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Pharmaceuticals, Volume 13, Issue 10

2020 October - 64 articles

Cover Story: This paper describes how novel anti-EGFR antibody-drug conjugates (ABT-414, ABBV-221, and ABBV-321) that selectively target a tumor-selective (mAb806) epitope were evaluated for the treatment of malignant mesothelioma. EGFR and mAb806 epitope expression in malignant mesothelioma cell lines was confirmed using in vitro assays. Biodistribution and imaging studies demonstrated specific targeting of malignant mesothelioma tumors using an 89Zr-labeled immunoconjugate-ch806. In vivo therapy studies were conducted in malignant mesothelioma xenograft and PDX tumor models. ABT-414, ABBV-221, and ABBV-322 resulted in significant growth inhibition in tumors with high EGFR and mAb806 epitope expression. In contrast, in an EGFR expressing PDX model that was negative for the mAb806 epitope, no growth inhibition was observed. View this paper.
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Articles (64)

  • Article
  • Open Access
19 Citations
5,041 Views
28 Pages

Novel Sulfonamide-Based Analogs of Metformin Exert Promising Anti-Coagulant Effects without Compromising Glucose-Lowering Activity

  • Magdalena Markowicz-Piasecka,
  • Adrianna Sadkowska,
  • Joanna Sikora,
  • Marlena Broncel and
  • Kristiina M. Huttunen

21 October 2020

Metformin, one of the most frequently prescribed oral anti-diabetic drugs, is characterized by multidirectional activity, including lipid lowering, cardio-protective and anti-inflammatory properties. This study presents synthesis and stability studie...

(This article belongs to the Special Issue Multitarget Drug Discovery and Pharmacology)
  • Article
  • Open Access
34 Citations
7,224 Views
20 Pages

Learnings from Regional Market Dynamics of Originator and Biosimilar Infliximab and Etanercept in Germany

  • Evelien Moorkens,
  • Teresa Barcina Lacosta,
  • Arnold G. Vulto,
  • Martin Schulz,
  • Gabriele Gradl,
  • Salka Enners,
  • Gisbert Selke,
  • Isabelle Huys and
  • Steven Simoens

21 October 2020

Drug budget and prescription control measures are implemented regionally in Germany, meaning that the uptake of pharmaceuticals, including biosimilars, can vary by region. We examine regional market dynamics of tumor necrosis factor alpha (TNFα...

(This article belongs to the Special Issue Biosimilars in Europe)
  • Communication
  • Open Access
18 Citations
8,832 Views
10 Pages

21 October 2020

Bipolar disorder is a chronic and remitting mental illness. Antidepressants are not effective in treating acute bipolar depression, and antipsychotic drugs used in the treatment of bipolar depression cause frequent side effects. This situation justif...

(This article belongs to the Special Issue New Drugs and Biologics For Treatment of Central Nervous Dysfunction)
  • Article
  • Open Access
34 Citations
7,949 Views
19 Pages

Cardiotoxicity Associated with Gemcitabine: Literature Review and a Pharmacovigilance Study

  • Marc Hilmi,
  • Stéphane Ederhy,
  • Xavier Waintraub,
  • Christian Funck-Brentano,
  • Ariel Cohen,
  • Aurore Vozy,
  • Bénédicte Lebrun-Vignes,
  • Javid Moslehi,
  • Lee S. Nguyen and
  • Joe-Elie Salem

21 October 2020

Background: Gemcitabine is a nucleoside analog, widely used either alone or in combination, for the treatment of multiple cancers. However, gemcitabine may also be associated with cardiovascular adverse-drug-reactions (CV-ADR). Methods: First, we sea...

(This article belongs to the Special Issue Cancer Drugs Treatment and Toxicity)
  • Article
  • Open Access
16 Citations
4,772 Views
13 Pages

Reversal of Ovarian Cancer Cell Lines Multidrug Resistance Phenotype by the Association of Apiole with Chemotherapies

  • Carolina Afonso de Lima,
  • Ian Lucas de Souza Bueno,
  • Stanley Nunes Siqueira Vasconcelos,
  • Juliana Mozer Sciani,
  • Ana Lúcia Tasca Gois Ruiz,
  • Mary Ann Foglio,
  • João Ernesto de Carvalho and
  • Giovanna Barbarini Longato

21 October 2020

Multidrug resistance (MDR) is the main obstacle in anticancer therapy. The use of drug combinations to circumvent tumor resistance is a well-established principle in the clinic. Among the therapeutic targets, glycoprotein-P (P-gp), an energy-dependen...

