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Pharmaceuticals, Volume 13, Issue 3

2020 March - 19 articles

Cover Story: Targeted imaging in oncology can provide tumor-type specific non-invasive diagnosis and the precise localization of tumors and metastases that, most importantly, have the potential for pre-therapeutic quantification of receptor status, uptake kinetics, and dosimetry. This technique can enable accurate therapy selection and planning as well as monitoring of the response to therapy, resulting in personalized medicine. For example, reliable whole-body, quantitative assessment of HER2 receptor expression is crucial to identify patients with HER2-positive tumors who can benefit from HER2-targeted treatments. It is as important to avoid unnecessary costs as well as the potential risk of serious adverse effects and time delay related to the treatment of patients with HER2-negative tumors. The number of radiopharmaceuticals contributing to the realization of theranostics/radiotheranostics in the context of personalized medicine is increasing. Vi

Articles (19)

  • Article
  • Open Access
20 Citations
6,364 Views
15 Pages

4-Amino-1,2,4-triazole-3-thione as a Promising Scaffold for the Inhibition of Serine and Metallo-β-Lactamases

  • Pasquale Linciano,
  • Eleonora Gianquinto,
  • Martina Montanari,
  • Lorenzo Maso and ,
  • Pierangelo Bellio,
  • Esmeralda Cebrián-Sastre,
  • Giuseppe Celenza,
  • Jesús Blázquez,
  • Laura Cendron and
  • Donatella Tondi
  • + 6 authors+ 1 author

The emergence of bacteria that co-express serine- and metallo- carbapenemases is a threat to the efficacy of the available β-lactam antibiotic armamentarium. The 4-amino-1,2,4-triazole-3-thione scaffold has been selected as the starting chemical...

(This article belongs to the Section Medicinal Chemistry)
  • Commentary
  • Open Access
72 Citations
13,773 Views
9 Pages

The COVID-19 coronavirus is currently spreading around the globe with limited treatment options available. This article presents the rationale for potentially using old drugs (emetine, other ipecac alkaloids or analogues) that have been used to treat...

(This article belongs to the Special Issue COVID-19 in Pharmaceuticals)
  • Article
  • Open Access
28 Citations
9,202 Views
20 Pages

Unveiling Pharmacological Responses and Potential Targets Insights of Identified Bioactive Constituents of Cuscuta reflexa Roxb. Leaves through In Vivo and In Silico Approaches

  • Md. Adnan,
  • Md. Nazim Uddin Chy,
  • A.T.M. Mostafa Kamal,
  • Md. Riad Chowdhury and ,
  • Md. Shariful Islam,
  • Md. Amzad Hossain,
  • Abu Montakim Tareq,
  • Md. Imam Hossain Bhuiyan,
  • Md Nasim Uddin and
  • Dong Ha Cho
  • + 8 authors+ 3 authors

Cuscuta reflexa Roxb. is traditionally used by the indigenous communities of Bangladesh to treat different diseases, such as pain, edema, tumor, jaundice, and skin infections. This study tested neuro-pharmacological, anti-nociceptive, and antidiarrhe...

(This article belongs to the Special Issue Medicinal Plants 2020)
  • Article
  • Open Access
8 Citations
5,025 Views
18 Pages

Infectious diseases in early postnatal ontogenesis often result in cognitive impairments, particularly learning and memory. The essential foundation of learning and memory is long-term synaptic plasticity, which depends on N-methyl-D-aspartate (NMDA)...

(This article belongs to the Special Issue Choices of the Journal)
  • Review
  • Open Access
63 Citations
9,040 Views
17 Pages

This network meta-analysis aimed to integrate the available direct and indirect evidence on regenerative injections—including 5% dextrose (D5W) and platelet-rich plasma (PRP)—for the treatment of carpal tunnel syndrome (CTS). Literature r...

(This article belongs to the Special Issue Therapeutics Agents for Neural Repair)
  • Article
  • Open Access
14 Citations
5,152 Views
16 Pages

In Vitro Anti-Prostate Cancer Activity of Two Ebselen Analogues

  • Katarzyna B. Kaczor-Keller,
  • Anna Pawlik,
  • Jacek Scianowski,
  • Agata Pacuła and ,
  • Magdalena Obieziurska,
  • Fabio Marcheggiani,
  • Ilenia Cirilli,
  • Luca Tiano and
  • Jedrzej Antosiewicz
  • + 4 authors+ 0 author

Scientific research has been underway for decades in order to develop an effective anticancer drug, and it has become crucial to find a novel and effective chemotherapeutics in the case of prostate cancer treatment. Ebselen derivatives have been show...

