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625 results
  • Searching for Novel Noncovalent Nuclear Export Inhibitors through a Drug Repurposing Approach. [Journal Article]
    J Med Chem. 2023 Jan 26; 66(2):1574-1582.Huang W, Wang JX, … Sun Q
  • Chromosomal region maintenance protein 1 (CRM1) is a validated anticancer drug target, and its covalent inhibitor KPT-330 has been approved for marketing. However, the development of CRM1 inhibitors, especially the noncovalent ones, is still very limited. Drug repurposing is an effective strategy to develop drug leads for new targets. In this work, we virtually screened a library of marketed drug…
  • StatPearls: Leukotriene Receptor Antagonists [BOOK]
    StatPearls. StatPearls Publishing: Treasure Island (FL)ChoiJaehwaJMercer University School of MedicineAzmatChaudhary EhtshamCERawalpindi Medical College and Allied HospitalsBOOK
  • Montelukast and zafirlukast are cysteinyl leukotriene receptor antagonists indicated for the prevention and treatment of chronic asthma. This activity will highlight the mechanism of action, adverse event profile, and monitoring pertinent for members of the interprofessional team in the management of patients with asthma and related conditions with leukotriene receptor antagonists.
  • Torasemide-induced Vascular Purpura in the Course of Eosinophilic Granulomatosis with Polyangiitis. [Case Reports]
    Acta Dermatovenerol Croat. 2022 Sep; 30(2):116-118.Frątczak A, Polak K, … Bergler-Czop B
  • Torasemide is a loop diuretic with a molecule that is chemically similar to the sulphonamides described as eosinophilic granulomatosis with polyangiitis (EGPA) triggering drugs. The presented case is probably the first description of torasemide-induced vascular purpura in the course of EGPA. Any diagnosis of vasculitis should be followed by an identification of drugs that may aggravate the diseas…
  • Lupeol and pristimerin do not inhibit activation of the human sperm CatSper Ca(2+)-channel. [Journal Article]
    F1000Res. 2022; 11:222.Rehfeld A, Marcus Pedersen C
  • Opposing findings have been published on the regulation of the sperm-specific Ca 2+ channel CatSper (cation channel of sperm) in human sperm cells by the plant triterpenoids lupeol and pristimerin. While the original study on this topic found these triterpenoids to act as potent inhibitors of human CatSper, subsequent studies have failed to replicate such an inhibitory effect. It has been suggest…
  • StatPearls: Zafirlukast [BOOK]
    StatPearls. StatPearls Publishing: Treasure Island (FL)DhaliwalAmareenABoston University School of MedicineBajajTusharTUCLA-Kern MedicalBOOK
  • Zafirlukast is a medication used in the management and treatment of chronic asthma. It is in the leukotriene receptor antagonist class. This activity reviews the indications, action, and contraindications for zafirlukast as an agent in the management and prophylaxis of chronic asthma. This activity will highlight the mechanism of action, adverse event profile, and other vital factors pertinent to…
  • Structured solubility behaviour in bioequivalent fasted simulated intestinal fluids. [Journal Article]
    Eur J Pharm Biopharm. 2022 Jul; 176:108-121.Abuhassan Q, Khadra I, … Halbert GW
  • Drug solubility in intestinal fluid is a key parameter controlling absorption after the administration of a solid oral dosage form. To measure solubility in vitro simulated intestinal fluids have been developed, but there are multiple recipes and the optimum is unknown. This situation creates difficulties during drug discovery and development research. A recent study characterised sampled fasted …
  • Choline-Amino Acid-Derived Bio-ionic Liquids for Solubility Enhancement of Zafirlukast. [Journal Article]
    AAPS PharmSciTech. 2022 May 18; 23(5):146.Gaikwad N, Kudal S, Avachat AM
  • This study investigated the application of bio-ionic liquids (ILs) prepared from choline as cation and amino acid as anion for solubility enhancement of poorly water-soluble drug, Zafirlukast (ZFL). Herein, the solubility of ZFL in water and mixtures of water and ILs was assessed using UV spectroscopy at two temperature points 25°C and 37°C with increasing concentrations of IL. ZFL solubility was…
  • A SWELL time to develop the molecular pharmacology of the volume-regulated anion channel (VRAC). [Review]
    Channels (Austin). 2022 12; 16(1):27-36.Figueroa EE, Denton JS
  • Newly emerging roles of LRRC8 volume-regulated anion channels (VRAC) raise important questions about the therapeutic potential of VRAC in the treatment of epilepsy, type 2 diabetes, and other human diseases. A critical barrier to evaluating whether VRAC represents a viable drug target is the lack of potent and specific small-molecule inhibitors and activators of the channel. Here we review recent…
  • Leukotriene Antagonists in Dermatology. [Journal Article]
    Indian J Dermatol. 2021 Sep-Oct; 66(5):575.Bubna AK
  • Leukotriene antagonists constitute an important group of drugs in the therapeutic armamentarium of all dermatologists. It has been quite valuable in the management of various types of urticaria and atopic dermatitis. Recently, the role of zileuton in the management of acne has been elaborated, and in the near future it could be used as a first-line agent for the same, thereby preventing adverse e…
  • Cysteinyl Leukotriene Pathway and Cancer. [Review]
    Int J Mol Sci. 2021 Dec 23; 23(1)Tsai MJ, Chang WA, … Hung JY
  • Cancer remains a leading cause of death worldwide, despite many advances being made in recent decades. Changes in the tumor microenvironment, including dysregulated immunity, may contribute to carcinogenesis and cancer progression. The cysteinyl leukotriene (CysLT) pathway is involved in several signal pathways, having various functions in different tissues. We summarized major findings of studie…
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