Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer

SUMO pathway inhibition targets an aggressive pancreatic cancer subtype

(2020) Alexander Biederstädt et al.   GUT

A small-molecule inhibitor of the ubiquitin activating enzyme for cancer treatment

(2018) Marc L Hyer et al.   NATURE MEDICINE

SUMO2 and SUMO3 redundantly prevent a noncanonical type I interferon response

(2018) John T. Crowl et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Crystal structure of a human ubiquitin E1–ubiquitin complex reveals conserved functional elements essential for activity

(2018) Zongyang Lv et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Molecular mechanism of a covalent allosteric inhibitor of SUMO E1 activating enzyme

(2018) Zongyang Lv et al.   Nature Communications

SUMO proteins: Guardians of immune system

(2017) Sabrina Adorisio et al.   JOURNAL OF AUTOIMMUNITY

Probing the roles of SUMOylation in cancer cell biology by using a selective SAE inhibitor

(2017) Xingyue He et al.   Nature Chemical Biology

Dissecting the Specificity of Adenosyl Sulfamate Inhibitors Targeting the Ubiquitin-Activating Enzyme

(2017) Mohit Misra et al.   STRUCTURE

Pevonedistat (MLN4924), a First-in-Class NEDD8-activating enzyme inhibitor, in patients with acute myeloid leukaemia and myelodysplastic syndromes: a phase 1 study

(2015) Ronan T. Swords et al.   BRITISH JOURNAL OF HAEMATOLOGY

Knockdown of SUMO-activating enzyme subunit 2 (SAE2) suppresses cancer malignancy and enhances chemotherapy sensitivity in small cell lung cancer

(2015) Xiaoke Liu et al.   Journal of Hematology & Oncology

Sumoylation coordinates the repression of inflammatory and anti-viral gene-expression programs during innate sensing

(2015) Adrien Decque et al.   NATURE IMMUNOLOGY

Characterization of the Loss of SUMO Pathway Function on Cancer Cells and Tumor Proliferation

(2015) Xingyue He et al.   PLoS One

Inhibition of protein SUMOylation by davidiin, an ellagitannin from Davidia involucrata

(2014) Misao Takemoto et al.   JOURNAL OF ANTIBIOTICS

Development of Activity-Based Probes for Ubiquitin and Ubiquitin-like Protein Signaling Pathways

(2013) Heeseon An et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Mechanistic Studies of Substrate-assisted Inhibition of Ubiquitin-activating Enzyme by Adenosine Sulfamate Analogues

(2011) Jesse J. Chen et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A SUMOylation-Dependent Transcriptional Subprogram Is Required for Myc-Driven Tumorigenesis

(2011) J. D. Kessler et al.   SCIENCE

Ubc9 expression predicts chemoresistance in breast cancer

(2011) Shi-Feng Chen et al.   Chinese Journal of Cancer

MLN4924, a NEDD8-activating enzyme inhibitor, is active in diffuse large B-cell lymphoma models: rationale for treatment of NF- B-dependent lymphoma

(2010) M. A. Milhollen et al.   BLOOD

Designed Semisynthetic Protein Inhibitors of Ub/Ubl E1 Activating Enzymes

(2010) Xuequan Lu et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

Substrate-Assisted Inhibition of Ubiquitin-like Protein-Activating Enzymes: The NEDD8 E1 Inhibitor MLN4924 Forms a NEDD8-AMP Mimetic In Situ

(2010) James E. Brownell et al.   MOLECULAR CELL

Active site remodelling accompanies thioester bond formation in the SUMO E1

(2010) Shaun K. Olsen et al.   NATURE

The SUMO pathway: emerging mechanisms that shape specificity, conjugation and recognition

(2010) Jaclyn R. Gareau et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Ginkgolic Acid Inhibits Protein SUMOylation by Blocking Formation of the E1-SUMO Intermediate

(2009) Isao Fukuda et al.   CHEMISTRY & BIOLOGY

Kerriamycin B inhibits protein SUMOylation

(2009) Isao Fukuda et al.   JOURNAL OF ANTIBIOTICS

Principles of ubiquitin and SUMO modifications in DNA repair

(2009) Steven Bergink et al.   NATURE

An inhibitor of NEDD8-activating enzyme as a new approach to treat cancer

(2009) Teresa A. Soucy et al.   NATURE

Ubiquitin-like protein activation by E1 enzymes: the apex for downstream signalling pathways

(2009) Brenda A. Schulman et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY