Albumin-Binding Lutetium-177-Labeled LLP2A Derivatives as Theranostics for Melanoma.

Very late antigen-4 (VLA-4) is a transmembrane integrin protein that is highly expressed in aggressive forms of metastatic melanoma. A small-molecule peptidomimetic, LLP2A, was found to have a low pM affinity binding to VLA-4. Because LLP2A itself does not inhibit cancer cell proliferation and survival, it is an ideal candidate for the imaging and delivery of therapeutic payloads.

Characterization of road-deposited sediment wash-off and accurate splitting of initial runoff pollution in heterogeneous urban spaces.

Particulate materials arising from road-deposited sediments (RDS) are an essential target for the control and management of surface runoff pollution. However, the heterogeneity of urban spaces hinders the identification and quantification of particulate pollution, which is challenging when formulating precise control measures. To elucidate the factors that drive particulate pollution in heterogeneous urban spaces, the accumulation of RDS on dry days and the total suspended solids during six natural rainfall events were investigated across three urban-rural spatial units (central urban, central suburban, and remote suburban).

Diversifying chemical space of DNA-encoded libraries: synthesis of 2-oxa-1-azaspiro(bicyclo[3.2.0])heptanes on-DNA visible light-mediated energy transfer catalysis.

Azaspiro[3.3]heptanes are valuable synthetic targets for drug discovery programs. The challenges associated with the preparation and diversification of this moiety as compared to other small, saturated rings have led to limited applications of compounds containing this spirocycle.

Dearomative intermolecular [2 + 2] photocycloaddition for construction of C(sp)-rich heterospirocycles on-DNA.

DNA-encoded library (DEL) screens have significantly impacted new lead compound identification efforts within drug discovery. An advantage of DELs compared to traditional screening methods is that an exponentially broader chemical space can be effectively screened using only nmol quantities of billions of DNA-tagged, drug-like molecules. The synthesis of DELs containing diverse, sp-rich spirocycles, an important class of molecules in drug discovery, has not been previously reported.

Analysis of multiple pathways and levels of fluoride intake in fluorosis areas of Southwest China.

In the coal-burning fluorosis areas of China, over 10 million people suffer from dental fluorosis caused by multiple pathways of fluoride intake. However, the link between dental fluorosis prevalence, the geochemical distribution of fluoride, and contributions of different exposure pathways remain unclear. Here, we aimed to quantify the various fluoride exposure pathways and establish the association between dental fluorosis and fluoride intake in Southwest China.

Metal-Free Photochemical Imino-Alkylation of Alkenes with Bifunctional Oxime Esters.

The concurrent installation of C-C and C-N bonds across alkene frameworks represents a powerful tool to prepare motifs that are ubiquitous in pharmaceuticals and bioactive compounds. To construct such prevalent bonds, most alkene difunctionalization methods demand the use of precious metals or activated alkenes. We report a metal-free, photochemically mediated imino-alkylation of electronically diverse alkenes to install both alkyl and iminyl groups in a highly efficient manner.

Exploiting the sp character of bicyclo[1.1.1]pentyl radicals in the transition-metal-free multi-component difunctionalization of [1.1.1]propellane.

Strained bicyclic substructures are increasingly relevant in medicinal chemistry discovery research because of their role as bioisosteres. Over the last decade, the successful use of bicyclo[1.1.

m6A Methylation in Cardiovascular Diseases: From Mechanisms to Therapeutic Potential.

Cardiovascular disease (CVD) is a leading cause of morbidity and mortality worldwide. Recent studies have shown that n6-methyladenosine (m6A) plays a major role in cardiovascular homeostasis and pathophysiology. These studies have confirmed that m6A methylation affects the pathophysiology of cardiovascular diseases by regulating cellular processes such as differentiation, proliferation, inflammation, autophagy, and apoptosis.

On-DNA Hydroalkylation to Introduce Diverse Bicyclo[1.1.1]pentanes and Abundant Alkyls via Halogen Atom Transfer.

