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Unbound Medicine.
(trifluoperazine hydrochloride)
5,156 results
  • Targeting Aquaporin-4 Subcellular Localization to Treat Central Nervous System Edema. [Journal Article]
    Cell. 2020 May 14; 181(4):784-799.e19.Kitchen P, Salman MM, … Bill RM
  • Swelling of the brain or spinal cord (CNS edema) affects millions of people every year. All potential pharmacological interventions have failed in clinical trials, meaning that symptom management is the only treatment option. The water channel protein aquaporin-4 (AQP4) is expressed in astrocytes and mediates water flux across the blood-brain and blood-spinal cord barriers. Here we show that AQP4…
  • The effect of neuroleptic drugs on DPPC/sphingomyelin/cholesterol membranes. [Journal Article]
    Chem Phys Lipids. 2020 Jul; 229:104913.Pérez-Isidoro R, Costas M
  • The hydrophobic nature of neuroleptic drugs renders that these molecules interact not only with protein receptors, but also with the lipids constituting the membrane bilayer. We present a systematic study of the effect of seven neuroleptic drugs on a biomembrane model composed of DPPC, sphingomyelin, and cholesterol. Differential scanning calorimetry (DSC) measurements were used to monitor the ge…
  • Competition Between Phenothiazines and BH3 Peptide for the Binding Site of the Antiapoptotic BCL-2 Protein. [Journal Article]
    Front Chem. 2020; 8:235.do Carmo AL, Bettanin F, … Honorio KM
  • The study of proteins and mechanisms involved in the apoptosis and new knowledge about cancer's biology are essential for planning new drugs. Tumor cells develop several strategies to gain proliferative advantages, including molecular alterations to evade from apoptosis. Failures in apoptosis could contribute to cancer pathogenesis, since these defects can cause the accumulation of dividing cells…
  • New Host-Directed Therapeutics for the Treatment of Clostridioides difficile Infection. [Journal Article]
    mBio. 2020 Mar 10; 11(2)Andersson JA, Peniche AG, … Dann SM
  • Frequent and excessive use of antibiotics primes patients to Clostridioides difficile infection (CDI), which leads to fatal pseudomembranous colitis, with limited treatment options. In earlier reports, we used a drug repurposing strategy and identified amoxapine (an antidepressant), doxapram (a breathing stimulant), and trifluoperazine (an antipsychotic), which provided significant protection to …
  • Antimicrobial Properties on Non-Antibiotic Drugs in the Era of Increased Bacterial Resistance. [Review]
    Antibiotics (Basel). 2020 Mar 02; 9(3)Lagadinou M, Onisor MO, … Marangos M
  • In recent years, due to the dramatic increase in and global spread of bacterial resistance to a number of commonly used antibacterial agents, many studies have been directed at investigating drugs whose primary therapeutic purpose is not antimicrobial action. In an era where it is becoming increasingly difficult to find new antimicrobial drugs, it is important to understand these antimicrobial ef…
  • Molecular characterization of functional UDP-glucuronosyltransferases 1A and 2B in common marmosets. [Journal Article]
    Biochem Pharmacol. 2020 Feb; 172:113748.Uno Y, Uehara S, … Yamazaki H
  • UDP-glucuronosyltransferases (UGTs) are essential drug-conjugation enzymes that metabolize a variety of endobiotic and xenobiotic substrates. The molecular characteristics of UGTs have been extensively investigated in humans, but remain to be investigated in common marmosets, a nonhuman primate species widely used in drug metabolism studies. In this study, 11 UGT cDNAs (UGT1A1, 1A3, 1A4, 1A6, 1A7…
  • Dissecting the Anticancer Mechanism of Trifluoperazine on Pancreatic Ductal Adenocarcinoma. [Journal Article]
    Cancers (Basel). 2019 Nov 26; 11(12)Huang C, Lan W, … Santofimia-Castaño P
