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Cell Painting unravels insecticidal modes of action on Spodoptera frugiperda insect cells.
Pestic Biochem Physiol
August 2024
R&D Hit Discovery, Bayer AG, Crop Science Division, Monheim, Germany. Electronic address:
The "Cell Painting" technology utilizes multiplexed fluorescent staining of various cell organelles, to produce high-content microscopy images of cells for multidimensional phenotype assessment. The phenotypic profiles extracted from those images can be analyzed upon perturbations with biologically active molecules to annotate the mode of action or biological activity by comparison with reference profiles of already known mechanisms of action, ultimately enabling the determination of on-target and off-target effects. This approach is already described in various human cell cultures, the most commonly used being the U2OS cell line, yet allows broad applications in additional areas of chemical-biological research.
View Article and Find Full Text PDFPharmacological Classes of Peptides Targeted to Calcium, Sodium, and Potassium Channels.
Protein Pept Lett
January 2024
Department of Physical Sciences, College of Science, University of the Philippines Baguio, Baguio City 2600, Philippines.
This review describes the specific features of families of Conus venom peptides (conotoxins or conopeptides) that represent twelve pharmacological classes. Members of these conopeptide families are targeted to voltage-gated ion channels, such as calcium, sodium, and potassium channels. The conopeptides covered in this work include omega-conotoxins and contryphans with calcium channels as targets; mu-conotoxins, muO-conotoxins, muP-conotoxins, delta-conotoxins and iota-conotoxin with sodium channels as targets; and kappa-conotoxins, kappaM-conotoxins, kappaO-conotoxin, conkunitzins, and conorfamide with potassium channels as targets.
View Article and Find Full Text PDFThe Insecticidal Activity of (Werner, 1894) Paratoid Secretion in Cocroaches.
Toxins (Basel)
October 2020
Laboratório de Neurobiologia e Toxinologia, LANETOX, Universidade Federal do Pampa, Campus São Gabriel, São Gabriel RS 97307-020, Brazil.
is a common toad found in South America, whose paratoid toxic secretion has never been explored as an insecticide. In order to evaluate its insecticidal potential, cockroaches were used as an experimental model in biochemical, physiological and behavioral procedures. Lethality assays with paratoid secretion (RSPS) determined the LD value after 24 h (58.
View Article and Find Full Text PDFGrp94 Regulates the Recruitment of Aneural AChR Clusters for the Assembly of Postsynaptic Specializations by Modulating ADF/Cofilin Activity and Turnover.
eNeuro
June 2021
School of Biomedical Sciences, Li Ka Shing Faculty of Medicine, The University of Hong Kong, Hong Kong
Temperature is a physiological factor that affects neuronal growth and synaptic homeostasis at the invertebrate neuromuscular junctions (NMJs); however, whether temperature stress could also regulate the structure and function of the vertebrate NMJs remains unclear. In this study, we use primary cultures as a vertebrate model system for investigating the involvement of heat shock protein 90 (HSP90) family of stress proteins in NMJ development. First, cold temperature treatment or HSP90 inhibition attenuates the formation of aneural acetylcholine receptor (AChR) clusters, but increases their stability after they are formed, in cultured muscles.
View Article and Find Full Text PDFResting-State Structure and Gating Mechanism of a Voltage-Gated Sodium Channel.
Cell
August 2019
Department of Pharmacology, University of Washington, Seattle, WA 98195, USA. Electronic address:
Voltage-gated sodium (Na) channels initiate action potentials in nerve, muscle, and other electrically excitable cells. The structural basis of voltage gating is uncertain because the resting state exists only at deeply negative membrane potentials. To stabilize the resting conformation, we inserted voltage-shifting mutations and introduced a disulfide crosslink in the VS of the ancestral bacterial sodium channel NaAb.
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