(Q90331262)

English

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

scientific article published on 10 December 2018

In more languages

default for all languages

No label defined

No description defined

Statements

scholarly article

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

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 (English)

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

1 reference

based on heuristic

inferred from title

10

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

author name string

Yangbing Li

1

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

Jiuling Yang

2

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

Angelo Aguilar

3

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

Donna McEachern

4

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

Sally Przybranowski

5

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

Liu Liu

6

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

Chao-Yie Yang

7

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

Mi Wang

8

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

Xin Han

9

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

publication date

10 December 2018

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

Journal of Medicinal Chemistry

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

62

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

2

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

448-466

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

The mdm-2 oncogene product forms a complex with the p53 protein and inhibits p53-mediated transactivation

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The p53-mdm-2 autoregulatory feedback loop

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Functions of the MDM2 oncoprotein

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Mdm2: the ups and downs

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

p53 and human cancer: the first ten thousand mutations.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

The p53 family in differentiation and tumorigenesis.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Awakening guardian angels: drugging the p53 pathway

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

MDM2, MDMX and p53 in oncogenesis and cancer therapy

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

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/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Discovery of AMG 232, a potent, selective, and orally bioavailable MDM2-p53 inhibitor in clinical development

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

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

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

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/30525597

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/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Small-molecule inhibitors of the MDM2-p53 protein-protein interaction (MDM2 Inhibitors) in clinical trials for cancer treatment.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

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/30525597

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/30525597

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/30525597

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/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Discovery of a Dihydroisoquinolinone Derivative (NVP-CGM097): A Highly Potent and Selective MDM2 Inhibitor Undergoing Phase 1 Clinical Trials in p53wt Tumors

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

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/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Inducing Protein Degradation as a Therapeutic Strategy.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

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/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Development of BCR-ABL degradation inducers via the conjugation of an imatinib derivative and a cIAP1 ligand.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

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/30525597

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/30525597

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/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Discovery of 4-((3'R,4'S,5'R)-6″-Chloro-4'-(3-chloro-2-fluorophenyl)-1'-ethyl-2″-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3″-indoline]-5'-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine [...]

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Degradation of the BAF Complex Factor BRD9 by Heterobifunctional Ligands.

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Chemically induced degradation of CDK9 by a proteolysis targeting chimera (PROTAC).

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Structural basis of thalidomide enantiomer binding to cereblon

1 reference

https://pubmed.ncbi.nlm.nih.gov/30525597

12 December 2020

based on heuristic

inferred from PubMed ID database lookup

Identifiers

10.1021/ACS.JMEDCHEM.8B00909

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

PMC publication ID

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

PubMed publication ID

1 reference

Europe PubMed Central

PMC publication ID

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:30525597%20AND%20SRC:MED&resulttype=core&format=json

12 April 2020

Sitelinks

Wikipedia(0 entries)

Wikibooks(0 entries)

Wikinews(0 entries)

Wikiquote(0 entries)

Wikisource(0 entries)

Wikiversity(0 entries)

Wikivoyage(0 entries)

Wiktionary(0 entries)

Multilingual sites(0 entries)

Retrieved from "https://www.wikidata.org/w/index.php?title=Q90331262&oldid=1644943902"