Spirooxindole: a versatile biologically active heterocyclic scaffold

SS Panda, AS Girgis, MN Aziz, MS Bekheit - Molecules, 2023 - mdpi.com
Spirooxindoles occupy an important place in heterocyclic chemistry. Many natural
spirooxindole-containing compounds have been identified as bio-promising agents …

[HTML][HTML] Computer-aided drug design in anti-cancer drug discovery: What have we learnt and what is the way forward?

O Iwaloye, PO Ottu, F Olawale, OO Babalola… - Informatics in Medicine …, 2023 - Elsevier
The escalating prevalence of cancer on a global scale, coupled with the inadequacies of
present-day therapies and the emergence of drug-resistant cancer strains, has necessitated …

p53 as a potential target for treatment of cancer: A perspective on recent advancements in small molecules with structural insights and SAR studies

R Bhatia, B Kumar - European Journal of Medicinal Chemistry, 2023 - Elsevier
Cancer represents one of the world's biggest hazardous diseases. p53 is the uttermost
researched tumour suppressor protein. It is commonly considered the “guardian of the …

[HTML][HTML] Methyltransferase set7/9 as a multifaceted regulator of ROS response

A Daks, O Shuvalov, O Fedorova… - … journal of biological …, 2023 - ncbi.nlm.nih.gov
Reactive oxygen species (ROS) induce multiple signaling cascades in the cell and hence
play an important role in the regulation of the cell's fate. ROS can cause irreversible damage …

Structure-based discovery of novel α-aminoketone derivatives as dual p53-MDM2/MDMX inhibitors for the treatment of cancer

H Luo, D Si, X Sun, M Wang, Y Yang, B Wang… - European Journal of …, 2023 - Elsevier
The function of the p53 protein is impaired by the overexpression of its negative regulator
murine double minute 2 protein (MDM2) and homologous protein MDMX. Disruption of the …

Discovery of JN122, a Spiroindoline-Containing Molecule that Inhibits MDM2/p53 Protein–Protein Interaction and Exerts Robust In Vivo Antitumor Efficacy

J Cheng, Z Yan, K Jiang, C Liu, D Xu… - Journal of Medicinal …, 2023 - ACS Publications
MDM2 and MDM4 cooperatively and negatively regulate p53, while this pathway is often
hijacked by cancer cells in favor of their survival. Blocking MDM2/p53 interaction with small …

Development and Nanoparticle-Mediated Delivery of Novel MDM2/MDM4 Heterodimer Peptide Inhibitors to Enhance 5-Fluorouracil Nucleolar Stress in Colorectal …

F Merlino, A Pecoraro, G Longobardi… - Journal of Medicinal …, 2024 - ACS Publications
Colorectal cancer (CRC) often involves wild-type p53 inactivation by MDM2 and MDM4
overexpression, promoting tumor progression and resistance to 5-fluoruracil (5-FU) …

Emerging role and therapeutic implications of p53 in intervertebral disc degeneration

Y Wang, S Hu, W Zhang, B Zhang, Z Yang - Cell Death Discovery, 2023 - nature.com
Lower back pain (LBP) is a common degenerative musculoskeletal disease that imposes a
huge economic burden on both individuals and society. With the aggravation of social aging …

Advancements in targeting tumor suppressor genes (p53 and BRCA 1/2) in breast cancer therapy

Chahat, N Nainwal, Y Murti, S Yadav, P Rawat… - Molecular Diversity, 2024 - Springer
Globally, among numerous cancer subtypes, breast cancer (BC) is one of the most prevalent
forms of cancer affecting the female population. A female's family history significantly …

Antineoplastic indole-containing compounds with potential VEGFR inhibitory properties

DR Aboshouk, MA Youssef, MS Bekheit, AR Hamed… - RSC …, 2024 - pubs.rsc.org
Cancer is one of the most significant health challenges worldwide. Various techniques, tools
and therapeutics/materials have been developed in the last few decades for the treatment of …