3 ubiquitin ligase E6AP-mediated TSC2 turnover in the presence and absence of HPV16 E6

(2008) Li Zheng et al.   GENES TO CELLS

A novel peptide motif binding to and blocking the intracellular activity of the human papillomavirus E6 oncoprotein

(2008) Susanne Dymalla et al.   JOURNAL OF MOLECULAR MEDICINE-JMM

PML tumor suppressor is regulated by HIPK2-mediated phosphorylation in response to DNA damage

(2008) E Gresko et al.   ONCOGENE

Phosphorylation of Activation Function-1 Regulates Proteasome-Dependent Nuclear Mobility and E6-Associated Protein Ubiquitin Ligase Recruitment to the Estrogen Receptor β

(2007) Nathalie Picard et al.   MOLECULAR ENDOCRINOLOGY

Are there distinctive sleep problems in Angelman syndrome?

(2007) Karine Pelc et al.   SLEEP MEDICINE