(This article belongs to the Special Issue Anticancer Compounds in Medicinal Plants)
  • Feature Paper
  • Article
  • Open Access
7 Citations
3,590 Views
9 Pages

Antiarrhythmic Effect of Ranolazine in Combination with Selective NCX-Inhibition in an Experimental Model of Atrial Fibrillation

  • Julian Wolfes,
  • Christian Ellermann,
  • Niklas Broer,
  • Benjamin Rath,
  • Kevin Willy,
  • Patrick Robert Leitz,
  • Philipp Sebastian Lange,
  • Lars Eckardt and
  • Gerrit Frommeyer

20 October 2020

The aim of this study was to investigate the effects of a combination of ranolazine with different selective inhibitors of the Na+/Ca2+-exchanger (NCX) in an established experimental model of atrial fibrillation (AF). Eighteen hearts of New Zealand w...

(This article belongs to the Section Medicinal Chemistry)
  • Feature Paper
  • Review
  • Open Access
17 Citations
5,075 Views
22 Pages

20 October 2020

Stress exposure represents a major environmental risk factor for schizophrenia and other psychiatric disorders, as it plays a pivotal role in the etiology as well as in the manifestation of disease symptomatology. It may be inferred that pharmacologi...

(This article belongs to the Special Issue Molecular and Cellular Targets of Old and New Atypical Antipsychotics)
  • Article
  • Open Access
23 Citations
5,857 Views
18 Pages

Attenuation of Spatial Memory in 5xFAD Mice by Halting Cholinesterases, Oxidative Stress and Neuroinflammation Using a Cyclopentanone Derivative

  • Rahim Ullah,
  • Gowhar Ali,
  • Nisar Ahmad,
  • Muhammad Akram,
  • Geeta Kumari,
  • Muhammad Usman Amin and
  • Muhammad Naveed Umar

19 October 2020

Alzheimer’s disease (AD) is an irreversible and chronic neurological disorder that gradually destroys memory and thinking skills. The research study was designed to investigate the underlying molecular signaling involved in the neuroprotective...

(This article belongs to the Section Pharmacology)
  • Review
  • Open Access
33 Citations
5,673 Views
25 Pages

19 October 2020

Exosomes are phospholipid-based particles endogenously produced by both normal and tumor cells. Initially identified as a pathway for shuttling cellular waste, for a long time they were thought to act as “garbage bags”, and only in the pa...

(This article belongs to the Special Issue Exosomes as a Tool for Disease Progression Monitoring in Humans and Animals)
  • Article
  • Open Access
16 Citations
4,729 Views
24 Pages

Impact of Washingtonia robusta Leaves on Gamma Irradiation-Induced Hepatotoxicity in Rats and Correlation with STING Pathway and Phenolic Composition

  • Nabil M. Selim,
  • Seham S. El-Hawary,
  • Soheir M. El Zalabani,
  • Rehab Nabil Shamma,
  • Nariman El Sayed Mahdy,
  • Noheir H. Sherif,
  • Hanan A. Fahmy,
  • Mai H. Mekkawy,
  • Abdelaziz Yasri and
  • Mansour Sobeh

19 October 2020

Exposure to ionizing radiation usually results in cellular oxidative damage and may induce liver toxicity. The efficiency of the ethanol extracts of Washingtonia filifera (EWF) and Washingtonia robusta (EWR) leaves in alleviating γ-radiation-induced...

(This article belongs to the Section Natural Products)
  • Feature Paper
  • Article
  • Open Access
33 Citations
6,730 Views
11 Pages

Effect of Tocilizumab in Hospitalized Patients with Severe COVID-19 Pneumonia: A Case-Control Cohort Study

  • Benjamin Rossi,
  • Lee S. Nguyen,
  • Philippe Zimmermann,
  • Faiza Boucenna,
  • Louis Dubret,
  • Louise Baucher,
  • Helene Guillot,
  • Marie-Anne Bouldouyre,
  • Yves Allenbach and
  • Helene Gros
  • + 3 authors

17 October 2020

Tocilizumab, an anti-interleukin-6 receptor, administrated during the right timeframe may be beneficial against coronavirus-disease-2019 (COVID-19) pneumonia. All patients admitted for severe COVID-19 pneumonia (SpO2 ≤ 96% despite O2-support ≥...

