New diphenylmethane derivatives as peroxisome proliferator-activated receptor alpha/gamma dual agonists endowed with anti-proliferative effects and mitochondrial activity

Polypharmacology of N6-(3-Iodobenzyl)adenosine-5′-N-methyluronamide (IB-MECA) and Related A3 Adenosine Receptor Ligands: Peroxisome Proliferator Activated Receptor (PPAR) γ Partial Agonist and PPARδ Antagonist Activity Suggests Their Antidiabetic Potential

“…58 Interaction of 1a with estrogen receptor (ER) α in a breast cancer cell line was reported as a potential A 3 AR-independent mechanism for its anticancer activity. 59 …”

“…Recently, it was reported that the ligand-induced PPAR γ activation could lead to apoptosis of cancer cells, suggesting that PPAR γ agonists have anticancer potential in some cancer subtypes. 59 In this regard, the PPAR γ partial agonist activity of 1a and 1b may contribute to their diverse anticancer activity. PPAR δ is upregulated in colorectal cancers and associated with the direct promotion of colorectal tumorigenesis.…”

Analysis of differentially expressed genes induced by drought stress in tef (Eragrostistef) root

“…Mitochondrial genes were also down-regulated (Table 1). The biosynthesis and morphological regulation of mitochondria were highly affected by the gene carnitine (Piemontese et al, 2017). This protein was involved in the metabolic pathways to regulate plants under drought stress (Rao et al, 2017).…”

Benchmarking Small-Dataset Structure-Activity-Relationship Models for Prediction of Wnt Signaling Inhibition

“…We chose this dataset because these 70 compounds are all experimentally validated with the same biological assay (i.e., the internalization of Frizzled receptor proteins in U2OS cells) and form a mild class imbalance. It is noted that assays targeted at the dynamics of other Wnt-signaling-inhibition related proteins are also available in the ChEMBL database [31]- [36]. However, these assays have yet to experimentally test a sufficient number of active or inactive compounds, therefore making the QSAR modeling challenging (e.g., 3 active compounds in [36]).…”

“…It is noted that assays targeted at the dynamics of other Wnt-signaling-inhibition related proteins are also available in the ChEMBL database [31]- [36]. However, these assays have yet to experimentally test a sufficient number of active or inactive compounds, therefore making the QSAR modeling challenging (e.g., 3 active compounds in [36]). On the other hand, we found that the size of our dataset, 70, is on par with other small-dataset QSAR studies (e.g., 16 in [19], and 48 in [20]); we thus believe this dataset has a sufficient number of data to build goodperforming QSAR models.…”