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Pharmaceuticals, Volume 10, Issue 2

2017 June - 25 articles

Cover Story: The transient receptor potential melastatin-subfamily member 7 (TRPM7) is a ubiquitously expressed ion channel with intrinsic kinase activity. Molecular and electrophysiological analyses of the structure and activity of TRPM7 have revealed functional coupling of its channel and kinase activity. Studies have indicated the important roles of TRPM7 channel-kinase in fundamental cellular processes, physiological responses, and embryonic development. Accumulating evidence has shown that TRPM7 is aberrantly expressed and/or activated in human diseases including cancer. TRPM7 plays a variety of functional roles in cancer cells including survival, cell cycle progression, proliferation, growth, migration, invasion, and epithelial-mesenchymal transition (EMT). Data from a study using mouse xenograft of human cancer show that TRPM7 is required for tumor growth and metastasis. View Paper here
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Articles (25)

  • Article
  • Open Access
12 Citations
6,064 Views
13 Pages

A Short-Term Biological Indicator for Long-Term Kidney Damage after Radionuclide Therapy in Mice

  • Giovanni Pellegrini,
  • Klaudia Siwowska,
  • Stephanie Haller,
  • Daniel J. Antoine,
  • Roger Schibli,
  • Anja Kipar and
  • Cristina Müller

Folate receptor (FR)-targeted radionuclide therapy using folate radioconjugates is of interest due to the expression of the FR in a variety of tumor types. The high renal accumulation of radiofolates presents, however, a risk of radionephropathy. A p...

  • Article
  • Open Access
7 Citations
6,797 Views
18 Pages

Exploring Wound-Healing Genomic Machinery with a Network-Based Approach

  • Francesca Vitali,
  • Simone Marini,
  • Martina Balli,
  • Hanne Grosemans,
  • Maurilio Sampaolesi,
  • Yves A. Lussier,
  • Maria Gabriella Cusella De Angelis and
  • Riccardo Bellazzi

The molecular mechanisms underlying tissue regeneration and wound healing are still poorly understood despite their importance. In this paper we develop a bioinformatics approach, combining biology and network theory to drive experiments for better u...

  • Article
  • Open Access
132 Citations
14,256 Views
28 Pages

In the context of radiopharmacy and molecular imaging, the concept of theranostics entails a therapy-accompanying diagnosis with the aim of a patient-specific treatment. Using the adequate diagnostic radiopharmaceutical, the disease and the state of...

  • Article
  • Open Access
30 Citations
8,693 Views
10 Pages

In Vitro and In Vivo Studies of Alar-Nasal Cartilage Using Autologous Micro-Grafts: The Use of the Rigenera® Protocol in the Treatment of an Osteochondral Lesion of the Nose

  • Gabriele Ceccarelli,
  • Pietro Gentile,
  • Marco Marcarelli,
  • Martina Balli,
  • Flavio Lorenzo Ronzoni,
  • Laura Benedetti and
  • Maria Gabriella Cusella De Angelis

Cartilage defects represent a serious problem due to the poor regenerative properties of this tissue. Regarding the nose, nasal valve collapse is associated with nasal blockage and persistent airway obstruction associated with a significant drop in t...

  • Review
  • Open Access
36 Citations
10,396 Views
53 Pages

The Good the Bad and the Ugly of Glycosaminoglycans in Tissue Engineering Applications

  • Bethanie I. Ayerst,
  • Catherine L.R. Merry and
  • Anthony J. Day

High sulfation, low cost, and the status of heparin as an already FDA- and EMA- approved product, mean that its inclusion in tissue engineering (TE) strategies is becoming increasingly popular. However, the use of heparin may represent a naïve approa...

