Diamino variants of piperazine-based tissue transglutaminase inhibitors.

Tissue transglutaminase (TG2) is a multifunctional protein that can catalyze the cross-linking between proteins, and function as a G-protein. TG2's unregulated behaviour has been associated with fibrosis, celiac disease and cancer metastasis. Recently, small molecule irreversible inhibitors have been designed, bearing an electrophilic warhead that can react with the catalytic cysteine, abolishing TG2's catalytic and G-protein capabilities.

Genetic analysis of chlorantraniliprole resistance in the non-target bio-control agent Trichogrammachilonis.

Trichogramma chilonis (Ishii) (Hymenoptera: Trichogrammatidae), a widely used egg parasitoid of lepidopteran pests in various crops, has developed very high levels of resistance when treated with chlorantraniliprole under laboratory conditions. This study assessed and characterized its mode of inheritance, degree of dominance, realized heritability (h), and cross-resistance. Toxicity bioassays were performed on T.

Biosynthesis of Zr-doped WO nanoparticles: Evaluation of antibacterial, antioxidant, and enzymatic activities.

Herein, biocompatible pure tungsten oxide (WO) and zirconium-doped tungsten oxide (Zr-doped WO) nanoparticles (NPs) were prepared via a green approach from moringa plants with different doping concentrations (3, 5, and 7 %). The as-synthesized materials were morphologically and optically characterized using scanning electron microscopy (SEM), energy dispersive X-ray (EDX), X-ray diffraction (XRD), Fourier-transform infrared (FTIR), and ultraviolet-visible (UV-Vis) spectroscopy. The FTIR spectra clearly showed that two distinguishing bands at 603 and 674 cm of WO were shifted to a higher wavenumber upon doping with zirconium.

Polygenic, autosomal, and stable spirotetramat resistance in Chrysoperla carnea resulting in increased fitness.

Green lacewing, Chrysoperla carnea (Stephens) is a generalist predator used as a biological control agent in agro ecosystems. In order to use chemical and biological control in an integrated way, it is advantageous to know about natural enemy resistance response to a selected chemical. To determine C.

Green synthesis of Zn-doped TIO nanoparticles from Zanthoxylum armatum.

Green synthesis is an easy, safe, and environmentally beneficial nanoparticle creation method. It is a great challenge to simultaneously improve the capping and stabilizing agent carrier separation efficiency of photocatalysts. Herein, Zn-doped Titanium dioxide (TiO) nanoparticles with high exposure of 360 nm using a UV/visible spectrophotometer were prepared via a one-step hydrothermal decomposition method.

Resistance of Lepidopteran Pests to Toxins: Evidence of Field and Laboratory Evolved Resistance and Cross-Resistance, Mode of Resistance Inheritance, Fitness Costs, Mechanisms Involved and Management Options.

() toxins are potential alternatives to synthetic insecticides for the control of lepidopteran pests. However, the evolution of resistance in some insect pest populations is a threat and can reduce the effectiveness of toxins. In this review, we summarize the results of 161 studies from 20 countries reporting field and laboratory-evolved resistance, cross-resistance, and inheritance, mechanisms, and fitness costs of resistance to different toxins.

Realized heritability, inheritance, and mechanism of chlorfenapyr resistance in biocontrol agent, Chrysoperla carnea (Stephens) (Neuroptera: Chrysopidae): A step towards sustainable pest management.

A field population of Chrysoperla carnea was exposed for 17 generations to chlorfenapyr insecticide that resulted in 217-fold resistance compared to a susceptible strain. The overlapping of LC values in reciprocal crosses and their dominance values indicated that chlorfenapyr resistance was autosomal and incompletely dominant. The chi-square analysis of back-cross mortality confirmed the polygenic nature of chlorfenapyr resistance.

Green synthesis of silver and iron nano composites using aqueous extract of seeds and their application for removal of acid black 234 dye.

