Choline kinase alpha—Putting the ChoK-hold on tumor metabolism

SP Arlauckas, AV Popov, EJ Delikatny - Progress in Lipid Research, 2016 - Elsevier
It is well established that lipid metabolism is drastically altered during tumor development
and response to therapy. Choline kinase alpha (ChoKα) is a key mediator of these changes …

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 …

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 …

Structure–activity relationship of sulfonyl piperazine LpxH inhibitors analyzed by an LpxE-coupled malachite green assay

M Lee, J Zhao, SH Kwak, J Cho, M Lee… - ACS infectious …, 2019 - ACS Publications
The UDP-2, 3-diacylglucosamine pyrophosphatase LpxH in the Raetz pathway of lipid A
biosynthesis is an essential enzyme in the vast majority of Gram-negative pathogens and an …

New more polar symmetrical bipyridinic compounds: new strategy for the inhibition of choline kinase α1

FF Castro-Navas, S Schiaffino-Ortega… - Future medicinal …, 2015 - Taylor & Francis
Aim: Research of the antitumor properties of biscationic compounds has received significant
attention over the last few years. Results: A novel family of 1, 1′-([2, 2′-bipyridine]-5, 5 …

Dimeric drugs

A Nudelman - Current Medicinal Chemistry, 2022 - ingentaconnect.com
This review intends to summarize the structures of an extensive number of symmetrical-
dimeric drugs, having two monomers, linked via a bridging entity emphasizing the versatility …

Anticancer activity of the choline kinase inhibitor PL48 is due to selective disruption of choline metabolism and transport systems in cancer cell lines

P García-Molina, A Sola-Leyva, PM Luque-Navarro… - Pharmaceutics, 2022 - mdpi.com
A large number of different types of cancer have been shown to be associated with an
abnormal metabolism of phosphatidylcholine (PC), the main component of eukaryotic cell …

A new family of choline kinase inhibitors with antiproliferative and antitumor activity derived from natural products

A Estévez-Braun, AG Ravelo, E Pérez-Sacau… - Clinical and …, 2015 - Springer
Abstract Background Choline kinase alpha (ChoKα) is a critical enzyme in the synthesis of
phosphatidylcholine, a major structural component of eukaryotic cell membranes. ChoKα is …

Microwave-assisted synthesis, antiproliferative, antibacterial activities, in silico, computational studies and molecular dynamics simulation of new bis-(aryl-based …

MM Al-Kaabi, HAR Al-Hazam, L Al-Maliki… - Journal of Molecular …, 2025 - Elsevier
A new series of bis-(aryl-based chalcone) derivatives 9–15 derived from 4, 4′-(ethane-1, 2-
diylbis (oxy))-bis-benzaldehyde (8) were synthesized, via Claisen–Schmidt condensation …

Synthesis, biological evaluation, in silico modeling and crystallization of novel small monocationic molecules with potent antiproliferative activity by dual mechanism

L Serran-Aguilera, E Mariotto, G Rubbini… - European Journal of …, 2020 - Elsevier
Seeking for new anticancer drugs with strong antiproliferative activity and simple molecular
structure, we designed a novel series of compounds based on our previous reported …