Targeting p53–MDM2 interaction by small-molecule inhibitors: Learning from MDM2 inhibitors in clinical trials

H Zhu, H Gao, Y Ji, Q Zhou, Z Du, L Tian… - Journal of hematology & …, 2022 - Springer
Abstract p53, encoded by the tumor suppressor gene TP53, is one of the most important
tumor suppressor factors in vivo and can be negatively regulated by MDM2 through p53 …

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 …

Catalytic enantioselective α-allylation of deconjugated butenolides with Aza-π-allylpalladium 1, 4-dipoles: access to optically pure 2-piperidones bearing an all-carbon …

SP Yuan, Q Bao, TJ Sun, JQ Zhao, ZH Wang… - Organic …, 2022 - ACS Publications
A palladium-catalyzed enantioselective α-allylation of deconjugated butenolides with aza-π-
allylpalladium 1, 4-diploes, in situ generated from palladium-mediated decarboxylation of …

Thiazole in the targeted anticancer drug discovery

A Ayati, S Emami, S Moghimi… - Future medicinal …, 2019 - Taylor & Francis
Cancer is known as one of the main causes of death in the world; and many compounds
have been synthesized to date with potential use in cancer therapy. Thiazole is a versatile …

Reviving the guardian of the genome: Small molecule activators of p53

D Nguyen, W Liao, SX Zeng, H Lu - Pharmacology & therapeutics, 2017 - Elsevier
The tumor suppressor p53 is one of the most important proteins for protection of genomic
stability and cancer prevention. Cancers often inactivate it by either mutating its gene or …

Spiro-oxindoles as a promising class of small molecule inhibitors of p53–MDM2 interaction useful in targeted cancer therapy

AK Gupta, M Bharadwaj, A Kumar… - Topics in Current …, 2017 - Springer
As a result of the toxicity of currently available anticancer drugs and the inefficiency of
chemotherapeutic treatments, the design and discovery of effective and selective antitumor …

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 …

Medicinal chemistry strategies to disrupt the p53–MDM2/MDMX interaction

A Lemos, M Leao, J Soares, A Palmeira… - Medicinal research …, 2016 - Wiley Online Library
The growth inhibitory activity of p53 tumor suppressor is tightly regulated by interaction with
two negative regulatory proteins, murine double minute 2 (MDM2) and X (MDMX), which are …

Molecular docking and molecular dynamics studies reveal the anticancer potential of medicinal-plant-derived lignans as MDM2-P53 interaction inhibitors

TH Shoaib, N Abdelmoniem, RM Mukhtar, AT Alqhtani… - Molecules, 2023 - mdpi.com
The interaction between the tumor suppressor protein p53 and its negative regulator, the
MDM2 oncogenic protein, has gained significant attention in cancer drug discovery. In this …

Small-molecule MDM2-p53 inhibitors: recent advances

B Zhang, BT Golding, IR Hardcastle - Future medicinal chemistry, 2015 - Taylor & Francis
Potent and selective small-molecule inhibitors of the p53-MDM2 interaction intended for the
treatment of p53 wild-type tumors have been designed and optimized in a number of …