4.7 Article

Development of MDM2 degraders based on ligands derived from Ugi reactions: Lessons and discoveries

Related references

Note: Only part of the references are listed.
Editorial Material Biochemistry & Molecular Biology

The Rise of Molecular Glues

Stuart L. Schreiber

Summary: The 30th anniversary of the discovery of cyclosporin A and FK506 marks a milestone in understanding their role as molecular glues that induce new protein-protein interactions. The emergence of new molecular-glue probes and medications has sparked interest in this field.
Article Biochemistry & Molecular Biology

Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15

Tyler B. Faust et al.

NATURE CHEMICAL BIOLOGY (2020)

Article Biochemistry & Molecular Biology

Structural basis of indisulam-mediated RBM39 recruitment to DCAF15 E3 ligase complex

Dirksen E. Bussiere et al.

NATURE CHEMICAL BIOLOGY (2020)

Article Biochemistry & Molecular Biology

Selective Degradation of GSPT1 by Cereblon Modulators Identified via a Focused Combinatorial Library

Chelsea E. Powell et al.

ACS CHEMICAL BIOLOGY (2020)

Article Multidisciplinary Sciences

Bardoxolone conjugation enables targeted protein degradation of BRD4

Bingqi Tong et al.

SCIENTIFIC REPORTS (2020)

Article Biochemistry & Molecular Biology

Cereblon Modulators Target ZBTB16 and Its Oncogenic Fusion Partners for Degradation via Distinct Structural Degrons

Mary E. Matyskiela et al.

ACS CHEMICAL BIOLOGY (2020)

Review Biochemistry & Molecular Biology

Applications of genome editing technology in the targeted therapy of human diseases: mechanisms, advances and prospects

Hongyi Li et al.

SIGNAL TRANSDUCTION AND TARGETED THERAPY (2020)

Article Biochemistry & Molecular Biology

A fluorinated indole-based MDM2 antagonist selectively inhibits the growth of p53wt osteosarcoma cells

Lukasz Skalniak et al.

FEBS JOURNAL (2019)

Article Biochemistry & Molecular Biology

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

Carl C. Ward et al.

ACS CHEMICAL BIOLOGY (2019)

Article Biochemistry & Molecular Biology

Harnessing the anti-cancer natural product nimbolide for targeted protein degradation

Jessica N. Spradlin et al.

NATURE CHEMICAL BIOLOGY (2019)

Article Biochemistry & Molecular Biology

Electrophilic PROTACs that degrade nuclear proteins by engaging DCAF16

Xiaoyu Zhang et al.

NATURE CHEMICAL BIOLOGY (2019)

Article Chemistry, Medicinal

Development of selective small molecule MDM2 degraders based on nutlin

Bo Wang et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Biochemistry & Molecular Biology

Development of Small Molecule Chimeras That Recruit AhR E3 Ligase to Target Proteins

Nobumichi Ohoka et al.

ACS CHEMICAL BIOLOGY (2019)

Article Chemistry, Medicinal

Hitting on the move: Targeting intrinsically disordered protein states of the MDM2-p53 interaction

Constantinos G. Neochoritis et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2019)

Article Chemistry, Medicinal

A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos

Mary E. Matyskiela et al.

JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Chemistry, Medicinal

Discovery of a Keap1-dependent peptide PROTAC to knockdown Tau by ubiquitination-proteasome degradation pathway

Mengchen Lu et al.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2018)

Article Biochemistry & Molecular Biology

Plasticity in binding confers selectivity in ligand-induced protein degradation

Radoslaw P. Nowak et al.

NATURE CHEMICAL BIOLOGY (2018)

Article Multidisciplinary Sciences

Delineating the role of cooperativity in the design of potent PROTACs for BTK

Adelajda Zorba et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2018)

Article Biochemistry & Molecular Biology

Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead

Daniel P. Bondeson et al.

CELL CHEMICAL BIOLOGY (2018)

Article Multidisciplinary Sciences

pSILAC mass spectrometry reveals ZFP91 as IMiD-dependent substrate of the CRL4CRBN ubiquitin ligase

Jian An et al.

NATURE COMMUNICATIONS (2017)

Article Multidisciplinary Sciences

A novel cereblon modulator recruits GSPT1 to the CRL4CRBN ubiquitin ligase

Mary E. Matyskiela et al.

NATURE (2016)

Article Multidisciplinary Sciences

Lenalidomide induces ubiquitination and degradation of CK1a in del(5q) MDS

Jan Kroenke et al.

NATURE (2015)

Article Multidisciplinary Sciences

Phthalimide conjugation as a strategy for in vivo target protein degradation

Georg E. Winter et al.

SCIENCE (2015)

Article Chemistry, Medicinal

Discovery of AMG 232, a Potent, Selective, and Orally Bioavailable MDM2-p53 Inhibitor in Clinical Development

Daqing Sun et al.

JOURNAL OF MEDICINAL CHEMISTRY (2014)

Article Multidisciplinary Sciences

Lenalidomide Causes Selective Degradation of IKZF1 and IKZF3 in Multiple Myeloma Cells

Jan Kroenke et al.

SCIENCE (2014)

Article Chemistry, Medicinal

Discovery of RG7388, a Potent and Selective p53-MDM2 Inhibitor in Clinical Development

Qingjie Ding et al.

JOURNAL OF MEDICINAL CHEMISTRY (2013)

Article Chemistry, Medicinal

Discovery of RG7112: A Small-Molecule MDM2 Inhibitor in Clinical Development

Binh Vu et al.

ACS MEDICINAL CHEMISTRY LETTERS (2013)

Article Chemistry, Medicinal

Exhaustive Fluorine Scanning toward Potent p53-Mdm2 Antagonists

Yijun Huang et al.

CHEMMEDCHEM (2012)

Article Chemistry, Multidisciplinary

Targeting the von Hippel-Lindau E3 Ubiquitin Ligase Using Small Molecules To Disrupt the VHL/HIF-1α Interaction

Dennis L. Buckley et al.

JOURNAL OF THE AMERICAN CHEMICAL SOCIETY (2012)

Article Multidisciplinary Sciences

In vivo activation of the p53 pathway by small-molecule antagonists of MDM2

LT Vassilev et al.

SCIENCE (2004)

Article Multidisciplinary Sciences

Protacs: Chimeric molecules that target proteins to the Skp1-Cullin-F box complex for ubiquitination and degradation

KM Sakamoto et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2001)