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

Y Zhao, A Aguilar, D Bernard… - Journal of medicinal …, 2015 - ACS Publications
Design of small-molecule inhibitors (MDM2 inhibitors) to block the MDM2–p53 protein–
protein interaction has been pursued as a new cancer therapeutic strategy. In recent years …

Modulators of protein–protein interactions

LG Milroy, TN Grossmann, S Hennig… - Chemical …, 2014 - ACS Publications
Since Hedin's characterization of trypsin and antitrypsin in 1906,(1) arguably the first
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …

Small-molecule MDM2 inhibitors in clinical trials for cancer therapy

S Wang, FE Chen - European journal of medicinal chemistry, 2022 - Elsevier
Disruption of the MDM2-p53 protein-protein interaction by small-molecule inhibitors has
been highly pursued by many academic laboratories and pharmaceutical companies as a …

[HTML][HTML] Small-molecule MDM2/X inhibitors and PROTAC degraders for cancer therapy: advances and perspectives

Y Fang, G Liao, B Yu - Acta Pharmaceutica Sinica B, 2020 - Elsevier
Abstract Blocking the MDM2/X–P53 protein–protein interaction has been widely recognized
as an attractive therapeutic strategy for the treatment of cancers. Numerous small-molecule …

Photoinduced radical cascade domino Heck coupling of N-aryl acrylamide with vinyl arenes enabled by palladium catalysis

P Li, Q Teng, M Chen - Chemical Communications, 2023 - pubs.rsc.org
Here, a redox-neutral palladium-catalyzed photo-induced radical cascade domino Heck
reaction of N-aryl acrylamide with vinyl arenes is described. A diverse range of bioactive …

Discovery of Novel Spiro[3H-indole-3,2′-pyrrolidin]-2(1H)-one Compounds as Chemically Stable and Orally Active Inhibitors of the MDM2–p53 Interaction

A Gollner, D Rudolph, H Arnhof, M Bauer… - Journal of medicinal …, 2016 - ACS Publications
Scaffold modification based on Wang's pioneering MDM2–p53 inhibitors led to novel,
chemically stable spiro-oxindole compounds bearing a spiro [3 H-indole-3, 2′-pyrrolidin]-2 …

Molecular hybridization design and synthesis of novel spirooxindole-based MDM2 inhibitors endowed with BCL2 signaling attenuation; a step towards the next …

G Lotfy, YMA Aziz, MM Said, H El Sayed, H El Sayed… - Bioorganic …, 2021 - Elsevier
Despite the achieved progress in developing efficient MDM2-p53 protein-protein interaction
inhibitors (MDM2 inhibitors), the acquired resistance of tumor cells to such p53 activators …

How to design a successful p53–MDM2/X interaction inhibitor: a thorough overview based on crystal structures

N Estrada‐Ortiz, CG Neochoritis, A Dömling - ChemMedChem, 2016 - Wiley Online Library
A recent therapeutic strategy in oncology is based on blocking the protein–protein
interaction between the murine double minute (MDM) homologues MDM2/X and the tumor …

Structure-based design of potent and orally active isoindolinone inhibitors of MDM2-p53 protein–protein interaction

G Chessari, IR Hardcastle, JS Ahn, B Anil… - Journal of Medicinal …, 2021 - ACS Publications
Inhibition of murine double minute 2 (MDM2)-p53 protein–protein interaction with small
molecules has been shown to reactivate p53 and inhibit tumor growth. Here, we describe …

Targeting p53-MDM2-MDMX loop for cancer therapy

Q Zhang, SX Zeng, H Lu - Mutant p53 and MDM2 in Cancer, 2014 - Springer
The tumor suppressor p53 plays a central role in anti-tumorigenesis and cancer therapy. It
has been described as “the guardian of the genome”, because it is essential for conserving …