DNA-encoded libraries have proven their tremendous value in the identification of new lead compounds for drug discovery. To access libraries in new chemical space, many methods have emerged to transpose traditional mol-scale reactivity to nmol-scale, on-DNA chemistry. However, procedures to access libraries with a greater fraction of C(sp) content are still limited, and the need to "escape from flatland" more readily on-DNA remains.

Optical coherence tomography-guided drug coated balloon in non-small de novo coronary artery lesions: a prospective clinical research.

Purpose: The combined use of drug coated balloon (DCB) and optical coherence tomography (OCT) for the treatment of non-small coronary de novo lesion remains to be evaluated. We investigated the safety and efficacy of OCT-guided DCB in non-small coronary de novo lesion patients with predilation of cutting balloon.

Methods: https://clinicaltrials.

The Role of Ferroptosis in Cardiovascular Disease and Its Therapeutic Significance.

Cardiovascular diseases (CVDs) are the leading cause of deaths worldwide with regulated cell death playing an important role in cardiac pathophysiology. However, the classical mode of cell death cannot fully explain the occurrence and development of heart disease. In recent years, much research has been performed on ferroptosis, a new type of cell death that causes cell damage and contributes to the development of atherosclerosis, myocardial infarction, heart failure, and other diseases.

Cut-off values of lesion and vessel quantitative flow ratio in de novo coronary lesion post-drug-coated balloon therapy predicting vessel restenosis at mid-term follow-up.

Background: Drug-coated balloons (DCBs) have emerged as potential alternatives to drug-eluting stents in specific lesion subsets for de novo coronary lesions. Quantitative flow ratio (QFR) is a method based on the three-dimensional quantitative coronary angiography and contrast flow velocity during coronary angiography (CAG), obviating the need for an invasive fractional flow reserve procedural. This study aimed to assess the serial angiographic changes of de novo lesions post-DCB therapy and further explore the cut-off values of lesion and vessel QFR, which predict vessel restenosis (diameter stenosis [DS] ≥50%) at mid-term follow-up.

The Role of Exosomal Non-Coding RNAs in Coronary Artery Disease.

Cardiovascular disease (CVD) remains the leading cause of morbidity and mortality worldwide. Atherosclerosis (AS) is a major cause of CVD. Oxidative stress, endothelial dysfunction, and inflammation are key factors involved in the development and progression of AS.

Coronary sequelae of Kawasaki disease treated with rotational atherectomy and drug coated balloon: A case report.

Introduction: Kawasaki disease (KD) is an acute vasculitis syndrome that mainly affects children and is the first cause of acquired heart disease. Coronary artery lesion is the most serious complication of KD. Only two previous studies have reported similar cases, but we reported patient was younger and had a longer follow-up.

Relative Rates of Metal-Free Azide-Alkyne Cycloadditions: Tunability over 3 Orders of Magnitude.

The thermal (3 + 2) dipolar azide-alkyne cycloaddition, proceeding without copper or strained alkynes, is an underutilized ligation with potential applications in materials, bioorganic, and synthetic chemistry. Herein, we investigate the effects of alkyne substitution on the rate of this reaction, both experimentally and computationally. Electron-withdrawing groups accelerate the reaction, providing a range of relative rates from 1.

Awareness of hypertension and related factors in northeastern China: a cross-sectional study.

Timely awareness of hypertension is among the most crucial components in reducing the burden of hypertension. However, there is limited information about the awareness of hypertension in northern China. Therefore, in this cross-sectional study, we aimed to investigate the awareness of hypertension and its associated factors in the Jilin province in China; the study was conducted between July 2014 and December 2015 in four cities and four rural counties in the Jilin province as part of a national study.

Differences in prevalence of hypertension and associated risk factors in urban and rural residents of the northeastern region of the People's Republic of China: A cross-sectional study.

Background: Hypertension is a significant global public health problem and recognized as an important risk factor for cardiovascular diseases. This study was designed to assess the current prevalence of hypertension and to explore risk factors associated with hypertension by urban and rural status to guide the prevention and control of hypertension in Jilin province.

Methods: A multi-stage stratified random cluster sampling method was used to obtain data on hypertension, which was investigated by physical examination and face-to-face questionnaire in July 2014-December 2015.

