(Q90328524)

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Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders

scientific article published on 21 October 2019

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12 April 2020

Simple Structural Modifications Converting a Bona fide MDM2 PROTAC Degrader into a Molecular Glue Molecule: A Cautionary Tale in the Design of PROTAC Degraders (English)

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12 April 2020

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12 April 2020

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12 April 2020

author name string

Jiuling Yang

1

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12 April 2020

Yangbing Li

2

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12 April 2020

Angelo Aguilar

3

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12 April 2020

Zhaomin Liu

4

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12 April 2020

publication date

21 October 2019

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12 April 2020

Journal of Medicinal Chemistry

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12 April 2020

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12 April 2020

21

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12 April 2020

9471-9487

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12 April 2020

Discovery of potent antagonists of the interaction between human double minute 2 and tumor suppressor p53

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The IARC TP53 database: new online mutation analysis and recommendations to users

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Development of Protacs to Target Cancer-promoting Proteins for Ubiquitination and Degradation

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structure-based design of potent non-peptide MDM2 inhibitors

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structural insights into eRF3 and stop codon recognition by eRF1

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identification of a primary target of thalidomide teratogenicity

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Discovery and optimization of a novel spiropyrrolidine inhibitor of β-secretase (BACE1) through fragment-based drug design

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Cereblon is a direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Diastereomeric spirooxindoles as highly potent and efficacious MDM2 inhibitors

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A potent small-molecule inhibitor of the MDM2-p53 interaction (MI-888) achieved complete and durable tumor regression in mice.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The myeloma drug lenalidomide promotes the cereblon-dependent destruction of Ikaros proteins

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Lenalidomide causes selective degradation of IKZF1 and IKZF3 in multiple myeloma cells

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Cryoelectron microscopic structures of eukaryotic translation termination complexes containing eRF1-eRF3 or eRF1-ABCE1

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structure of the DDB1–CRBN E3 ubiquitin ligase in complex with thalidomide

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Design of chemically stable, potent, and efficacious MDM2 inhibitors that exploit the retro-mannich ring-opening-cyclization reaction mechanism in spiro-oxindoles.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Elucidation of Acquired Resistance to Bcl-2 and MDM2 Inhibitors in Acute Leukemia In Vitro and In Vivo.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

DRUG DEVELOPMENT. Phthalimide conjugation as a strategy for in vivo target protein degradation

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Selective Small Molecule Induced Degradation of the BET Bromodomain Protein BRD4.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Catalytic in vivo protein knockdown by small-molecule PROTACs.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Modular PROTAC Design for the Degradation of Oncogenic BCR-ABL.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Small-Molecule PROTACS: New Approaches to Protein Degradation

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

SPLINTS: small-molecule protein ligand interface stabilizers

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structural basis of lenalidomide-induced CK1α degradation by the CRL4(CRBN) ubiquitin ligase

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A novel cereblon modulator recruits GSPT1 to the CRL4(CRBN) ubiquitin ligase

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Induced protein degradation: an emerging drug discovery paradigm

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Targeted Degradation of BET Proteins in Triple-Negative Breast Cancer.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Targeted protein degradation by PROTACs

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Proteolysis-Targeting Chimeras: Induced Protein Degradation as a Therapeutic Strategy.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Anticancer sulfonamides target splicing by inducing RBM39 degradation via recruitment to DCAF15.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Waste disposal-An attractive strategy for cancer therapy.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Selective degradation of splicing factor CAPERα by anticancer sulfonamides

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Targeted Protein Degradation: from Chemical Biology to Drug Discovery

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Molecular recognition of ternary complexes: a new dimension in the structure-guided design of chemical degraders

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Translation Termination Factor GSPT1 Is a Phenotypically Relevant Off-Target of Heterobifunctional Phthalimide Degraders.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery.

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression

1 reference

https://pubmed.ncbi.nlm.nih.gov/31560543

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.1021/ACS.JMEDCHEM.9B00846

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:31560543%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

PubMed publication ID

1 reference

Europe PubMed Central

PubMed publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:31560543%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

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