Thrips Species Composition in Ontario Greenhouse Floriculture: Innovative Identification Tools and Implications for Integrated Pest Management.

Proper species identification is the keystone of successful integrated pest management (IPM). However, efforts to identify thrips species in Canadian greenhouses have not been formally made since the 1980s. In response to recent increases in crop damage, we sampled thrips communities from eight commercial floriculture greenhouses in the Niagara region (Ontario, Canada) from May until August 2016.

Biotransformation research advances - 2022 year in review.

This annual review is the eighth of its kind since 2016 (Baillie et al. 2016, Khojasteh et al. 2017, Khojasteh et al.

Characterization of Divergent Metabolic Pathways in Elucidating an Unexpected, Slow-Forming, and Long Half-Life Major Metabolite of Iclepertin.

Purpose: After single oral dosing of the glycine reuptake transporter (GlyT1) inhibitor, iclepertin (BI 425809), a single major circulating metabolite, M530a, was identified. However, upon multiple dosing, a second major metabolite, M232, was observed with exposure levels ~ twofold higher than M530a. Studies were conducted to characterize the metabolic pathways and enzymes responsible for formation of both major human metabolites.

Bioactivation and reactivity research advances - 2021 year in review.

This year's review on bioactivation and reactivity began as a part of the annual review on biotransformation and bioactivation led by Cyrus Khojasteh (see references). Increased contributions from experts in the field led to the development of a stand alone edition for the first time this year focused specifically on bioactivation and reactivity. Our objective for this review is to highlight and share articles which we deem influential and significant regarding the development of covalent inhibitors, mechanisms of reactive metabolite formation, enzyme inactivation, and drug safety.

Biotransformation novel advances - 2021 year in review.

Biotransformation field is constantly evolving with new molecular structures and discoveries of metabolic pathways that impact efficacy and safety. Recent review by Kramlinger et al. (2022) nicely captures the future (and the past) of highly impactful science of biotransformation (see the first article).

A unique sequential C-S or N-S inductive cleavage and retro-Diels-Alder fragmentation mechanism for alkylsulfonyl piperidine- and piperazine-containing compounds.

Rationale: BI 605906 undergoes a collision-induced dissociation (CID) fragmentation resulting in the loss of methylsulfinic acid and butadiene to produce a corresponding imine. The fragmentation is hypothesized to occur via inductive cleavage of the C-S bond, generating a six-membered cyclic ene, followed by the retro-Diels-Alder (RDA) reaction. The aim of this study was to provide mechanistic evidence for the proposed fragmentation by investigating the CID spectra of BI 605906 and other alkylsulfonyl piperidine- and piperazine-containing compounds.

Geographic distribution, host preferences and molecular diversity within the genus Pentalonia (Hemiptera: Aphididae).

Both Pentalonia nigronervosa and P. caladii are distributed throughout the tropics and subtropics wherever suitable hosts are grown. To clarify the host relationships of both species on a global scale, the morphology of museum specimens of Pentalonia comprising 447 samples from 77 countries was examined, and all available mitochondrial COI sequences were analysed.

Thysanoptera of Canada.

The known Canadian Thysanoptera fauna currently consists of 147 species, including 28 non-native species, and there are five additional species found only indoors. DNA barcoding data, presence of species in adjacent regions, and preliminary evidence of the presence of host-associated cryptic species suggest that there may be as many as 255 additional species awaiting discovery or description in Canada.

Hemiptera of Canada.

The Canadian Hemiptera (Sternorrhyncha, Auchenorrhyncha, and Heteroptera) fauna is reviewed, which currently comprises 4011 species, including 405 non-native species. DNA barcodes available for Canadian specimens are represented by 3275 BINs. The analysis was based on the most recent checklist of Hemiptera in Canada (Maw et al.

-Methylation of BI 187004 by Thiol -Methyltransferase.

BI 187004, an 11-hydroxysteroid dehydrogenase 1 inhibitor, was administered once daily for 14 days to eight patients with type 2 diabetes mellitus. -methylation was identified as a major biotransformation pathway. In four patients treated with BI 187004, the plasma exposure of an -methylbenzimidazole metabolite [-methylbenzimidazole regioisomer 1 (M1)] was 7-fold higher than the remaining four patients, indicating a substantial degree of metabolic variation.

A Predominant Oxidative Renal Metabolite of Empagliflozin in Male Mice Is Cytotoxic in Mouse Renal Tubular Cells but not Genotoxic.

In a previously reported CD-1 mouse 2-year carcinogenicity study with the sodium glucose cotransporter-2 inhibitor empagliflozin, an increased incidence of renal tubular adenomas and carcinomas was identified only in the male high-dose group. Follow-up investigative studies have shown that the renal tumors in male high-dose mice were preceded by a number of renal degenerative/regenerative findings. Prior cross-species in vitro metabolism studies using microsomes identified an oxidative metabolite (M466/2) predominantly formed in the male mouse kidney and which spontaneously degrades to a metabolite (M380/1) and reactive 4-OH crotonaldehyde (CTA).