  • Pancreatic ductal adenocarcinoma (PDAC) is one of the most aggressive cancers with almost no curative chemotherapeutic treatment. Besides the development of new compounds, repurposing of approved drugs to treat cancer, alone or in combination, has become an attractive strategy, showing many therapeutic and economic advantages. However, it is necessary to improve our knowledge about the mechanism …
  • Targeting the Stress-Induced Protein NUPR1 to Treat Pancreatic Adenocarcinoma. [Review]
    Cells. 2019 11 17; 8(11)Santofimia-Castaño P, Xia Y, … Iovanna J
  • Cancer cells activate stress-response mechanisms to adapt themselves to a variety of stressful conditions. Among these protective mechanisms, those controlled by the stress-induced nuclear protein 1 (NUPR1) belong to the most conserved ones. NUPR1 is an 82-residue-long, monomeric, basic and intrinsically disordered protein (IDP), which was found to be invariably overexpressed in some, if not all,…
  • Computational Biology: Toward Early Detection of Pancreatic Cancer. [Journal Article]
    Crit Rev Oncog. 2019; 24(2):191-198.Gupta MK, Sarojamma V, … Vadde R
  • Pancreatic cancer is the eleventh most common cancer type and the seventh leading cause of cancer mortality globally. Although chemotherapy is widely employed in the treatment of any cancer type, the response rate in pancreatic cancer is very low. Hence, new and effective techniques in the treatment of pancreatic cancer are needed. Recent advances in molecular profiling as well as high-throughput…
  • LiverTox: Clinical and Research Information on Drug-Induced Liver Injury: Antipsychotic Agents [BOOK]
    . National Institute of Diabetes and Digestive and Kidney Diseases: Bethesda (MD)BOOK
  • Psychotic disorders include schizophrenia, the manic phase of manic-depressive illness (bipolar illness), acute psychosis and other conditions marked by acute, severe agitation. The antipsychotic medications are invaluable adjuncts to the treatment of psychosis and bipolar illness and have revolutionized management of these conditions. The antipsychotic agents in clinical use include the phenothi…
  • Antipsychotic Drug Trifluoperazine Suppresses Colorectal Cancer by Inducing G0/G1 Arrest and Apoptosis. [Journal Article]
    Front Pharmacol. 2019; 10:1029.Xia Y, Jia C, … Ye T
  • Repurposing existing drugs for cancer treatment is an effective strategy. An approved antipsychotic drug, trifluoperazine (TFP), has been reported to have potential anticancer effects against several cancer types. Here, we investigated the effect and molecular mechanism of TFP in colorectal cancer (CRC). In vitro studies showed that TFP induced G0/G1 cell cycle arrest to dramatically inhibit CRC …
  • Design, synthesis and evaluation of novel phenothiazine derivatives as inhibitors of breast cancer stem cells. [Review]
    Eur J Med Chem. 2019 Dec 01; 183:111692.Gao Y, Sun TY, … Bai CG
  • A novel series of phenothiazine derivatives containing diethanolamine, methoxyethylamine, flavonoids, and a nitric oxide (NO) donor was designed and synthesized for the treatment of breast cancer. Phenothiazine derivatives (l) did not noticeably inhibit the growth of SUM159, MDA-MB-231, MCF-7, and SKBR-3 cells, whereas phenothiazine derivatives (ll) containing the NO donor were more potent or had…
  • Effects of antidepressant and antipsychotic use on weight gain: A systematic review. [Review]
    Obes Rev. 2019 12; 20(12):1680-1690.Alonso-Pedrero L, Bes-Rastrollo M, Marti A
  • Weight gain is an adverse effect of antidepressants and antipsychotics. This side effect can lead to numerous comorbidities and reduces life expectancy. The use of these drugs is increasing worldwide, and the weight gain produced by them represents a common clinical challenge. The goal of this systematic review was to evaluate the potential association of antidepressant and antipsychotic therapy …
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