(This article belongs to the Special Issue COVID-19 in Pharmaceuticals)
  • Communication
  • Open Access
17 Citations
4,988 Views
20 Pages

Metformin Reduces NGF-Induced Tumour Promoter Effects in Epithelial Ovarian Cancer Cells

  • Maritza P. Garrido,
  • Renato Salvatierra,
  • Manuel Valenzuela-Valderrama,
  • Christopher Vallejos,
  • Nicole Bruneau,
  • Andrea Hernández,
  • Margarita Vega,
  • Alberto Selman,
  • Andrew F. G. Quest and
  • Carmen Romero

16 October 2020

Epithelial ovarian cancer (EOC) is a lethal gynaecological neoplasm characterized by rapid growth and angiogenesis. Nerve growth factor (NGF) and its high affinity receptor tropomyosin receptor kinase A (TRKA) contribute to EOC progression by increas...

(This article belongs to the Special Issue Metformin: Mechanism and Application 2022)
  • Article
  • Open Access
18 Citations
5,150 Views
10 Pages

Novel Photosensitizer β-Mannose-Conjugated Chlorin e6 as a Potent Anticancer Agent for Human Glioblastoma U251 Cells

  • Yo Shinoda,
  • Kohei Kujirai,
  • Kohei Aoki,
  • Mai Morita,
  • Masato Masuda,
  • Lihao Zhang,
  • Zhou Kaixin,
  • Akihiro Nomoto,
  • Tsutomu Takahashi and
  • Yasuyuki Fujiwara
  • + 7 authors

16 October 2020

A photosensitizer is a molecular drug for photodynamic diagnosis and photodynamic therapy (PDT) against cancer. Many studies have developed photosensitizers, but improvements in their cost, efficacy, and side effects are needed for better PDT of pati...

(This article belongs to the Special Issue Photodynamic Therapy 2021)
  • Article
  • Open Access
4 Citations
4,760 Views
15 Pages

Development of a Multivariate Predictive Dissolution Model for Tablets Coated with Cellulose Ester Blends

  • Eman M. Mohamed,
  • Tahir Khuroo,
  • Hamideh Afrooz,
  • Sathish Dharani,
  • Khaldia Sediri,
  • Phillip Cook,
  • Rajendran Arunagiri,
  • Mansoor A. Khan and
  • Ziyaur Rahman

15 October 2020

The focus of the present investigation was to develop a predictive dissolution model for tablets coated with blends of cellulose acetate butyrate (CAB) 171-15 and cellulose acetate phthalate (C-A-P) using the design of experiment and chemometric appr...

(This article belongs to the Section Pharmaceutical Technology)
  • Article
  • Open Access
26 Citations
5,921 Views
17 Pages

New Class of Efficient T2 Magnetic Resonance Imaging Contrast Agent: Carbon-Coated Paramagnetic Dysprosium Oxide Nanoparticles

  • Huan Yue,
  • Ji Ae Park,
  • Son Long Ho,
  • Mohammad Yaseen Ahmad,
  • Hyunsil Cha,
  • Shuwen Liu,
  • Tirusew Tegafaw,
  • Shanti Marasini,
  • Adibehalsadat Ghazanfari and
  • Gang Ho Lee
  • + 3 authors

15 October 2020

Nanoparticles are considered potential candidates for a new class of magnetic resonance imaging (MRI) contrast agents. Negative MRI contrast agents require high magnetic moments. However, if nanoparticles can exclusively induce transverse water proto...

(This article belongs to the Special Issue Next Generation of MRI Agents)
  • Article
  • Open Access
32 Citations
5,451 Views
20 Pages

Brain-Targeted Delivery of Pre-miR-29b Using Lactoferrin-Stearic Acid-Modified-Chitosan/Polyethyleneimine Polyplexes

  • Patrícia Pereira,
  • Maria Barreira,
  • Carla Cruz,
  • Joana Tomás,
  • Ângelo Luís,
  • Augusto Q. Pedro,
  • João A. Queiroz and
  • Fani Sousa

15 October 2020

The efficacy of brain therapeutics is largely hampered by the presence of the blood–brain barrier (BBB), mainly due to the failure of most (bio) pharmaceuticals to cross it. Accordingly, this study aims to develop nanocarriers for targeted deli...

