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Pharmaceuticals, Volume 14, Issue 10

2021 October - 118 articles

Cover Story: Tumors develop within a complex microenvironment consisting of diverse cell types surrounded by a matrix rich of proteins, termed tumor stroma. Stroma includes immune cells, fibroblasts, and vascular endothelial cells. Cancer cells rely on extensive support from the stroma to survive, proliferate, and invade, making stroma elements important potential targets for anticancer therapy. One of those elements is the fibroblast activation protein (FAP), which is overexpressed on activated fibroblasts on several tumors while absent in healthy tissues and nonmalignant tumors. Given the diversity of tumors that express FAP, it would be a great progress if nuclear medicine could have a diagnostic and therapeutic tool suitable for in vivo stroma tumor imaging and targeted radiotherapy. View this paper
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Articles (118)

  • Article
  • Open Access
39 Citations
5,058 Views
14 Pages

19 October 2021

The rise of coronavirus (COVID-19) cases worldwide has driven the need to discover and develop novel therapeutics with superior efficacy to treat this disease. This study aims to develop an innovative aerosolized nano-formulation of favipiravir (FPV)...

(This article belongs to the Section Pharmaceutical Technology)
  • Article
  • Open Access
9 Citations
5,720 Views
18 Pages

Macrosphelide A Exhibits a Specific Anti-Cancer Effect by Simultaneously Inactivating ENO1, ALDOA, and FH

  • Kyoung Song,
  • Nirmal Rajasekaran,
  • Chaithanya Chelakkot,
  • Hun Seok Lee and ,
  • Seung-Mann Paek,
  • Hobin Yang,
  • Lina Jia,
  • Hee Geon Park,
  • Woo Sung Son and
  • Young Kee Shin
  • + 10 authors+ 5 authors

19 October 2021

Aerobic glycolysis in cancer cells, also known as the Warburg effect, is an indispensable hallmark of cancer. This metabolic adaptation of cancer cells makes them remarkably different from normal cells; thus, inhibiting aerobic glycolysis is an attra...

(This article belongs to the Topic Compounds with Medicinal Value)
  • Article
  • Open Access
11 Citations
14,634 Views
11 Pages

Poppers Use and High Methaemoglobinaemia: ‘Dangerous Liaisons’

  • Malcolm Barrangou-Poueys-Darlas,
  • Marie Gerardin,
  • Sylvie Deheul,
  • Marion Istvan and ,
  • Marylène Guerlais,
  • FAN,
  • Pascale Jolliet,
  • Thomas Dejoie and
  • Caroline Victorri-Vigneau
  • + 4 authors+ 0 author

19 October 2021

Poppers are legal and largely used in France despite severe side effects, such as methaemoglobinaemia (MetHbia). Our work aimed to assess the prevalence of poppers consumers among patients with a MetHbia higher than or equal to 5% in French universit...

(This article belongs to the Special Issue Pharmacokinetics and Pharmacodynamics of Psychoactive Substances: Clinical and Forensic Aspects)
  • Review
  • Open Access
62 Citations
27,271 Views
99 Pages

19 October 2021

We review the use of molecular dynamics (MD) simulation as a drug design tool in the context of the role that the lipid membrane can play in drug action, i.e., the interaction between candidate drug molecules and lipid membranes. In the standard “loc...

(This article belongs to the Special Issue In Silico Approaches in Drug Design)
  • Article
  • Open Access
18 Citations
7,635 Views
15 Pages

The Probiotic VSL#3® Does Not Seem to Be Efficacious for the Treatment of Gastrointestinal Symptomatology of Patients with Fibromyalgia: A Randomized, Double-Blind, Placebo-Controlled Clinical Trial

  • Elena P. Calandre,
  • Javier Hidalgo-Tallon,
  • Rocio Molina-Barea,
  • Fernando Rico-Villademoros and ,
  • Cristina Molina-Hidalgo,
  • Juan M. Garcia-Leiva,
  • Maria Dolores Carrillo-Izquierdo and
  • Mahmoud Slim
  • + 3 authors+ 0 author

19 October 2021

Gastrointestinal symptomatology is frequent among patients with fibromyalgia, which increases disease burden and lacks specific treatment, either pharmacological or non-pharmacological. We aimed to evaluate the efficacy and tolerability of a multi-st...

(This article belongs to the Special Issue Rheumatic Diseases: Pathophysiology, Targeted Therapy, Focus on Vascular and Pulmonary Manifestations)
  • Article
  • Open Access
1 Citations
3,371 Views
14 Pages

Individualized versus Standardized Risk Assessment in Patients at High Risk for Adverse Drug Reactions (The IDrug Randomized Controlled Trial)–Never Change a Running System?

  • Katja S. Just,
  • Catharina Scholl,
  • Miriam Boehme,
  • Kathrin Kastenmüller and ,
  • Johannes M. Just,
  • Markus Bleckwenn,
  • Stefan Holdenrieder,
  • Florian Meier,
  • Klaus Weckbecker and
  • Julia C. Stingl
  • + 5 authors+ 0 author

18 October 2021

The aim of this study was to compare effects of an individualized with a standardized risk assessment for adverse drug reactions to improve drug treatment with antithrombotic drugs in older adults. A randomized controlled trial was conducted in gener...

(This article belongs to the Special Issue Clinical Utility of Applying PGx and Deprescribing-Based Decision Support in Polypharmacy: Future Perspectives)
  • Review
  • Open Access
81 Citations
15,759 Views
23 Pages

Epilepsy in Neurodegenerative Diseases: Related Drugs and Molecular Pathways

  • Amanda Cano,
  • Elena Fonseca,
  • Miren Ettcheto,
  • Elena Sánchez-López and ,
  • Itziar de Rojas,
  • Silvia Alonso-Lana,
  • Xavier Morató,
  • Eliana B. Souto,
  • Manuel Toledo and
  • Agustín Ruíz
  • + 7 authors+ 2 authors

18 October 2021

Epilepsy is a chronic disease of the central nervous system characterized by an electrical imbalance in neurons. It is the second most prevalent neurological disease, with 50 million people affected around the world, and 30% of all epilepsies do not...

(This article belongs to the Special Issue Epilepsy and Neurodegeneration: Current Therapeutic Implications 2021)
  • Review
  • Open Access
57 Citations
10,630 Views
19 Pages

18 October 2021

In humans, cutaneous wounds may heal without scars during embryogenesis. However, in the adult phase, the similar wound may undergo a few events such as homeostasis, blood clotting, inflammation, vascularization, and the formation of granulation tiss...

(This article belongs to the Special Issue Zebrafish as a Powerful Tool for Drug Discovery 2021)
  • Article
  • Open Access
15 Citations
4,711 Views
26 Pages

Synthesis, Computational Analysis, and Antiproliferative Activity of Novel Benzimidazole Acrylonitriles as Tubulin Polymerization Inhibitors: Part 2

  • Anja Beč,
  • Lucija Hok,
  • Leentje Persoons,
  • Els Vanstreels and ,
  • Dirk Daelemans,
  • Robert Vianello and
  • Marijana Hranjec
  • + 2 authors+ 0 author

17 October 2021

We used classical linear and microwave-assisted synthesis methods to prepare novel N-substituted, benzimidazole-derived acrylonitriles with antiproliferative activity against several cancer cells in vitro. The most potent systems showed pronounced ac...

(This article belongs to the Section Medicinal Chemistry)
  • Review
  • Open Access
71 Citations
14,672 Views
26 Pages

Mucin1 and Mucin16: Therapeutic Targets for Cancer Therapy

  • Dong-Hee Lee,
  • Seunghyun Choi,
  • Yoon Park and
  • Hyung-seung Jin

17 October 2021

The mucin (MUC) family is a group of highly glycosylated macromolecules that are abundantly expressed in mammalian epithelial cells. MUC proteins contribute to the formation of the mucus barrier and thus have protective functions against infection. I...

(This article belongs to the Special Issue Anticancer Drugs 2021)
  • Review
  • Open Access
6 Citations
3,467 Views
13 Pages

The Impact of SARS-CoV-2 Infection, and Application of Immunosuppressive Agents in Kidney Transplant Recipients Suffering from COVID-19

  • Horng-Ta Tseng,
  • Xiang-Chi Wu,
  • Chun-Yao Huang,
  • Chun-Ming Shih and ,
  • Yi-Wen Lin and
  • Feng-Yen Lin
  • + 1 author+ 0 author

17 October 2021

In December 2019, the COVID-19 pandemic began to ravage the world quickly, causing unprecedented losses in human life and the economy. A statistical study revealed that the proportion of solid organ transplant (SOT) recipients with severe symptoms an...

(This article belongs to the Special Issue COVID-19 in Pharmaceuticals)
  • Article
  • Open Access
22 Citations
35,699 Views
15 Pages

17 October 2021

To date, there have been rapidly spreading new SARS-CoV-2 “variants of concern”. They all contain multiple mutations in the ACE2 receptor recognition site of the spike protein, compared to the original Wuhan sequence, which is of great concern, becau...

