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Pharmaceuticals, Volume 9, Issue 2

2016 June - 17 articles

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Articles (17)

  • Review
  • Open Access
99 Citations
12,608 Views
11 Pages

Tumor heterogeneity has been compared with Darwinian evolution and survival of the fittest. The evolutionary ecosystem of tumors consisting of heterogeneous tumor cell populations represents a considerable challenge to tumor therapy, since all geneti...

  • Article
  • Open Access
24 Citations
7,721 Views
10 Pages

Novel esters of γ-aminobutyric acid (GABA) with monocyclic terpenes were synthesized via Steglich esterification and characterized by 1H-NMR, IR and mass spectral studies. Their anticonvulsant, analgesic and anti-inflammatory activities were evaluate...

  • Article
  • Open Access
11 Citations
5,982 Views
13 Pages

Objectives: Fibrosis is involved in many chronic diseases. It affects the functionality of vital organs, such as liver, lung, heart and kidney. Two novel imaging agents for positron emission tomography (PET) imaging of fibrosis have previously pre-cl...

  • Article
  • Open Access
16 Citations
5,149 Views
13 Pages

Staphylococcus aureus (SA) colonizes the vast majority of patients with atopic dermatitis (AD). Its resistance to antibiotics and ability to form biofilms are the main origins of therapeutic complications. Endogenous antimicrobial peptides (AMPs) exh...

  • Article
  • Open Access
14 Citations
5,036 Views
11 Pages

Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide

  • Alexey P. Sarapultsev,
  • Oleg N. Chupakhin,
  • Petr A. Sarapultsev,
  • Larisa P. Sidorova and
  • Tatiana A. Tseitler

Substituted thiadiazines exert a reliable therapeutic effect in treating stress, and a schematic description of their ability to influence all aspects of a stress response has been depicted. This study was conducted to pharmacologically evaluate comp...

  • Review
  • Open Access
8 Citations
5,497 Views
12 Pages

Pediatric Non-Hodgkin Lymphomas (NHL) are a diverse group of malignancies and as such treatment can vary based on the different biological characteristics of each malignancy. Significant advancements are being made in the treatment and outcomes of th...

  • Article
  • Open Access
57 Citations
10,160 Views
21 Pages

Improved Aptamers for the Diagnosis and Potential Treatment of HER2-Positive Cancer

  • Marlies Gijs,
  • Gregory Penner,
  • Garth B. Blackler,
  • Nathalie R.E.N. Impens,
  • Sarah Baatout,
  • André Luxen and
  • An M. Aerts

Aptamers provide a potential source of alternative targeting molecules for existing antibody diagnostics and therapeutics. In this work, we selected novel DNA aptamers targeting the HER2 receptor by an adherent whole-cell SELEX approach. Individual a...

  • Review
  • Open Access
15 Citations
11,262 Views
16 Pages

“Greening” a chemical transformation is not about only changing the nature of a solvent or decreasing the reaction temperature. There are metrics enabling a critical quantification of the efficiency of an experimental protocol. Some of them are appli...

  • Feature Paper
  • Review
  • Open Access
34 Citations
13,218 Views
33 Pages

Chemical Variations on the p53 Reactivation Theme

  • Carlos J. A. Ribeiro,
  • Cecília M. P. Rodrigues,
  • Rui Moreira and
  • Maria M. M. Santos

Among the tumor suppressor genes, p53 is one of the most studied. It is widely regarded as the “guardian of the genome”, playing a major role in carcinogenesis. In fact, direct inactivation of the TP53 gene occurs in more than 50% of malignancies, an...

  • Feature Paper
  • Review
  • Open Access
20 Citations
9,093 Views
20 Pages

Unexploited Antineoplastic Effects of Commercially Available Anti-Diabetic Drugs

  • Panagiota Papanagnou,
  • Theodora Stivarou and
  • Maria Tsironi

The development of efficacious antitumor compounds with minimal toxicity is a hot research topic. Numerous cancer cell targeted agents are evaluated daily in laboratories for their antitumorigenicity at the pre-clinical level, but the process of thei...