  • Article
  • Open Access
5 Citations
6,658 Views
16 Pages

Anti-Mycobacterial Evaluation of 7-Chloro-4-Aminoquinolines and Hologram Quantitative Structure–Activity Relationship (HQSAR) Modeling of Amino–Imino Tautomers

  • Marcelle L. F. Bispo,
  • Camilo H. S. Lima,
  • Laura N. F. Cardoso,
  • André L. P. Candéa,
  • Flávio A. F. M. Bezerra,
  • Maria C. S. Lourenço,
  • Maria G. M. O. Henriques,
  • Ricardo B. Alencastro,
  • Carlos R. Kaiser and
  • Magaly G. Albuquerque
  • + 1 author

In an ongoing research program for the development of new anti-tuberculosis drugs, we synthesized three series (A, B, and C) of 7-chloro-4-aminoquinolines, which were evaluated in vitro against Mycobacterium tuberculosis (MTB). Now, we report the ant...

  • Review
  • Open Access
44 Citations
9,509 Views
17 Pages

Advances in Drug Discovery of New Antitubercular Multidrug-Resistant Compounds

  • Guilherme Felipe dos Santos Fernandes,
  • Chung Man Chin and
  • Jean Leandro Dos Santos

Tuberculosis (TB), a disease caused mainly by the Mycobacterium tuberculosis (Mtb), is according to the World Health Organization (WHO) the infectious disease responsible for the highest number of deaths worldwide. The increased number of multidrug-r...

  • Article
  • Open Access
32 Citations
8,473 Views
13 Pages

Chiral Derivatives of Xanthones: Investigation of the Effect of Enantioselectivity on Inhibition of Cyclooxygenases (COX-1 and COX-2) and Binding Interaction with Human Serum Albumin

  • Carla Fernandes,
  • Andreia Palmeira,
  • Inês I. Ramos,
  • Carlos Carneiro,
  • Carlos Afonso,
  • Maria Elizabeth Tiritan,
  • Honorina Cidade,
  • Paula C.A.G. Pinto,
  • M. Lúcia M.F.S. Saraiva and
  • Madalena M.M. Pinto
  • + 1 author

Searching of new enantiomerically pure chiral derivatives of xanthones (CDXs) with potential pharmacological properties, particularly those with anti-inflammatory activity, has remained an area of interest of our group. Herein, we describe in silico...

  • Article
  • Open Access
9 Citations
6,004 Views
11 Pages

Dysregulated expression or activation of matrix metalloproteinases (MMPs) is observed in many kinds of live-threatening diseases. Therefore, MMP imaging for example with radiolabelled MMP inhibitors (MMPIs) potentially represents a valuable tool for...

  • Review
  • Open Access
7 Citations
7,439 Views
14 Pages

PKC in Regenerative Therapy: New Insights for Old Targets

  • Marta Rui,
  • Rita Nasti,
  • Emanuele Bignardi,
  • Serena Della Volpe,
  • Giacomo Rossino,
  • Daniela Rossi and
  • Simona Collina

Effective therapies for chronic or non-healing wounds are still lacking. These tissue insults often result in severe clinical complications (i.e., infections and/or amputation) and sometimes lead to patient death. Accordingly, several research groups...

  • Article
  • Open Access
27 Citations
8,716 Views
10 Pages

Esters based on mono- and bicyclic terpenoids with glycine have been synthesized via Steglich esterification and characterized by 1H-NMR, IR, and mass spectral studies. Their analgesic and anti-inflammatory activities were investigated after transder...

  • Review
  • Open Access
52 Citations
9,196 Views
12 Pages

Novel Radiolabeled Bisphosphonates for PET Diagnosis and Endoradiotherapy of Bone Metastases

  • Nina Pfannkuchen,
  • Marian Meckel,
  • Ralf Bergmann,
  • Michael Bachmann,
  • Chandrasekhar Bal,
  • Mike Sathekge,
  • Wolfgang Mohnike,
  • Richard P. Baum and
  • Frank Rösch

Bone metastases, often a consequence of breast, prostate, and lung carcinomas, are characterized by an increased bone turnover, which can be visualized by positron emission tomography (PET), as well as single-photon emission computed tomography (SPEC...