BTG-AC: Break-the-Glass Access Control Model for Medical Data in Wireless Sensor Networks.

Wireless sensor networks (WSNs) have recently attracted much interest in the research community because of their wide range of applications. An emerging application for WSNs involves their use in healthcare where they are generally termed wireless medical sensor networks. In a hospital, outfitting every patient with tiny, wearable, wireless vital sign sensors would allow doctors, nurses, and other caregivers to continuously monitor the state of their patients.

How narratives can change nursing practice.

This series has explored the value of patient narratives in enabling nurses to reflect on how their practice is perceived by, and affects, patients and their families. This article describes how two student learning disability nurses used patient and carer narratives to highlight the effect of a hospital trust's lack of toilet provision for people with physical impairments, using the stories to persuade the trust to develop appropriate facilities.

The hemiptera (insecta) of Canada: constructing a reference library of DNA barcodes.

DNA barcode reference libraries linked to voucher specimens create new opportunities for high-throughput identification and taxonomic re-evaluations. This study provides a DNA barcode library for about 45% of the recognized species of Canadian Hemiptera, and the publically available R workflow used for its generation. The current library is based on the analysis of 20,851 specimens including 1849 species belonging to 628 genera and 64 families.

Comparison between Ki-67 index and mitotic index for predicting outcome in canine mast cell tumours.

Objectives: To assess correlation between Ki67 index and mitotic index and determine which more accurately predicts survival in canine mast cell tumours.

Methods: Retrospective analysis of cases from three UK referral hospitals. Correlation between Ki67 index and mitotic index was assessed and survival analysis performed.

Unexpected interaction between CYP3A4 and BI 11634: is BI 11634 interacting with CYP3A4 similar to nifedipine?

Background: Interactions between cytochrome P450 3A4 (CYP3A4) and its substrates are complex with multiple binding sites within the active site. BI 11634 is a factor Xa inhibitor in drug development and its interaction with CYP3A4 was evaluated.

Methods: Reaction phenotyping studies were conducted to determine human isoform(s) of cytochrome P450 responsible for BI 11634 metabolism using recombinant CYPs and specific chemical inhibitors.

Native aphids of New Zealand--diversity and host associations.

At least 15 species of aphids are now recognised as New Zealand natives and most of these are very likely to be endemic. Most native aphids belong in the subfamily Aphidinae (Aphidini), with a possible single species in Aphidinae-Macrosiphini, at least two in Neophyllaphidinae and one in Taiwanaphidinae. With one exception, native aphids are restricted to a single host plant genus, and these hosts are from 13 genera and 12 plant families in the Pinales and Angiospermae-Eudicotyledonae, suggesting that the aphids are a remnant fauna.

Chemical and biological evaluation of dipeptidyl boronic acid proteasome inhibitors for use in prodrugs and pro-soft drugs targeting solid tumors.

Bortezomib, a dipeptidyl boronic acid and potent inhibitor of the 26S proteasome, is remarkably effective against multiple myeloma (MM) but not against solid tumors. Dose-limiting adverse effects from "on target" inhibition of the proteasome in normal cells and tissues appear to be a key obstacle. Achieving efficacy against solid tumors therefore is likely to require making the inhibitor more selective for tumor tissue over normal tissues.

DNA barcodes to identify species and explore diversity in the Adelgidae (Insecta: Hemiptera: Aphidoidea).

The Adelgidae are relatively small, cryptic insects, exhibiting complex life cycles with parthenogenetic reproduction. Due to these characteristics, the taxonomy of the group is problematic. Here, we test the effectiveness of the standard 658-bp barcode fragment from the 5'-end of the mitochondrial cytochrome c oxidase 1 gene (COI) in differentiating among 17 species of Adelgidae, in associating life-cycle stages, and in assessing patterns of geographical variation in selected species.

Species identification of aphids (Insecta: Hemiptera: Aphididae) through DNA barcodes.

A 658-bp fragment of mitochondrial DNA from the 5' region of the mitochondrial cytochrome c oxidase 1 (COI) gene has been adopted as the standard DNA barcode region for animal life. In this study, we test its effectiveness in the discrimination of over 300 species of aphids from more than 130 genera. Most (96%) species were well differentiated, and sequence variation within species was low, averaging just 0.

Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potency and in vivo efficacy and safety.

Dipeptidyl peptidase IV (DPP-IV; E.C. 3.

Synthesis and characterization of constrained peptidomimetic dipeptidyl peptidase IV inhibitors: amino-lactam boroalanines.

We describe here the epimerization-free synthesis and characterization of a new class of conformationally constrained lactam aminoboronic acid inhibitors of dipeptidyl peptidase IV (DPP IV; E.C. 3.