(This article belongs to the Special Issue COVID-19 in Pharmaceuticals)
  • Article
  • Open Access
4 Citations
4,580 Views
13 Pages

Identification of Novel Anthracycline Resistance Genes and Their Inhibitors

  • Onat Kadioglu,
  • Mohamed Elbadawi,
  • Edmond Fleischer and
  • Thomas Efferth

16 October 2021

Differentially expressed genes have been previously identified by us in multidrug-resistant tumor cells mainly resistant to doxorubicin. In the present study, we exemplarily focused on some of these genes to investigate their causative relationship w...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
29 Citations
9,028 Views
19 Pages

SARS-CoV-2 Fears Green: The Chlorophyll Catabolite Pheophorbide A Is a Potent Antiviral

  • Guillermo H. Jimenez-Aleman,
  • Victoria Castro,
  • Addis Londaitsbehere,
  • Marta Gutierrez-Rodríguez and ,
  • Urtzi Garaigorta,
  • Roberto Solano and
  • Pablo Gastaminza
  • + 2 authors+ 0 author

15 October 2021

SARS-CoV-2 pandemic is having devastating consequences worldwide. Although vaccination advances at good pace, effectiveness against emerging variants is unpredictable. The virus has displayed a remarkable resistance to treatments and no drugs have be...

(This article belongs to the Special Issue COVID-19 in Pharmaceuticals)
  • Article
  • Open Access
37 Citations
9,197 Views
16 Pages

Side Effects of mRNA-Based COVID-19 Vaccines among Young Adults (18–30 Years Old): An Independent Post-Marketing Study

  • Abanoub Riad,
  • Andrea Pokorná,
  • Jitka Klugarová,
  • Natália Antalová and ,
  • Lucia Kantorová,
  • Michal Koščík and
  • Miloslav Klugar
  • + 2 authors+ 0 author

15 October 2021

Young adults had been widely perceived as a low-risk group for COVID-19 severity; therefore, they were deprioritised within the mass vaccination strategies as their prognosis of COVID-19 infection is relatively more favourable than older age groups....

(This article belongs to the Section Biopharmaceuticals)
  • Review
  • Open Access
68 Citations
8,685 Views
20 Pages

Extracellular Vesicles in Human Milk

  • Yong Hu,
  • Johannes Thaler and
  • Rienk Nieuwland

15 October 2021

Milk supports the growth and development of infants. An increasing number of mostly recent studies have demonstrated that milk contains a hitherto undescribed component called extracellular vesicles (EVs). This presents questions regarding why milk c...

(This article belongs to the Special Issue Extracellular Vesicles: Biology and Emerging Therapeutic Opportunities)
  • Article
  • Open Access
12 Citations
4,740 Views
18 Pages

Pioglitazone Is a Mild Carrier-Dependent Uncoupler of Oxidative Phosphorylation and a Modulator of Mitochondrial Permeability Transition

  • Ekaterina S. Kharechkina,
  • Anna B. Nikiforova,
  • Konstantin N. Belosludtsev,
  • Tatyana I. Rokitskaya and ,
  • Yuri N. Antonenko and
  • Alexey G. Kruglov
  • + 1 author+ 0 author

14 October 2021

Pioglitazone (PIO) is an insulin-sensitizing antidiabetic drug, which normalizes glucose and lipid metabolism but may provoke heart and liver failure and chronic kidney diseases. Both therapeutic and adverse effects of PIO can be accomplished through...

(This article belongs to the Special Issue Heterocyclic Compounds and Their Application in Therapy)
  • Article
  • Open Access
38 Citations
6,275 Views
12 Pages

Corylin Ameliorates LPS-Induced Acute Lung Injury via Suppressing the MAPKs and IL-6/STAT3 Signaling Pathways

  • I-Chen Chen,
  • Shu-Chi Wang,
  • Yi-Ting Chen,
  • Hsin-Han Tseng and ,
  • Po-Len Liu,
  • Tzu-Chieh Lin,
  • Hsin-En Wu,
  • Yuan-Ru Chen,
  • Yu-Hsin Tseng and
  • Chia-Yang Li
  • + 8 authors+ 3 authors

14 October 2021

Acute lung injury (ALI) is a high mortality disease with acute inflammation. Corylin is a compound isolated from the whole plant of Psoralea corylifolia L. and has been reported to have anti-inflammatory activities. Herein, we investigated the therap...

(This article belongs to the Special Issue Lung Injury and Repair)
  • Article
  • Open Access
15 Citations
7,820 Views
20 Pages

Formulation Study of a Co-Processed, Rice Starch-Based, All-in-One Excipient for Direct Compression Using the SeDeM-ODT Expert System

  • Karnkamol Trisopon,
  • Nisit Kittipongpatana,
  • Phanphen Wattanaarsakit and
  • Ornanong Suwannapakul Kittipongpatana

14 October 2021

A co-processed, rice starch-based excipient (CS), previously developed and shown to exhibit good pharmaceutical properties, is investigated as an all-in-one excipient for direct compression (DC). An SeDeM-ODT expert system is applied to evaluate the...