  • Review
  • Open Access
50 Citations
11,332 Views
24 Pages

Flaviviruses are enveloped, positive single stranded ribonucleic acid (RNA) viruses with various routes of transmission. While the type and severity of symptoms caused by pathogenic flaviviruses vary from hemorrhagic fever to fetal abnormalities, the...

  • Article
  • Open Access
16 Citations
6,922 Views
18 Pages

Glycosaminoglycan Binding and Non-Endocytic Membrane Translocation of Cell-Permeable Octaarginine Monitored by Real-Time In-Cell NMR Spectroscopy

  • Yuki Takechi-Haraya,
  • Kenzo Aki,
  • Yumi Tohyama,
  • Yuichi Harano,
  • Toru Kawakami,
  • Hiroyuki Saito and
  • Emiko Okamura

Glycosaminoglycans (GAGs), which are covalently-linked membrane proteins at the cell surface have recently been suggested to involve in not only endocytic cellular uptake but also non-endocytic direct cell membrane translocation of arginine-rich cell...

  • Article
  • Open Access
26 Citations
5,456 Views
12 Pages

The synthesis and characterization of biotinylated chlorin photosensitizer and the corresponding zinc and indium complexes are described for potential applications in photodynamic therapy (PDT) for cancer. Phototoxicity of the biotin-chlorin conjugat...

  • Review
  • Open Access
43 Citations
11,135 Views
39 Pages

The unfolded protein response is responsible for the detection of misfolded proteins and the coordination of their disposal and is necessary to maintain the cellular homoeostasis. Multiple myeloma cells secrete large amounts of immunoglobulins, prote...

  • Review
  • Open Access
80 Citations
10,280 Views
15 Pages

The transient receptor potential melastatin-subfamily member 7 (TRPM7) is a ubiquitously expressed ion channel with intrinsic kinase activity. Molecular and electrophysiological analyses of the structure and activity of TRPM7 have revealed functional...

  • Article
  • Open Access
28 Citations
12,216 Views
15 Pages

Systematic Analysis of Pharmaceutical Preparations of Chondroitin Sulfate Combined with Glucosamine

  • Gustavo R.C. Santos,
  • Adriana A. Piquet,
  • Bianca F. Glauser,
  • Ana M.F. Tovar,
  • Mariana S. Pereira,
  • Eduardo Vilanova and
  • Paulo A.S. Mourão

Glycosaminoglycans are carbohydrate-based compounds widely employed as nutraceuticals or prescribed drugs. Oral formulations of chondroitin sulfate combined with glucosamine sulfate have been increasingly used to treat the symptoms of osteoarthritis...

  • Article
  • Open Access
19 Citations
7,106 Views
19 Pages

Development of a Glycosaminoglycan Derived, Selectin Targeting Anti-Adhesive Coating to Treat Endothelial Cell Dysfunction

  • James R. Wodicka,
  • Andrea M. Chambers,
  • Gurneet S. Sangha,
  • Craig J. Goergen and
  • Alyssa Panitch

Endothelial cell (EC) dysfunction is associated with many disease states including deep vein thrombosis (DVT), chronic kidney disease, sepsis and diabetes. Loss of the glycocalyx, a thin glycosaminoglycan (GAG)-rich layer on the EC surface, is a key...

  • Review
  • Open Access
31 Citations
16,411 Views
15 Pages

The indispensable roles of dermatan sulfate-proteoglycans (DS-PGs) have been demonstrated in various biological events including construction of the extracellular matrix and cell signaling through interactions with collagen and transforming growth fa...

  • Review
  • Open Access
9 Citations
6,306 Views
8 Pages

Modulation of TRP Channel Activity by Hydroxylation and Its Therapeutic Potential

  • Yagnesh Nagarajan,
  • Grigori Y. Rychkov and
  • Daniel J. Peet

Two transient receptor potential (TRP) channels—TRPA1 and TRPV3—are post-translationally hydroxylated, resulting in oxygen-dependent regulation of channel activity. The enzymes responsible are the HIF prolyl hydroxylases (PHDs) and the asparaginyl hy...

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Pharmaceuticals - ISSN 1424-8247