Green nanotechnology has gained attraction in recent years due to the growing awareness of the environmental and health risks associated with traditional methods of nanomaterial synthesis. In the present study, nanocomposite (NCs) of silver and Iron were prepared using Zanthoxylum Armatum seeds aqueous extract which acts as a reducing, stabilizing, and capping agent. The synthesized NCs were characterized using UV/Vis Spectroscopy, powder X-ray diffraction (XRD), Scanning Electron Microscopy (SEM), and EDX.

Concurrent Olaparib and Radiation Therapy in Older Patients With Newly Diagnosed Glioblastoma: The Phase 1 Dose-Escalation PARADIGM Trial.

Purpose: Patients with glioblastoma who are older or have poor performance status (PS) experience particularly poor clinical outcomes. At the time of study initiation, these patients were treated with short-course radiation therapy (40 Gy in 15 fractions). Olaparib is an oral inhibitor of the DNA repair enzyme poly (ADP-ribose) polymerase (PARP) that is well tolerated as a single agent but exacerbates acute radiation toxicity in extracranial sites.

Development of alpha-cypermethrin resistance and its effect on biological parameters of yellow fever mosquito, Aedes aegypti (L.) (Diptera: Culicidae).

Alpha-cypermethrin interacts with the sodium channel and causes nerve blockage in insects. It is used to manage Aedes aegypti (Linnaeus) (Diptera: Culicidae), a primary vector of dengue worldwide. It not only affects both target and non-target organisms, but overuse of this insecticide increases the chances of resistance development in insect pests.

Staging by Thoracoscopy in potentially radically treatable Lung Cancer associated with Minimal Pleural Effusion (STRATIFY): protocol of a prospective, multicentre, observational study.

Introduction: Recurrence rate following radical therapy for lung cancer remains high, potentially reflecting occult metastatic disease, and better staging tools are required. Minimal pleural effusion (mini-PE) is associated with particularly high recurrence risk and is defined as an ipsilateral pleural collection (<1/3 hemithorax on chest radiograph), which is either too small to safely aspirate fluid for cytology using a needle, or from which fluid cytology is negative. Thoracoscopy (local anaesthetic thoracoscopy (LAT) or video-assisted thoracoscopic surgery (VATS)) is the gold-standard diagnostic test for pleural malignancy in patients with larger symptomatic effusions.

Comparison Of Soft Tissue Chin And Lower Lip Thickness In Adult Patients With Various Mandibular Divergence Patterns.

Background: The influence of hard tissue discrepancies on soft tissue cannot be ignored. The divergence or angle of the mandible can influence the lower lip and chin (soft tissue), similar to the influence of incisors inclinations on the pro/ retrusion of the lips. Hence this study was carried out to find out the impact of mandibular divergence patterns on the contour and thickness of lower facial soft tissues.

Negative Impact of Unstable Spiromesifen Resistance on Fitness of Tetranychus urticae (Acari: Tetranychidae).

Two-spotted spider mite, Tetranychus urticae Koch (Acari: Tetranychidae), is a phytophagous haplodiploid mite and its control is largely based on the use of pesticides. But, the short life cycle and high reproductive rate allow them to develop resistance to many pesticides. To design a strategy for resistance management, a fitness cost study was conducted on different populations of T.

Unstable fipronil resistance associated with fitness costs in fipronil-selected Aedes aegypti L.

Mosquitoes are very serious household and medically important pests transmitting many diseases of humans and animals. Among mosquitoes, Aedes aegypti L., is an active transmitter of dengue and lumpy skin disease virus, horrible and terrifying diseases, causing human and animal death throughout the world.

Facile one-step synthesis of gold nanoparticles using and evaluation of their antibacterial potential.

Nanostructure gold nanoparticles (Au NPs) are well-known biological active materials, synthesised under different environment-friendly approaches that has gained significant interest in the field of biomedicine. This study investigated a novel, fast, easy, cost-effective and the eco-friendly method to synthesise Au NPs from mediated Viscum album Linn plant extract, where the plant metabolites act as stabilising and reducing agents. The synthesised Au NPs were analysed by UV/Vis spectroscopy that gave strong signals and a sharp absorption peak at 545nm due to the presence of surface plasmon resonance (SPR) bands.