(This article belongs to the Special Issue Therapeutic Agents for Neurological Disorders)
  • Review
  • Open Access
71 Citations
11,227 Views
17 Pages

Medicinal Plants to Strengthen Immunity during a Pandemic

  • Olga Babich,
  • Stanislav Sukhikh,
  • Alexander Prosekov,
  • Lyudmila Asyakina and
  • Svetlana Ivanova

15 October 2020

The development of new effective anti-coronavirus drugs and therapies is important, but it requires significant human, financial and, most importantly, time expenditures. The current pandemic is neither the first nor the last. Humanity has already ac...

(This article belongs to the Special Issue Medicinal Plants 2020)
  • Review
  • Open Access
83 Citations
12,212 Views
29 Pages

14 October 2020

Diabetes mellitus is a chronic endocrine disease, affecting more than 400 million people around the world. Patients with poorly controlled blood glucose levels are liable to suffer from life-threatening complications, such as cardiovascular, neuropat...

(This article belongs to the Section Pharmaceutical Technology)
  • Article
  • Open Access
32 Citations
4,843 Views
21 Pages

14 October 2020

Five novel peptides (LPLF, WLQL, LPSW, VPGLAL, and LVGLPL) bearing dipeptidyl peptidase IV (DPP-IV) inhibitory activities were identified from the gastrointestinal enzymatic hydrolysate of soft-shelled turtle yolk (SSTY) proteins. Peptides were isola...

(This article belongs to the Section Biopharmaceuticals)
  • Feature Paper
  • Review
  • Open Access
38 Citations
46,470 Views
51 Pages

Pharmacology of Herbal Sexual Enhancers: A Review of Psychiatric and Neurological Adverse Effects

  • Pietro Brunetti,
  • Alfredo Fabrizio Lo Faro,
  • Anastasio Tini,
  • Francesco Paolo Busardò and
  • Jeremy Carlier

14 October 2020

Sexual enhancers increase sexual potency, sexual pleasure, or libido. Substances increasing libido alter the concentrations of specific neurotransmitters or sex hormones in the central nervous system. Interestingly, the same pathways are involved in...

(This article belongs to the Special Issue Clinical and Forensic Toxicology: The Latest Updates)
  • Article
  • Open Access
33 Citations
7,313 Views
17 Pages

Additive Effect of a Combination of Artocarpus lakoocha and Glycyrrhiza glabra Extracts on Tyrosinase Inhibition in Melanoma B16 Cells

  • Tasanee Panichakul,
  • Teerapat Rodboon,
  • Prasit Suwannalert,
  • Chanchai Tripetch,
  • Rittipun Rungruang,
  • Nattaporn Boohuad and
  • Piyawan Youdee

14 October 2020

Artocarpus lakoocha (Al) and Glycyrrhiza glabra (Gg) extracts have been reported to show tyrosinase inhibitory activity and melanin pigment reduction. This is the first study to assess the combination of Al and Gg extracts in enhancing inhibition of...

(This article belongs to the Special Issue Natural Pharmacons: Biologically Active Plant Based Pharmaceuticals)
  • Article
  • Open Access
34 Citations
5,044 Views
12 Pages

Prediction of Antidepressant Treatment Response and Remission Using an Ensemble Machine Learning Framework

  • Eugene Lin,
  • Po-Hsiu Kuo,
  • Yu-Li Liu,
  • Younger W.-Y. Yu,
  • Albert C. Yang and
  • Shih-Jen Tsai

13 October 2020

In the wake of recent advances in machine learning research, the study of pharmacogenomics using predictive algorithms serves as a new paradigmatic application. In this work, our goal was to explore an ensemble machine learning approach which aims to...

(This article belongs to the Special Issue The Pharmacogenomics of Mood Stabilizers)
  • Review
  • Open Access
80 Citations
15,775 Views
15 Pages

Dimethyl Fumarate and Its Esters: A Drug with Broad Clinical Utility?

  • Stephanie Kourakis,
  • Cara A. Timpani,
  • Judy B. de Haan,
  • Nuri Gueven,
  • Dirk Fischer and
  • Emma Rybalka

13 October 2020

Fumaric acid esters (FAEs) are small molecules with anti-oxidative, anti-inflammatory and immune-modulating effects. Dimethyl fumarate (DMF) is the best characterised FAE and is approved and registered for the treatment of psoriasis and Relapsing-Rem...