Prevalence and distribution of hypertension and related risk factors in Jilin Province, China 2015: a cross-sectional study.

Objective: This study aimed to investigate the prevalence and distribution of hypertension and its related factors in Jilin province, China.

Design: A cross-sectional study in four cities and four rural counties in Jilin as part of a national Chinese study.

Participants And Setting: A total of 15 206 participants who were ≥15 years old and were selected using a stratified multistage random sampling method.

MicroRNA-210 Modulates the Cellular Energy Metabolism Shift During H2O2-Induced Oxidative Stress by Repressing ISCU in H9c2 Cardiomyocytes.

Background/aims: The myocardial energy metabolism shift is one of the most important pathological features of ischemic heart disease (IHD). Although several microRNAs (miRs) are involved in the regulation of myocardial energy metabolism, their exact effects and underlying mechanisms remain unclear. The aim of this study was to investigate whether microRNA(miR-210) regulates the energy metabolism shift during oxidative stress in H9c2 cardiomyocytes.

Facile and efficient access to Androsten-17-(1',3',4')-pyrazoles and Androst-17β-(1',3',4')-pyrazoles via Vilsmeier reagents, and their antiproliferative activity evaluation in vitro.

In this work, twenty-seven novel steroidal pyrazole derivatives were designed and effectively synthesized with two different commercially available staring material, Isopregnanolone 1 and 5,16-Pregnadienolone 7, via the key intermediates, 17β-(4'-formyl)pyrazolylandrost-3β-yl formate and 17-(4'-formyl)pyrazolylandrost- 5,16-dienes-3β-yl formate, which were obtained from the cyclization of steroidal phenylhydrazone with Vilsmeier reagent catalyzed by phosphorous oxychloride followed by hydrolysis, then Borch reduction to afford the target derivatives under mild conditions. Structures of these compounds were identified by H NMR, C NMR and high resolution mass spectrometry. Based on our previous work, the cytotoxicity of these derivatives were evaluated by the SRB method against 293T cell lines and three cancer cell lines: A549, Hela and MCF-7.

Initial clinical experience of CrossBoss catheter for in-stent chronic total occlusion lesions: A case report.

Background: The CrossBoss coronary chronic total occlusion (CTO) crossing catheter has been demonstrated to have greatly improved the success rate of crossing CTO lesions, but there are no published data on its application for in-stent CTO lesions.

Methods: In the current study, we retrospectively reviewed the clinical data of 8 patients with in-stent CTO lesions that were managed with the CrossBoss catheter and herein we report the efficacy and safety of the CrossBoss crossing and re-entry system for this clinically challenging condition.

Results: The CrossBoss catheter was used for 8 patients with in-stent CTO lesions, which resulted in success in 6 cases and failure in 2 cases, with a 75% success rate.

Synthesis and Antimicrobial Activity of Calycanthaceous Alkaloid Analogues.

A series of 24 novel derivatives of the calycanthaceous alkaloids with a tetrahydropyrroloindol-based core structure was synthesized from tryptophan in good yields. Their structures were characterized by IR, ¹H NMR, and ¹³C NMR spectroscopy and ESI-MS. The synthesized compounds were evaluated against a wide variety of plant pathogenic fungi.

Synthesis and fungicidal activity of tryptophan analogues - the unexpected calycanthaceous alkaloid derivatives.

A series of 21 N-protected tryptophan derivatives were synthesised from tryptophan in good yields. Their structures were characterised by IR, H NMR, C NMR, DEPT (90° and 135°) and MS analysis. The synthesised compounds were evaluated against a wide variety of plant pathogen fungi.

Efficient Synthesis and Antibacterial Evaluation of (±)-Yanglingmycin and Its Analogues.

An efficient synthetic route was developed for the large-scale preparation of (±)-Yanglingmycin and its analogues. Three series of derivatives of (±)-Yanglingmycin were synthesized and the structures of all compounds were elucidated by analyses of NMR and ESI-MS spectra data. Moreover, their antibacterial activities against seven species of bacteria were systematically evaluated by the micro-broth dilution method, most of which displayed considerable activity.