Peptidic Inhibitors and a Fluorescent Probe for the Selective Inhibition and Labelling of Factor XIIIa Transglutaminase.

Factor XIIIa (FXIIIa) is a transglutaminase of major therapeutic interest for the development of anticoagulants due to its essential role in the blood coagulation cascade. While numerous FXIIIa inhibitors have been reported, they failed to reach clinical evaluation due to their lack of metabolic stability and low selectivity over transglutaminase 2 (TG2). Furthermore, the chemical tools available for the study of FXIIIa activity and localization are extremely limited.

Remediation of Water Using a Nanofabricated Cellulose Membrane Embedded with Silver Nanoparticles.

The removal of pesticide pollution is imperative, because of their high environmental load and persistence, and their potential for bioaccumulation in, and toxicity to the environment. Most pesticides are found to be toxic even at trace levels. AgNPs can be effectively used for the adsorption of pesticides, and the incorporation of the AgNPs onto a support polymeric membrane enhances their effectiveness and reduces the potential unwanted consequences of intentionally adding free nanoparticles to the environment.

Preparation of polar embedded C18 stationary phase for efficient separation of peptides and proteins in high performance liquid chromatography.

Peptides and proteins have great therapeutic potential, and owing to their unique biological properties, their separation is very challenging. A polar embedded C18 stationary phase was prepared by functionalization of porous silica monolith particles with N-3-(trimethoxysilyl) propyl stearamide. The stationary phase was packed in narrow bore column (100 × 2.

Toxicities and Cross-Resistance of Imidacloprid, Acetamiprid, Emamectin Benzoate, Spirotetramat, and Indoxacarb in Field Populations of (Diptera: Culicidae).

is a major vector of several pathogens and is capable of breeding in various aquatic habitats. The extensive and injudicious use of synthetic chemicals against the mosquito species has led to the problem of insecticide resistance. To explore this resistance in detail, toxicity bioassays of imidacloprid, acetamiprid, emamectin benzoate, spirotetramat, and indoxacarb were performed on five field populations from Pakistan in addition to a laboratory susceptible strain.

Standardizing Pathologic Evaluation of Breast Carcinoma After Neoadjuvant Chemotherapy.

Context.—: Neoadjuvant systemic therapy refers to the use of systemic agent(s) for malignancy prior to surgical treatment and has recently emerged as an option for most breast cancer patients eligible for adjuvant systemic therapy. Consequently, treated breast carcinomas have become routine specimens in pathology practices.

Structure-activity relationships of hydrophobic alkyl acrylamides as tissue transglutaminase inhibitors.

Tissue transglutaminase (TG2) is a multifunctional protein that plays biological roles based on its ability to catalyse protein cross-linking and to function as a non-canonical G-protein known as Ghα. The non-regulated activity of TG2 has been implicated in fibrosis, celiac disease and the survival of cancer stem cells, underpinning the therapeutic potential of cell permeable small molecule inhibitors of TG2. In the current study, we designed a small library of inhibitors to explore the importance of a terminal hydrophobic moiety, as well as the length of the tether to the irreversible acrylamide warhead.

Treatment Efficacy Score-continuous residual cancer burden-based metric to compare neoadjuvant chemotherapy efficacy between randomized trial arms in breast cancer trials.

Background: Difference in pathologic complete response (pCR) rate after neoadjuvant chemotherapy does not capture the impact of treatment on downstaging of residual cancer in the experimental arm. We developed a method to compare the entire distribution of residual cancer burden (RCB) values between clinical trial arms to better quantify the differences in cytotoxic efficacy of treatments.

Patients And Methods: The Treatment Efficacy Score (TES) reflects the area between the weighted cumulative distribution functions of RCB values from two trial arms.