(This article belongs to the Collection Old Pharmaceuticals with New Applications)
  • Article
  • Open Access
24 Citations
4,942 Views
17 Pages

Products Derived from Buchenavia tetraphylla Leaves Have In Vitro Antioxidant Activity and Protect Tenebrio molitor Larvae against Escherichia coli-Induced Injury

  • Tiago Fonseca Silva,
  • José Robson Neves Cavalcanti Filho,
  • Mariana Mirelle Lima Barreto Fonsêca,
  • Natalia Medeiros dos Santos and ,
  • Ana Carolina Barbosa da Silva,
  • Adrielle Zagmignan,
  • Afonso Gomes Abreu,
  • Ana Paula Sant’Anna da Silva,
  • Vera Lúcia de Menezes Lima and
  • Luís Cláudio Nascimento da Silva
  • + 10 authors+ 5 authors

The relevance of oxidative stress in the pathogenesis of several diseases (including inflammatory disorders) has traditionally led to the search for new sources of antioxidant compounds. In this work, we report the selection of fractions with high an...

(This article belongs to the Special Issue Novel Antibacterial Agents)
  • Article
  • Open Access
15 Citations
9,330 Views
22 Pages

Background: The current and potential uses of adaptogens are mainly related to treatment of stress-induced fatigue, impaired cognitive function, mental illness, and behavioral- and age-related disorders. However, clinical evidence regarding the effic...

(This article belongs to the Special Issue Medicinal Plants 2020)
  • Article
  • Open Access
69 Citations
5,918 Views
16 Pages

Preparation, Characterization, and Evaluation of Cisplatin-Loaded Polybutylcyanoacrylate Nanoparticles with Improved In Vitro and In Vivo Anticancer Activities

  • Mohsen Ghaferi,
  • Samar Amari,
  • Bhalchandra Vivek Mohrir,
  • Aun Raza and ,
  • Hasan Ebrahimi Shahmabadi and
  • Seyed Ebrahim Alavi
  • + 1 author+ 0 author

This study aimed to evaluate the therapeutic efficacy of the cisplatin encapsulated into polybutylcyanoacrylate (PBCA) nanoparticles for the treatment of kidney cancer. The nanoformulation was successfully developed using the miniemulsion polymerizat...

(This article belongs to the Section Biopharmaceuticals)
  • Article
  • Open Access
20 Citations
5,569 Views
19 Pages

Fatty Acid Amides Synthesized from Andiroba Oil (Carapa guianensis Aublet.) Exhibit Anticonvulsant Action with Modulation on GABA-A Receptor in Mice: A Putative Therapeutic Option

  • Fábio Rodrigues de Oliveira,
  • Keuri Eleuterio Rodrigues,
  • Moisés Hamoy,
  • Ícaro Rodrigues Sarquis and ,
  • Akira Otake Hamoy,
  • Maria Elena Crespo Lopez,
  • Irlon Maciel Ferreira,
  • Barbarella de Matos Macchi and
  • José Luiz Martins do Nascimento
  • + 4 authors+ 0 author

Epilepsy is a chronic neurological disease characterized by excessive neuronal activity leading to seizure; about 30% of affected patients suffer from the refractory and pharmacoresistant form of the disease. The anticonvulsant drugs currently used f...

(This article belongs to the Special Issue Therapeutics Agents for Neural Repair)
  • Brief Report
  • Open Access
16 Citations
5,959 Views
11 Pages

Is There a Role for the Therapeutic Drug Monitoring of Colistin? An Overview

  • Maria-Paula Avila,
  • Tatiana Pacheco,
  • Sara Arias,
  • Rosa-Helena Bustos and ,
  • Julio-Cesar Garcia and
  • Diego Jaimes
  • + 1 author+ 0 author

Colistin is used as a last-line antibiotic for the treatment of Gram-negative multiresistant bacteria. Due to its high nephrotoxicity, Therapeutic Drug Monitoring (TDM) is recommended for dose adjustment. We aimed to evaluate the available evidence o...

(This article belongs to the Special Issue The Story of Successful Drugs and Recent FDA-Approved Molecules)
  • Review
  • Open Access
18 Citations
8,077 Views
25 Pages

The role of nuclear medicine in the management of oncological patients has expanded during last two decades. The number of radiopharmaceuticals contributing to the realization of theranostics/radiotheranostics in the context of personalized medicine...

