Month: September 2022

TRIGGERED ALARM RESPONSE. "Activation of TRPA1 can cause extreme irritation, lacrimation, coughing, bronchial contraction and depressed respiration. Therefore, potent electrophilic compounds (for example, 1-chloroacetophenone, dibenz[b,f][1,4]-oxazepine, 2-chlorobenzylidene malononitrile, and chloropicrin) are used as tear gases and riot control agents." https://lnkd.in/e-WBvC9 View in LinkedIn

ROLE IN PAIN. "A clear role for TRPA1 in pain transduction is established...Furthermore, the role of TRPA1 in pain signaling is underscored by its involvement in an autosomal familial episodic pain syndrome, migraine headaches, and other human pain disorders." https://lnkd.in/e-WBvC9 View in LinkedIn

PSYCHIATRIC LINK. "Transient receptor potential vanilloid 1 (TRPV1) and TRP ankyrin 1 (TRPA1) are involved in many biological processes, including nociception and hyperalgesia. Whereas the involvement of TRPV1 in psychiatric disorders such as anxiety and depression has been reported, little is known regarding the role of TRPA1 in these conditions." https://lnkd.in/e-Efbhd View in LinkedIn

BLOCKING TRPA1. "Genetic deletion or pharmacological blockade of TRPA1 produces inhibitory activity in mouse models of anxiety and depression. These results imply that TRPA1 exerts tonic control, promoting anxiety and depression, and that TRPA1 antagonism has potential as an innovative strategy for the treatment of anxiety and mood disorders." https://lnkd.in/e-Efbhd View in LinkedIn

ANTAGONISTS. "The importance of TRPA1 in pain signaling makes it a potential target for the treatment of pathological pain. While some small-molecule TRPA1 antagonists have been identified, no peptide antagonists of TRPA1 have been reported." https://lnkd.in/ecaVp5Q View in LinkedIn

VENOM ANTAGONISTS. "The venoms of predators, such as spiders, scorpions, cone snails, sea anemones, and snakes, have been an excellent source of peptide diversity for drug discovery and as pharmacological tools for elucidating the structure, function, and physiological properties of ion channels." https://lnkd.in/ecaVp5Q View in LinkedIn

VENOM PAYLOAD. "A key issue in ion channel toxin biology has been the mining of this great pharmacological diversity—e.g., spiders alone are estimated to collectively contain millions of distinct peptide toxins in their venoms —to identify toxins with high affinity for particular ion channel targets." https://lnkd.in/ecaVp5Q View in LinkedIn

TOXINEERING. "The researchers identified a tarantula spider peptide, protoxin-I, as the first high-affinity peptide antagonist of the transient receptor potential ankyrin 1 (TRPA1) channel. Nitabach’s team also used toxineering to create a novel protoxin-I mutant with improved specificity for TRPA1, underscoring the value of the approach for pharmaceutical discovery." https://lnkd.in/eQA7Yck View in LinkedIn

DIVERSE ACTIVATORS AND OUTCOMES. "TRPA1 was found to be activated by a variety of chemical compounds, including mustard oil and cannabinoids. Subsequent studies identified additional ligands and revealed roles in pain, inflammation, itch, mechanical sensation, oxygen regulation, and more." https://lnkd.in/e-WBvC9 View in LinkedIn

RADS, ASTHMA, COPD. "In addition to directly activating a cough reflex, TRPA1 ligands may also be involved in the hypersensitization of cough and other sensory reflexes." https://lnkd.in/ey47aVM View in LinkedIn