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http://dx.doi.org/10.22037/aaem.v10i1.1704 | DOI Listing |
Am J Transplant
August 2025
Department of Medicine, University of Alberta, Edmonton, Canada. Electronic address:
Chronic allograft vasculopathy (CAV) limits graft and recipient survival after heart transplantation despite modern immune suppression. We examined the effect of sacubitril, an inhibitor of neprilysin neutral endopeptidase activity, on progression of CAV in HY-antigen mismatched mouse heart transplantation. We found sacubitril treatment of the recipient markedly blunted the progressive occlusion of the coronary arterial lumen versus the vehicle control.
View Article and Find Full Text PDFBioorg Med Chem Lett
August 2025
Department of Pharmaceutical Sciences, The State University of New York at Buffalo, Buffalo, NY 14214, USA. Electronic address:
The apelin receptor (APJ), a G protein-coupled receptor, has emerged as a promising therapeutic target in oncology due to its role in tumor growth, angiogenesis, metastasis, and resistance to anti-VEGF therapy. However, ML221, the only reported small-molecule APJ antagonist, exhibits extremely poor plasma (<1 % remaining after 1 h) and liver microsomal (t < 1 min) stability, limiting its translational potential. To address this, we designed and synthesized a focused series of ML221 analogs incorporating amide, ether, and sulfonate linkages to block esterase-mediated degradation aiming to improve metabolic stability while maintaining APJ antagonistic activity.
View Article and Find Full Text PDFParasit Vectors
July 2025
Research Center for Parasites & Vectors, College of Veterinary Medicine, Hunan Agricultural University, Changsha, 410128, Hunan, People's Republic of China.
Background: Baylisascaris procyonis is an intestinal ascarid worm that parasitizes in raccoons and causes fatal neural, visceral, and ocular larva migrans in humans. Phosphorylated proteins and protein kinases have been studied as vaccine and drug target candidates against parasitic infections. However, no data are available on protein phosphorylation in the raccoon roundworm.
View Article and Find Full Text PDFBackground: Atherosclerosis is a progressive arterial disease characterized by chronic inflammation and plaque formation in blood vessel walls. ELABELA, an endogenous ligand for the G protein-coupled receptor APJ (apelin peptide jejunum, apelin receptor), has multiple pharmacological activities for protecting the cardiovascular system. This study aimed to determine the potential antiatherosclerotic effect of ELABELA and reveal the underlying mechanisms.
View Article and Find Full Text PDFAnimal
July 2025
Graduate School of Bioresource and Bioenvironmental Sciences, Kyushu University, Fukuoka, Fukuoka 819-0395, Japan; Field Science Center for Northern Biosphere, Hokkaido University, Sapporo, Hokkaido 060-0811, Japan. Electronic address:
We previously reported that high nutrition early in life enhances the growth and intramuscular fat (IMF; i.e., marbling) content of grass-fattened beef cattle.
View Article and Find Full Text PDF