(This article belongs to the Special Issue Therapeutic Agents for Neurological Disorders)
  • Article
  • Open Access
27 Citations
4,451 Views
12 Pages

12 October 2020

Bisphenol A (BPA) is a chemical compound used in the manufacturing of plastics and resins whose presence in the body in low concentrations can cause serious health problems. Due to this, there is a growing interest in the scientific community to deve...

(This article belongs to the Special Issue Applications of Liquid Chromatography in Analysis of Pharmaceuticals and Natural Products)
  • Article
  • Open Access
18 Citations
4,738 Views
14 Pages

12 October 2020

Rosmarinic acid methyl ester (RAME), a derivative of rosmarinic acid (RA), is reported to have several therapeutic effects, including anti-tumor effects against cervical cancer. However, its anti-tumor effects in ovarian cancer is unclear. In this st...

(This article belongs to the Special Issue Bioactive Compounds from Plants and Foods with Pharmaceutical Interest)
  • Article
  • Open Access
17 Citations
5,943 Views
21 Pages

Terminalia bentzoë, a Mascarene Endemic Plant, Inhibits Human Hepatocellular Carcinoma Cells Growth In Vitro via G0/G1 Phase Cell Cycle Arrest

  • Nawraj Rummun,
  • Philippe Rondeau,
  • Emmanuel Bourdon,
  • Elisabete Pires,
  • James McCullagh,
  • Timothy D. W. Claridge,
  • Theeshan Bahorun,
  • Wen-Wu Li and
  • Vidushi S. Neergheen

12 October 2020

Tropical forests constitute a prolific sanctuary of unique floral diversity and potential medicinal sources, however, many of them remain unexplored. The scarcity of rigorous scientific data on the surviving Mascarene endemic taxa renders bioprospect...

(This article belongs to the Special Issue Anticancer Compounds in Medicinal Plants)
  • Article
  • Open Access
35 Citations
5,845 Views
12 Pages

Antibacterial Drug-Release Polydimethylsiloxane Coating for 3D-Printing Dental Polymer: Surface Alterations and Antimicrobial Effects

  • Hang-Nga Mai,
  • Dong Choon Hyun,
  • Ju Hayng Park,
  • Do-Yeon Kim,
  • Sang Min Lee and
  • Du-Hyeong Lee

12 October 2020

Polymers are the most commonly used material for three-dimensional (3D) printing in dentistry; however, the high porosity and water absorptiveness of the material adversely influence biofilm formation on the surface of the 3D-printed dental prosthese...

(This article belongs to the Special Issue Novel Antibacterial Agents)
  • Review
  • Open Access
45 Citations
6,389 Views
13 Pages

10 October 2020

Today, researchers are looking at new ways to treat severe infections caused by resistance to standard antibiotic therapy. This is quite challenging due to the complex and interdependent relationships involved: the cause of infection–the patien...

(This article belongs to the Section Biopharmaceuticals)
  • Article
  • Open Access
20 Citations
4,482 Views
20 Pages

10 October 2020

Efficient and specific delivery of nucleic acid (NA) therapeutics to tumor cells is extremely important for cancer gene therapy. Various therapeutic strategies include delivery of DNA-therapeutics such as immunostimulatory or suicide genes and delive...

(This article belongs to the Special Issue Multi-Component Delivery Systems for Targeted Delivery of Nucleic Acids)
  • Article
  • Open Access
9 Citations
4,921 Views
12 Pages

9 October 2020

The search for new therapeutics for the treatment of Alzheimer’s disease (AD) is still in progress. Aberrant pathways of synaptic transmission in basal forebrain cholinergic neural circuits are thought to be associated with the progression of A...

(This article belongs to the Special Issue New Drugs and Biologics For Treatment of Central Nervous Dysfunction)
  • Communication
  • Open Access
10 Citations
3,288 Views
14 Pages

Impact of S1P Mimetics on Mesenteric Ischemia/Reperfusion Injury

  • Francesco Potì,
  • Carmine Giorgio,
  • Irene Zini,
  • Jerzy-Roch Nofer,
  • Valentina Vivo,
  • Simone Palese,
  • Vigilio Ballabeni,
  • Elisabetta Barocelli and
  • Simona Bertoni

9 October 2020

Mesenteric ischemia/reperfusion (I/R), following the transient deprivation of blood flow to the gut, triggers an acute flogistic process involving the disruption of endothelial and epithelial barriers integrity, the activation of immune cells, and th...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
3 Citations
5,215 Views
14 Pages

A Photocleavable Contrast Agent for Light-Responsive MRI

  • Friederike Reeßing,
  • Sèvrin E. M. Huijsse,
  • Rudi A. J. O. Dierckx,
  • Ben L. Feringa,
  • Ronald J.H. Borra and
  • Wiktor Szymański

8 October 2020

Thanks to its innocuousness and high spatiotemporal resolution, light is used in several established and emerging applications in biomedicine. Among them is the modulation of magnetic resonance imaging (MRI) contrast agents’ relaxivity with the...

