Quantitative characterisation of carotid atherosclerotic plaque neovascularisation using contrast-enhanced ultrasound imaging: A feasibility study.

Introduction: Contrast-enhanced ultrasound (CEUS), an in vivo imaging tool for evaluating intraplaque neovascularisation (IPN), is an increasingly researched marker of susceptible atherosclerotic plaque. This study aims to assess the feasibility of quantifying carotid IPN using CEUS and to identify and characterise the neovascularisation in carotid plaques. The hospital's ethical committee approved the study, and the informed individual consent form of CEUS was obtained from all patients before the examination.

Improved Predictability of Diagnosis and Prognosis Using Serum- and Tissue-Derived Extracellular Vesicles From Bulk mRNA Sequencing in Pancreatic Ductal Adenocarcinoma.

Background: Early-stage pancreatic ductal adenocarcinoma (PDAC) is frequently misdiagnosed, contributing to its high mortality rate. Exosomal microRNAs (miRNAs) have emerged as potential biomarkers for the early detection of PDAC.

Aims: This study aimed to evaluate the feasibility of using exosomal miRNAs from PDAC tissues and serum as biomarkers for early detection and prognosis.

Direct β-C-H ketoalkylation of enaminoesters with cyclopropanols under metal-free conditions.

A TEMPO-mediated β-ketoalkylation of enaminoesters with cyclopropanols under metal-free conditions is herein described. This reaction provides a straightforward and highly efficient route to β-keto alkyl substituted enaminoesters for the first time, which could be rapidly and efficiently converted into synthetically useful 2-alkoxycarbonyl functionalized 1,5-diketones. Moreover, the practicability of this protocol is successfully demonstrated by scale-up experiments and the late-stage functionalization of natural products and pharmaceutically relevant molecules.

Discovery of Novel Pyrimidine Derivatives as Human Pin1 Covalent Inhibitors.

Pin1 (peptidyl-prolyl cis-trans isomerase NIMA-interacting 1) is a unique peptidyl-prolyl isomerase (PPIase), and inactivation of Pin1 with a covalent inhibitor is a potential strategy for developing anticancer agents. Herein, a series of sulfolane amino-substituted 2-chloro-5-nitropyrimidine derivatives were disclosed as structurally distinct covalent inhibitors toward Pin1, which were validated for their covalent binding to Cys113 of Pin1 by X-ray cocrystal structures of compounds (IC = 11.55 μM) and (IC = 3.