(This article belongs to the Special Issue The Future Direction of Radiopharmaceutical Development for Cancer Theranostics)
  • Review
  • Open Access
69 Citations
11,970 Views
15 Pages

2019 FDA TIDES (Peptides and Oligonucleotides) Harvest

  • Danah Al Shaer,
  • Othman Al Musaimi,
  • Fernando Albericio and
  • Beatriz G. de la Torre

2019 has been an excellent year in terms of peptides and oligonucleotides (TIDES) approved by the FDA. Despite the drop in the number of total drugs approved by the FDA in 2019 in comparison with 2018 (48 vs. 59), the total number of TIDES authorized...

(This article belongs to the Special Issue The Story of Successful Drugs and Recent FDA-Approved Molecules)
  • Article
  • Open Access
5 Citations
7,721 Views
19 Pages

Opipramol Inhibits Lipolysis in Human Adipocytes without Altering Glucose Uptake and Differently from Antipsychotic and Antidepressant Drugs with Adverse Effects on Body Weight Control

  • Christian Carpéné,
  • Francisco Les,
  • Josep Mercader,
  • Saioa Gomez-Zorita and ,
  • Jean-Louis Grolleau,
  • Nathalie Boulet,
  • Jessica Fontaine,
  • Mari Carmen Iglesias-Osma and
  • Maria José Garcia-Barrado
  • + 4 authors+ 0 author

Treatment with several antipsychotic drugs exhibits a tendency to induce weight gain and diabetic complications. The proposed mechanisms by which the atypical antipsychotic drug olanzapine increases body weight include central dysregulations leading...

  • Review
  • Open Access
131 Citations
23,730 Views
19 Pages

Imidazole and its derivatives are one of the most vital and universal heterocycles in medicinal chemistry. Owing to their special structural features, these compounds exhibit a widespread spectrum of significant pharmacological or biological activiti...

(This article belongs to the Section Medicinal Chemistry)
  • Review
  • Open Access
163 Citations
21,539 Views
12 Pages

In the United States, [68Ga]Ga-DOTA-TOC has been approved by the Food and Drug Administration (FDA) in 2019 as the first 68Ga-radiopharmaceutical for imaging of somatostatin receptor (SSTR) positive gastroenteropancreatic neuroendocrine tumors while...

(This article belongs to the Special Issue The Story of Successful Drugs and Recent FDA-Approved Molecules)
  • Review
  • Open Access
54 Citations
16,720 Views
16 Pages

28 February 2020

Bioisosteric replacement is a powerful tool for modulating the drug-like properties, toxicity, and chemical space of experimental therapeutics. In this review, we focus on selected cases where bioisosteric replacement and scaffold hopping have been u...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
43 Citations
8,199 Views
22 Pages

Efficacy of Bacteriophages Against Staphylococcus aureus Isolates from Bovine Mastitis

  • Isabel Titze,
  • Tatiana Lehnherr,
  • Hansjörg Lehnherr and
  • Volker Krömker

26 February 2020

The lytic efficacy of bacteriophages against Staphylococcus aureus isolates from bovine milk was investigated in vitro, regarding possible applications in the therapy of udder inflammation caused by bacterial infections (mastitis). The host range of...

(This article belongs to the Special Issue Phage Therapy and Phage-Mediated Biological Control)
  • Article
  • Open Access
12 Citations
6,862 Views
13 Pages

Targeted Protein Degradation by Chimeric Compounds using Hydrophobic E3 Ligands and Adamantane Moiety

  • Takuji Shoda,
  • Nobumichi Ohoka,
  • Genichiro Tsuji,
  • Takuma Fujisato and ,
  • Hideshi Inoue,
  • Yosuke Demizu,
  • Mikihiko Naito and
  • Masaaki Kurihara
  • + 3 authors+ 0 author

25 February 2020

Targeted protein degradation using small chimeric molecules, such as proteolysis-targeting chimeras (PROTACs) and specific and nongenetic inhibitors of apoptosis protein [IAP]-dependent protein erasers (SNIPERs), is a promising technology in drug dis...

(This article belongs to the Special Issue Targeted Protein Degradation: From Chemical Biology to Drug Discovery)
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Pharmaceuticals - ISSN 1424-8247