Small-molecule inhibitors as potential therapeutics and as tools to understand the role of phospholipases A2

A Nikolaou, MG Kokotou, S Vasilakaki… - Biochimica et Biophysica …, 2019 - Elsevier
Abstract Phospholipase A 2 (PLA 2) enzymes are involved in various inflammatory
pathological conditions including arthritis, cardiovascular and autoimmune diseases. The …

The design and discovery of phospholipase A2 inhibitors for the treatment of inflammatory diseases

CS Batsika, ADD Gerogiannopoulou… - Expert Opinion on …, 2021 - Taylor & Francis
ABSTRACT Phospholipase A2 (PLA2) enzymes are implicated in several pathological
conditions such as arthritis, cardiovascular diseases, and diabetes. It is highly important to …

Inhibitors of phospholipase A2 and their therapeutic potential: an update on patents (2012-2016)

MG Kokotou, D Limnios, A Nikolaou… - Expert opinion on …, 2017 - Taylor & Francis
Introduction: The regulation of the catalytic activity of the various phospholipase A2 enzymes
is of high importance because these enzymes are involved in various pathological …

Antitumoral effects of γCdcPLI, a PLA2 inhibitor from Crotalus durissus collilineatus via PI3K/Akt pathway on MDA-MB-231 breast cancer cell

SNC Gimenes, DS Lopes, PT Alves, FVPV Azevedo… - Scientific reports, 2017 - nature.com
Abstract Phospholipases A2 (PLA2s) overexpression is closely associated with the
malignant potential of breast cancers. Here, we showed for the first the antitumoral effects of …

New quinoxalinone inhibitors targeting secreted phospholipase A2 and α-glucosidase

FAS Alasmary, FS Alnahdi, A Ben Bacha… - Journal of enzyme …, 2017 - Taylor & Francis
Elevated blood glucose and increased activities of secreted phospholipase A2 (sPLA2) are
strongly linked to coronary heart disease. In this report, our goal was to develop small …

Current Anti-Inflammatory Therapies and the Potential of Secretory Phospholipase A2 Inhibitors in the Design of New Anti-Inflammatory Drugs: A Review of 2012-2018

TA Sales, S Marcussi… - Current Medicinal …, 2020 - ingentaconnect.com
The inflammatory process is a natural self-defense response of the organism to damage
agents and its action mechanism involves a series of complex reactions. However, in some …

Small Peptides Able to Suppress Prostaglandin E2 Generation in Renal Mesangial Cells

S Vasilakaki, O Pastukhov, T Mavromoustakos… - Molecules, 2018 - mdpi.com
Peptide drug discovery may play a key role in the identification of novel medicinal agents.
Here, we present the development of novel small peptides able to suppress the production …

Serum metabolomics coupled with network pharmacology strategy to explore therapeutic effects of Scutellaria Baicalensis Georgi on diabetic nephropathy

MEN Li-Hui, PI Zi-Feng, HU Ming-Xin, LIU Shu… - Chinese Journal of …, 2021 - Elsevier
Scutellaria baicalensis Georgi (S. baicalensis) is a traditional Chinese medicine that has
been used in the treatment of diabetes for centuries. Although it has curative effects on …

N-Acylated and N-Alkylated 2-Aminobenzothiazoles Are Novel Agents That Suppress the Generation of Prostaglandin E2

MA Theodoropoulou, A Psarra, M Erhardt, A Nikolaou… - Biomolecules, 2022 - mdpi.com
The quest for novel agents to regulate the generation of prostaglandin E2 (PGE2) is of high
importance because this eicosanoid is a key player in inflammatory diseases. We …

α-Ketoheterocycles Able to Inhibit the Generation of Prostaglandin E2 (PGE2) in Rat Mesangial Cells

A Psarra, MA Theodoropoulou, M Erhardt, M Mertiri… - Biomolecules, 2021 - mdpi.com
Prostaglandin E2 (PGE2) is a key mediator of inflammation, and consequently huge efforts
have been devoted to the development of novel agents able to regulate its formation. In this …