  • Article
  • Open Access
22 Citations
5,953 Views
12 Pages

The use of a combined therapy with low doses of estrogens plus antidepressants to treat depression associated to perimenopause could be advantageous. However the use of these combinations is controversial due to several factors, including the time of...

  • Article
  • Open Access
18 Citations
7,218 Views
14 Pages

Evaluating the Role of p38 MAPK in the Accelerated Cell Senescence of Werner Syndrome Fibroblasts

  • Terence Davis,
  • Amy J. C. Brook,
  • Michal J. Rokicki,
  • Mark C. Bagley and
  • David Kipling

Progeroid syndromes show features of accelerated ageing and are used as models for human ageing, of which Werner syndrome (WS) is one of the most widely studied. WS fibroblasts show accelerated senescence that may result from p38 MAP kinase activatio...

  • Article
  • Open Access
14 Citations
7,039 Views
15 Pages

Development of a New Radiofluorinated Quinoline Analog for PET Imaging of Phosphodiesterase 5 (PDE5) in Brain

  • Jianrong Liu,
  • Barbara Wenzel,
  • Sladjana Dukic-Stefanovic,
  • Rodrigo Teodoro,
  • Friedrich-Alexander Ludwig,
  • Winnie Deuther-Conrad,
  • Susann Schröder,
  • Jean-Michel Chezal,
  • Emmanuel Moreau and
  • Aurélie Maisonial-Besset
  • + 1 author

Phosphodiesterases (PDEs) are enzymes that play a major role in cell signalling by hydrolysing the secondary messengers cyclic adenosine monophosphate (cAMP) and/or cyclic guanosine monophosphate (cGMP) throughout the body and brain. Altered cyclic n...

  • Article
  • Open Access
6 Citations
5,349 Views
11 Pages

Alkanediamide-Linked Bisbenzamidines Are Promising Antiparasitic Agents

  • Jean Jacques Vanden Eynde,
  • Annie Mayence,
  • Madhusoodanan Mottamal,
  • Cyrus J. Bacchi,
  • Nigel Yarlett,
  • Marcel Kaiser,
  • Reto Brun and
  • Tien L. Huang

A series of 15 alkanediamide-linked bisbenzamidines and related analogs was synthesized and tested in vitro against two Trypanosoma brucei (T.b.) subspecies: T.b. brucei and T.b. rhodesiense, Trypanosoma cruzi, Leishmania donovani and two Plasmodium ...

  • Article
  • Open Access
6 Citations
6,082 Views
14 Pages

Search for Potent and Selective Aurora A Inhibitors Based on General Ser/Thr Kinase Pharmacophore Model

  • Natalya I. Vasilevich,
  • Victor V. Tatarskiy,
  • Elena A. Aksenova,
  • Denis N. Kazyulkin and
  • Ilya I. Afanasyev

Based on the data for compounds known from the literature to be active against various types of Ser/Thr kinases, a general pharmachophore model for these types of kinases was developed. The search for the molecules fitting to this pharmacophore among...

  • Article
  • Open Access
13 Citations
6,764 Views
14 Pages

A Selenium Containing Inhibitor for the Treatment of Hepatocellular Cancer

  • Hephzibah Rani S. Tagaram,
  • Dhimant Desai,
  • Guangfu Li,
  • Dai Liu,
  • C. Bart Rountree,
  • Kavitha Gowda,
  • Arthur Berg,
  • Shantu Amin,
  • Kevin F. Staveley-O’Carroll and
  • Eric T. Kimchi

Hepatocellular carcinoma (HCC) is the third most deadly cancer in the world. New treatment strategies are desperately needed due to limited standard therapies. Activation of the Erk, Akt, and STAT3pathways is implicated in the prognosis of HCC. The S...

  • Review
  • Open Access
26 Citations
10,905 Views
18 Pages

Aspirin (ASA) and non-steroidal anti-inflammatory drugs (NSAIDs) are a mainstay of therapy for the treatment of idiopathic pericarditis (IP). A comprehensive review consisting of pertinent clinical literature, pharmacokinetic, and pharmacodynamic con...

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Pharmaceuticals - ISSN 1424-8247