(This article belongs to the Special Issue Next Generation of MRI Agents)
  • Review
  • Open Access
233 Citations
20,247 Views
25 Pages

Overcoming Barriers for siRNA Therapeutics: From Bench to Bedside

  • Muhammad Imran Sajid,
  • Muhammad Moazzam,
  • Shun Kato,
  • Kayley Yeseom Cho and
  • Rakesh Kumar Tiwari

7 October 2020

The RNA interference (RNAi) pathway possesses immense potential in silencing any gene in human cells. Small interfering RNA (siRNA) can efficiently trigger RNAi silencing of specific genes. FDA Approval of siRNA therapeutics in recent years garnered...

(This article belongs to the Special Issue Multi-Component Delivery Systems for Targeted Delivery of Nucleic Acids)
  • Article
  • Open Access
24 Citations
7,627 Views
18 Pages

A Novel Integrated Active Herbal Formulation Ameliorates Dry Eye Syndrome by Inhibiting Inflammation and Oxidative Stress and Enhancing Glycosylated Phosphoproteins in Rats

  • Omer Ersin Muz,
  • Cemal Orhan,
  • Fusun Erten,
  • Mehmet Tuzcu,
  • Ibrahim Hanifi Ozercan,
  • Prafull Singh,
  • Abhijeet Morde,
  • Muralidhara Padigaru,
  • Deshanie Rai and
  • Kazim Sahin

7 October 2020

Dry eye syndrome (DES) is a chronic condition of the eye with insufficient production of tears leading to inadequate lubrication of eyes. Symptoms of DES are associated with discomfort and redness of the eye, blurred vision, and tear film instability...

(This article belongs to the Special Issue Bioactive Compounds from Plants and Foods with Pharmaceutical Interest)
  • Article
  • Open Access
13 Citations
4,085 Views
25 Pages

Cytotoxicity Effects of Water-Soluble Multi-Walled Carbon Nanotubes Decorated with Quaternized Hyperbranched Poly(ethyleneimine) Derivatives on Autotrophic and Heterotrophic Gram-Negative Bacteria

  • Nikolaos S. Heliopoulos,
  • Georgia Kythreoti,
  • Kyriaki Marina Lyra,
  • Katerina N. Panagiotaki,
  • Aggeliki Papavasiliou,
  • Elias Sakellis,
  • Sergios Papageorgiou,
  • Antonios Kouloumpis,
  • Dimitrios Gournis and
  • Zili Sideratou
  • + 2 authors

6 October 2020

Oxidized multi-walled carbon nanotubes (oxCNTs) were functionalized by a simple non-covalent modification procedure using quaternized hyperbranched poly(ethyleneimine) derivatives (QPEIs), with various quaternization degrees. Structural characterizat...

(This article belongs to the Special Issue Novel Antibacterial Agents)
  • Review
  • Open Access
20 Citations
5,372 Views
28 Pages

5 October 2020

Uncontrolled proliferation is a feature defining cancer and it is linked to the ability of cancer cells to effectively adapt their metabolic needs in response to a harsh tumor environment. Metabolic reprogramming is considered a hallmark of cancer an...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
10 Citations
3,820 Views
13 Pages

Isoeugenol and Hybrid Acetamides against Candida albicans Isolated from the Oral Cavity

  • Daianne Medeiros,
  • José Oliveira-Júnior,
  • Jefferson Nóbrega,
  • Laísa Cordeiro,
  • Jeane Jardim,
  • Helivaldo Souza,
  • Gracielle Silva,
  • Petrônio Athayde-Filho,
  • José Barbosa-Filho and
  • Edeltrudes Lima
  • + 1 author

3 October 2020

Isougenol is a phytoconstituent found in several essential oils. Since many natural products are potent antimicrobials, the synthesis of hybrid molecules—combining the chemical skeleton of the phytochemical with synthetic groups—can gener...

