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Pharmaceuticals, Volume 13, Issue 4

April 2020 - 26 articles

Cover Story: Over the past two decades since the identification of the first gene mutation in idiopathic epilepsy in 1994, the detail pathomechanism of idiopathic epilepsy has yet to be clarified. A valid genetic animal model of epilepsy fulfilled by face, construct, and estimated validities is a powerful tool for understanding epileptogenesis/ictogenesis. The genetic model of autosomal dominant sleep-related hypermotor epilepsy, named S286L-TG, bearing a missense S286L-mutation of rat Chrna4 corresponding to an S284L mutation in human CHRNA4 provides information on ADSHE pathomechanisms. Hyperactivated glutamatergic transmission via GABAergic disinhibition induced by loss-of-function S286L mutant nicotinic acetylcholine receptor (nAChR) plays important roles in the epileptogenesis/ictogenesis. Unexpectedly, the loss-of-function S286L-mutant nAChR resulted in the upregulation/activation of the astroglial hemichannel. View this paper
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Articles (26)

  • Feature Paper
  • Article
  • Open Access
32 Citations
5,911 Views
13 Pages

Methanolic Extract of the Herb Ononis spinosa L. Is an Antifungal Agent with no Cytotoxicity to Primary Human Cells

  • Dejan Stojković,
  • Maria Inês Dias,
  • Danijela Drakulić,
  • Lillian Barros,
  • Milena Stevanović,
  • Isabel C. F. R. Ferreira and
  • Marina D. Soković

Ononis spinosa L. is a plant traditionally used as folk remedy. There are numerous studies regarding chemical constituents and health beneficial properties of Ononidis Radix. The following study was designed to investigate chemical composition and an...

  • Review
  • Open Access
39 Citations
7,429 Views
21 Pages

Atomic in vivo nanogenerators such as actinium-225, thorium-227, and radium-223 are of increasing interest and importance in the treatment of patients with metastatic cancer diseases. This is due to their peculiar physical, chemical, and biological c...

  • Article
  • Open Access
14 Citations
6,270 Views
17 Pages

Drug Conjugates for Targeting Eph Receptors in Glioblastoma

  • Puja Sharma,
  • Callie Roberts,
  • Denise Herpai,
  • Izabela D. Fokt,
  • Waldemar Priebe and
  • Waldemar Debinski

Glioblastoma (GBM) is a complex and heterogeneous tumor that warrants a comprehensive therapeutic approach for treatment. Tumor-associated antigens offer an opportunity to selectively target various components of the GBM microenvironment while sparin...

  • Review
  • Open Access
16 Citations
9,861 Views
10 Pages

Mutations in the cystic fibrosis transmembrane conductance regulator (CFTR) gene decrease the structural stability and function of the CFTR protein, resulting in cystic fibrosis. Recently, the effect of CFTR-targeting combination therapy has dramatic...

  • Review
  • Open Access
23 Citations
6,815 Views
19 Pages

Selective Degradation of Target Proteins by Chimeric Small-Molecular Drugs, PROTACs and SNIPERs

  • Minoru Ishikawa,
  • Shusuke Tomoshige,
  • Yosuke Demizu and
  • Mikihiko Naito

New therapeutic modalities are needed to address the problem of pathological but undruggable proteins. One possible approach is the induction of protein degradation by chimeric drugs composed of a ubiquitin ligase (E3) ligand coupled to a ligand for...

  • Communication
  • Open Access
39 Citations
6,899 Views
9 Pages

Identification and Quantification of Stilbenes (Piceatannol and Resveratrol) in Passiflora edulis By-Products

  • Karolline Krambeck,
  • Ana Oliveira,
  • Delfim Santos,
  • Maria Manuela Pintado,
  • João Baptista Silva,
  • José Manuel Sousa Lobo and
  • Maria Helena Amaral

Recently, studies on the by-products from the food industry, such as passion fruit seeds, have significantly increased, as these can have an added value, due to their properties, such as potential antioxidant activity. This study was conducted to det...

  • Article
  • Open Access
3 Citations
3,112 Views
11 Pages

Electroanalysis Applied to Compatibility and Stability Assays of Drugs: Carvedilol Study Case

  • Murilo Ferreira de Carvalho,
  • Luane Ferreira Garcia,
  • Isaac Yves Lopes de Macedo,
  • Ricardo Neves Marreto,
  • Mayk Teles de Oliveira,
  • Renê Oliveira do Couto,
  • Carlos Eduardo Peixoto da Cunha,
  • Karla Carneiro de Siqueira Leite,
  • Kênnia Rocha Rezende and
  • Fabio Bahls Machado
  • + 2 authors

Carvedilol (CRV) is a non-selective blocker of α and β adrenergic receptors, which has been extensively used for the treatment of hypertension and congestive heart failure. Owing to its poor biopharmaceutical properties, CRV has been incor...

  • Article
  • Open Access
19 Citations
4,905 Views
14 Pages

Antioxidant, Anti-Inflammatory, and Antidiabetic Activities of Leaves and Stems of Uapaca bojeri Bail. (EUPHORBIACEAE), an Endemic Plant of Madagascar

  • Zoarilala Rinah Razafindrakoto,
  • Dario Donno,
  • Nantenaina Tombozara,
  • Harilala Andriamaniraka,
  • Charles Andrianjara,
  • David Ramanitrahasimbola and
  • Gabriele Loris Beccaro

Uapaca bojeri is an endemic Malagasy plant used by the local population. This work aimed to evaluate antioxidant, anti-inflammatory, and antidiabetic activities of the methanol extracts of U. bojeri leaves and stems and to report their total phenolic...

  • Article
  • Open Access
1 Citations
3,402 Views
11 Pages

Evaluation of the Anti-Tumor Activity of Small Molecules Targeting Eph/Ephrins in APC min/J Mice

  • Miriam Corrado,
  • Carmine Giorgio,
  • Elisabetta Barocelli,
  • Giuseppe Vittucci Marzetti,
  • Anna Maria Cantoni,
  • Rosanna Di Lecce,
  • Matteo Incerti,
  • Riccardo Castelli,
  • Alessio Lodola and
  • Massimiliano Tognolini

The Eph receptors are the largest receptors tyrosine kinases (RTKs) family in humans and together with ephrin ligands constitute a complex cellular communication system often dysregulated in many tumors. The role of the Eph-ephrin system in colorecta...

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Pharmaceuticals - ISSN 1424-8247