Design strategies, structure activity relationship and mechanistic insights for purines as kinase inhibitors

S Sharma, J Singh, R Ojha, H Singh, M Kaur… - European journal of …, 2016 - Elsevier
Kinases control a diverse set of cellular processes comprising of reversible phosphorylation
of proteins. Protein kinases play a pivotal role in human tumor cell proliferation, migration …

Recent advances in the design of choline kinase α inhibitors and the molecular basis of their inhibition

B Rubio‐Ruiz, L Serrán‐Aguilera… - Medicinal research …, 2021 - Wiley Online Library
Upregulated choline metabolism, characterized by an increase in phosphocholine (PCho),
is a hallmark of oncogenesis and tumor progression. Choline kinase (ChoK), the enzyme …

Alterations of choline phospholipid metabolism in endometrial cancer are caused by choline kinase alpha overexpression and a hyperactivated deacylation pathway

S Trousil, P Lee, DJ Pinato, JK Ellis, R Dina… - Cancer research, 2014 - AACR
Metabolic rearrangements subsequent to malignant transformation are not well
characterized in endometrial cancer. Identification of altered metabolites could facilitate …

New bioisosteric sulphur-containing choline kinase inhibitors with a tracked mode of action

PM Luque-Navarro, MP Carrasco-Jiménez… - European journal of …, 2023 - Elsevier
Since the identification of human choline kinase as a protein target against cancer
progression, many compounds have been designed to inhibit its function and reduce the …

Choline kinase inhibitors EB-3D and EB-3P interferes with lipid homeostasis in HepG2 cells

A Sola-Leyva, LC López-Cara, P Ríos-Marco, A Ríos… - Scientific Reports, 2019 - nature.com
A full understanding of the molecular mechanism of action of choline kinase α (ChoKα)
inhibitors at the cell level is essential for developing therapeutic and preventive approaches …

[HTML][HTML] Targeted breast cancer therapy using novel nanovesicle formulations of Olea europaea extract

M del Carmen Villegas-Aguilar… - Biomedicine & …, 2024 - Elsevier
Olive leaf is a byproduct of the olive tree that is rich in phenolic compounds with potential
anticarcinogenic effects against various cancers, including breast cancer. Nevertheless, the …

The mechanism of allosteric coupling in choline kinase α1 revealed by the action of a rationally designed inhibitor

M Sahún‐Roncero, B Rubio‐Ruiz… - Angewandte Chemie …, 2013 - Wiley Online Library
Choline kinase (CHOK) is a homodimeric enzyme that catalyzes the transfer of a phosphate
group from ATP to choline to produce ADP and phosphocholine (PCho; Figure 1A), the first …

Design, synthesis, crystallization and biological evaluation of new symmetrical biscationic compounds as selective inhibitors of human Choline Kinase α1 (ChoKα1)

S Schiaffino-Ortega, E Baglioni, E Mariotto… - Scientific reports, 2016 - nature.com
A novel family of compounds derivative of 1, 1′-(((ethane-1, 2-diylbis (oxy)) bis (4, 1-
phenylene)) bis (methylene))-bispyridinium or–bisquinolinium bromide (10a-l) containing a …

Plasmodium falciparum Choline Kinase Inhibition Leads to a Major Decrease in Phosphatidylethanolamine Causing Parasite Death

L Serrán-Aguilera, H Denton, B Rubio-Ruiz… - Scientific reports, 2016 - nature.com
Malaria is a life-threatening disease caused by different species of the protozoan parasite
Plasmodium, with P. falciparum being the deadliest. Increasing parasitic resistance to …

Synthesis and Cytotoxic Activity of the Derivatives of N-(Purin-6-yl)aminopolymethylene Carboxylic Acids and Related Compounds

VP Krasnov, OA Vozdvizhenskaya, MA Baryshnikova… - Molecules, 2023 - mdpi.com
Testing a number of N-[omega-(purin-6-yl) aminoalkanoyl] derivatives of 7, 8-difluoro-3, 4-
dihydro-3-methyl-2 H-[1, 4] benzoxazine in a panel of nine tumor cell lines has shown that …