(This article belongs to the Section Natural Products)
  • Article
  • Open Access
16 Citations
5,966 Views
14 Pages

Targeting and Efficacy of Novel mAb806-Antibody-Drug Conjugates in Malignant Mesothelioma

  • Puey-Ling Chia,
  • Sagun Parakh,
  • Ming-Sound Tsao,
  • Nhu-An Pham,
  • Hui K. Gan,
  • Diana Cao,
  • Ingrid J. G. Burvenich,
  • Angela Rigopoulos,
  • Edward B. Reilly and
  • Andrew M. Scott
  • + 1 author

2 October 2020

Epidermal growth factor receptor (EGFR) is highly overexpressed in malignant mesothelioma (MM). MAb806 is a novel anti-EGFR antibody that selectively targets a tumor-selective epitope. MAb806-derived antibody drug conjugates (ADCs), ABT-414, ABBV-221...

(This article belongs to the Special Issue Antibody-Drug Conjugates (ADC): 2021)
  • Article
  • Open Access
32 Citations
5,508 Views
16 Pages

Enhancement of α-Mangostin Wound Healing Ability by Complexation with 2-Hydroxypropyl-β-Cyclodextrin in Hydrogel Formulation

  • Nasrul Wathoni,
  • Diah Permata Sari,
  • Ine Suharyani,
  • Keiichi Motoyama,
  • Ahmed Fouad Abdelwahab Mohammed,
  • Arief Cahyanto,
  • Marline Abdassah and
  • Muchtaridi Muchtaridi

2 October 2020

α-Mangostin (α-M), one of the active compounds in Garcinia mangostana peel, has been effectively used in wound healing. However, its poor solubility in aqueous solution causes low bioavailability for skin ulcers, hindering its application...

(This article belongs to the Special Issue Bioactive Compounds from Plants and Foods with Pharmaceutical Interest)
  • Article
  • Open Access
8 Citations
4,620 Views
16 Pages

Kinin B2 Receptor Activation Prevents the Evolution of Alzheimer’s Disease Pathological Characteristics in a Transgenic Mouse Model

  • Marielza Andrade Nunes,
  • Mariana Toricelli,
  • Natalia Mendes Schöwe,
  • Helena Nascimento Malerba,
  • Karis Ester Dong-Creste,
  • Daniela Moura Azevedo Tuma Farah,
  • Katia De Angelis,
  • Maria Claudia Irigoyen,
  • Fernand Gobeil and
  • Hudson Sousa Buck
  • + 1 author

1 October 2020

Background: Alzheimer’s disease is mainly characterized by remarkable neurodegeneration in brain areas related to memory formation. This progressive neurodegeneration causes cognitive impairment, changes in behavior, functional disability, and...

(This article belongs to the Special Issue Kinins and Their Receptors as Potential Therapeutic Targets —— A Tribute to Professor Domenico Regoli, A Key Figure in the Field of Kinins)
  • Article
  • Open Access
26 Citations
6,895 Views
27 Pages

30 September 2020

Citrus hystrix (CH) is a beneficial plant utilized in traditional folk medicine to relieve various health ailments. The antisenescent mechanisms of CH extracts were investigated using human neuroblastoma cells (SH-SY5Y). Phytochemical contents and an...

(This article belongs to the Special Issue Medicinal Plants 2020)
  • Article
  • Open Access
9 Citations
3,422 Views
20 Pages

Synthesis, Antiproliferative Activity, and DNA Binding Studies of Nucleoamino Acid-Containing Pt(II) Complexes

  • Claudia Riccardi,
  • Domenica Capasso,
  • Angela Coppola,
  • Chiara Platella,
  • Daniela Montesarchio,
  • Sonia Di Gaetano,
  • Giovanni N. Roviello and
  • Domenica Musumeci

30 September 2020

We here report our studies on the reaction with the platinum(II) ion of a nucleoamino acid constituted by the l-2,3-diaminopropanoic acid linked to the thymine nucleobase through a methylenecarbonyl linker. The obtained new platinum complexes, charac...

(This article belongs to the Special Issue Metal-Based Drugs: Updates and Perspectives)
  • Opinion
  • Open Access
1 Citations
2,502 Views
9 Pages

30 September 2020

Switch maintenance, or using alternative therapeutic agents that were not administered during a prior course of cancer treatment, has emerged as an active clinical research and regulatory agency-approvable path in the National Cancer Institute (NCI)...

