(Q58546852)

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MDM2-recruiting PROTAC Offers Superior, Synergistic Anti-proliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53

scientific article published on 01 November 2018

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1 May 2020

MDM2-Recruiting PROTAC Offers Superior, Synergistic Antiproliferative Activity via Simultaneous Degradation of BRD4 and Stabilization of p53 (English)

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1 May 2020

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1 May 2020

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John Hines

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1 May 2020

Schan Lartigue

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1 May 2020

Hanqing Dong

3

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1 May 2020

Yimin Qian

4

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1 May 2020

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1 November 2018

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1 May 2020

Cancer Research

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1 May 2020

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1 May 2020

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1 May 2020

251-262

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1 May 2020

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/30385614

12 December 2020

based on heuristic

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Chemical genetic control of protein levels: selective in vivo targeted degradation

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

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A rapid, reversible, and tunable method to regulate protein function in living cells using synthetic small molecules

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

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Development of an aryl hydrocarbon receptor antagonist using the proteolysis-targeting chimeric molecules approach: a potential tool for chemoprevention

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Small molecules destabilize cIAP1 by activating auto-ubiquitylation

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

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/30385614

12 December 2020

based on heuristic

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Protein knockdown using methyl bestatin-ligand hybrid molecules: design and synthesis of inducers of ubiquitination-mediated degradation of cellular retinoic acid-binding proteins.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Two-headed PROTAC: an effective new tool for targeted protein degradation

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Targeting the undruggable proteome: the small molecules of my dreams

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Selective inhibition of BET bromodomains

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Impact of linker length on the activity of PROTACs

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Small-molecule displacement of a cryptic degron causes conditional protein degradation

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Functional genomics identifies therapeutic targets for MYC-driven cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1α

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Posttranslational protein knockdown coupled to receptor tyrosine kinase activation with phosphoPROTACs

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Discovery of RG7388, a potent and selective p53-MDM2 inhibitor in clinical development

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Development of hybrid small molecules that induce degradation of estrogen receptor-alpha and necrotic cell death in breast cancer cells.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

BET and HDAC inhibitors induce similar genes and biological effects and synergize to kill in Myc-induced murine lymphoma

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

BRD4 inhibitor inhibits colorectal cancer growth and metastasis

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

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/30385614

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/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

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/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Inhibition of bromodomain and extra-terminal proteins (BET) as a potential therapeutic approach in haematological malignancies: emerging preclinical and clinical evidence

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Analysis of drug combinations: current methodological landscape

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

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/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

CCAT1 is an enhancer-templated RNA that predicts BET sensitivity in colorectal cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

BET inhibitors in the treatment of hematologic malignancies: current insights and future prospects

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

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/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structural basis of PROTAC cooperative recognition for selective protein degradation

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Ubiquitin Ligases: Structure, Function, and Regulation.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Impact of Target Warhead and Linkage Vector on Inducing Protein Degradation: Comparison of Bromodomain and Extra-Terminal (BET) Degraders Derived from Triazolodiazepine (JQ1) and Tetrahydroquinoline (I-BET726) BET Inhibitor Scaffolds

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Targeted protein knockdown using small molecule degraders

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Oridonin synergizes with Nutlin-3 in osteosarcoma cells by modulating the levels of multiple Bcl-2 family proteins

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Small-Molecule Modulation of Protein Homeostasis.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

MDM2 antagonists synergize with PI3K/mTOR inhibition in well-differentiated/dedifferentiated liposarcomas

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Homo-PROTACs: bivalent small-molecule dimerizers of the VHL E3 ubiquitin ligase to induce self-degradation.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Activation of the p53 Transcriptional Program Sensitizes Cancer Cells to Cdk7 Inhibitors.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

A Chemoproteomic Approach to Query the Degradable Kinome Using a Multi-kinase Degrader.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Lessons in PROTAC Design from Selective Degradation with a Promiscuous Warhead.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Protac-Induced Protein Degradation in Drug Discovery: Breaking the Rules or Just Making New Ones?

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Targeting negative regulation of p53 by MDM2 and WIP1 as a therapeutic strategy in cutaneous melanoma

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Pharmacological perturbation of CDK9 using selective CDK9 inhibition or degradation.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

BET Bromodomain Inhibition Synergizes with PARP Inhibitor in Epithelial Ovarian Cancer

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Targeting c-Myc: JQ1 as a promising option for c-Myc-amplified esophageal squamous cell carcinoma

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Nutlin-3a as a novel anticancer agent for adrenocortical carcinoma with CTNNB1 mutation.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Derivatization of inhibitor of apoptosis protein (IAP) ligands yields improved inducers of estrogen receptor α degradation.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Targeting the C481S Ibrutinib-Resistance Mutation in Bruton's Tyrosine Kinase using PROTAC-mediated Degradation.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Small Molecules Simultaneously Inhibiting p53-Murine Double Minute 2 (MDM2) Interaction and Histone Deacetylases (HDACs): Discovery of Novel Multitargeting Antitumor Agents

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance

1 reference

https://pubmed.ncbi.nlm.nih.gov/30385614

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.1158/0008-5472.CAN-18-2918

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1 May 2020

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1 May 2020

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1 May 2020

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