(This article belongs to the Section Radiopharmaceutical Sciences)
  • Article
  • Open Access
26 Citations
5,971 Views
17 Pages

Resveratrol Metabolites Are Able to Reduce Steatosis in Cultured Hepatocytes

  • Jenifer Trepiana,
  • Stéphanie Krisa,
  • Elodie Renouf and
  • María Puy Portillo

30 September 2020

Steatosis is characterized primarily by excessive lipid accumulation in the form of triglycerides in the liver. Although resveratrol shows a low bioavailability, it has significant positive effects on steatosis. The aim of this study was to analyze w...

(This article belongs to the Special Issue Bioactive Compounds from Plants and Foods with Pharmaceutical Interest)
  • Article
  • Open Access
19 Citations
4,603 Views
18 Pages

Penetration into Cancer Cells via Clathrin-Dependent Mechanism Allows L-Asparaginase from Rhodospirillum rubrum to Inhibit Telomerase

  • Anna A. Plyasova,
  • Marina V. Pokrovskaya,
  • Olga M. Lisitsyna,
  • Vadim S. Pokrovsky,
  • Svetlana S. Alexandrova,
  • Abdullah Hilal,
  • Nikolay N. Sokolov and
  • Dmitry D. Zhdanov

30 September 2020

The anticancer effect of L-asparaginases (L-ASNases) is attributable to their ability to hydrolyze L-asparagine in the bloodstream and cancer cell microenvironment. Rhodospirillum rubrum (RrA) has dual mechanism of action and plays a role in the supp...

(This article belongs to the Special Issue Amino Acids Metabolism and Cancer Therapy)
  • Article
  • Open Access
20 Citations
6,154 Views
20 Pages

Pharmacological Modulation of Blood–Brain Barrier Permeability by Kinin Analogs in Normal and Pathologic Conditions

  • Dina Sikpa,
  • Lisa Whittingstall,
  • Martin Savard,
  • Réjean Lebel,
  • Jérôme Côté,
  • Stephen McManus,
  • Sylvain Chemtob,
  • David Fortin,
  • Martin Lepage and
  • Fernand Gobeil

29 September 2020

The blood–brain barrier (BBB) is a major obstacle to the development of effective diagnostics and therapeutics for brain cancers and other central nervous system diseases. Peptide agonist analogs of kinin B1 and B2 receptors, acting as BBB perm...

(This article belongs to the Special Issue Kinins and Their Receptors as Potential Therapeutic Targets —— A Tribute to Professor Domenico Regoli, A Key Figure in the Field of Kinins)
  • Article
  • Open Access
17 Citations
3,849 Views
20 Pages

29 September 2020

Depression is a global threat. Tricyclic antidepressants (TCAs) are still efficacious in treating depression, albeit with more side effects. Cyclodextrins (CDs) with a suitable nanocavity are potential drug carriers and can enhance the drug bioavaila...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
10 Citations
3,537 Views
18 Pages

Peptide-Based TNF-α-Binding Decoy Therapy Mitigates Lipopolysaccharide-Induced Liver Injury in Mice

  • Chao-Yuan Chang,
  • Hao-Jen Hsu,
  • Jossen Foo,
  • Hung-Jen Shih and
  • Chun-Jen Huang

29 September 2020

A peptide named SEM18, possessing structural similarity to the binding site of tumor necrosis factor (TNF)-α to TNF receptor 1 (TNFR1), was designed. We investigated whether the SEM18 peptide can mitigate lipopolysaccharide (LPS)-induced liver...

(This article belongs to the Section Biopharmaceuticals)
  • Review
  • Open Access
46 Citations
5,900 Views
20 Pages

Cyclic Oligosaccharides as Active Drugs, an Updated Review

  • Adrián Matencio,
  • Fabrizio Caldera,
  • Claudio Cecone,
  • José Manuel López-Nicolás and
  • Francesco Trotta

29 September 2020

There have been many reviews of the cyclic oligosaccharide cyclodextrin (CD) and CD-based materials used for drug delivery, but the capacity of CDs to complex different agents and their own intrinsic properties suggest they might also be considered f...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
10 Citations
3,813 Views
11 Pages

29 September 2020

Blood-pool agents (BPAs) are MRI contrast agents (CAs) characterized by their long circulation in the vascular system to provide an extended time window for high-resolution MR angiography (MRA). Prolonged vascular retention, however, impedes the excr...

(This article belongs to the Special Issue Next Generation of MRI Agents)

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Pharmaceuticals - ISSN 1424-8247