(This article belongs to the Section Pharmaceutical Technology)
  • Article
  • Open Access
8 Citations
4,760 Views
19 Pages

Inhibition of 11β-HSD1 Ameliorates Cognition and Molecular Detrimental Changes after Chronic Mild Stress in SAMP8 Mice

  • Dolors Puigoriol-Illamola,
  • Júlia Companys-Alemany,
  • Kris McGuire,
  • Natalie Z. M. Homer and ,
  • Rosana Leiva,
  • Santiago Vázquez,
  • Damian J. Mole,
  • Christian Griñán-Ferré and
  • Mercè Pallàs
  • + 4 authors+ 0 author

13 October 2021

Impaired glucocorticoid (GC) signaling is a significant factor in aging, stress, and neurodegenerative diseases such as Alzheimer’s disease. Therefore, the study of GC-mediated stress responses to chronic moderately stressful situations, which occur...

(This article belongs to the Section Pharmacology)
  • Review
  • Open Access
17 Citations
6,305 Views
19 Pages

13 October 2021

Platelet concentrates have been widely used in regenerative medicine, including endodontics. The aim of this manuscript was to assess critically the efficacy of PRF in the treatment of endodontic periapical lesions in adult patients on the basis of t...

(This article belongs to the Section Pharmacology)
  • Review
  • Open Access
51 Citations
14,157 Views
25 Pages

Recent Developments in the Synthesis of β-Diketones

  • Gonzalo de Gonzalo and
  • Andrés R. Alcántara

13 October 2021

Apart from being one of the most important intermediates in chemical synthesis, broadly used in the formation of C–C bonds among other processes, the β-dicarbonyl structure is present in a huge number of biologically and pharmaceutically active compo...

(This article belongs to the Special Issue β-Diketones and Their Derivatives: Synthesis, Characterization and Biomedical Applications)
  • Article
  • Open Access
11 Citations
5,604 Views
10 Pages

Ten-Year Outcomes of Intravitreal Bevacizumab for Myopic Choroidal Neovascularization: Analysis of Prognostic Factors

  • Fabiana Mallone,
  • Rosalia Giustolisi,
  • Federica Franzone,
  • Marco Marenco and ,
  • Rocco Plateroti,
  • Marcella Nebbioso,
  • Alessandro Lambiase and
  • Magda Gharbiya
  • + 3 authors+ 0 author

13 October 2021

The current standard treatment of myopic choroidal neovascularisation (mCNV) is intravitreal injection of VEGF antagonists. This study was proposed to assess efficacy and safety of intravitreal bevacizumab (IVB) for the treatment of mCNV across a 10-...

(This article belongs to the Special Issue Advances in Ocular Pharmacology)
  • Feature Paper
  • Article
  • Open Access
13 Citations
3,839 Views
16 Pages

Esculetin Provides Neuroprotection against Mutant Huntingtin-Induced Toxicity in Huntington’s Disease Models

  • Letizia Pruccoli,
  • Carlo Breda,
  • Gabriella Teti,
  • Mirella Falconi and ,
  • Flaviano Giorgini and
  • Andrea Tarozzi
  • + 1 author+ 0 author

13 October 2021

Huntington’s disease (HD) is a neurodegenerative disorder caused by an abnormal CAG trinucleotide repeat expansion within exon 1 of the huntingtin (HTT) gene. This mutation leads to the production of mutant HTT (mHTT) protein which triggers neuronal...

(This article belongs to the Special Issue Natural Bioactive Compounds and Neurological Disorders: Exploiting Resources from Nature)
  • Article
  • Open Access
13 Citations
4,884 Views
15 Pages

Development of a Topical Amphotericin B and Bursera graveolens Essential Oil-Loaded Gel for the Treatment of Dermal Candidiasis

  • Lupe Carolina Espinoza,
  • Lilian Sosa,
  • Paulo C. Granda,
  • Nuria Bozal and ,
  • Natalia Díaz-Garrido,
  • Brenda Chulca-Torres and
  • Ana Cristina Calpena
  • + 2 authors+ 0 author

12 October 2021

The higher molecular weight and low solubility of amphotericin B (AmB) hinders its topical administration. The aim of this study was to incorporate Bursera graveolens essential oil into an AmB topical gel (AmB + BGEO gel) in order to promote the diff...

(This article belongs to the Special Issue Plant and Marine-Derived Natural Product Research in Drug Discovery: Strengths and Perspective)
  • Article
  • Open Access
16 Citations
17,006 Views
11 Pages

The Extract of Corydalis yanhusuo Prevents Morphine Tolerance and Dependence

  • Lamees Alhassen,
  • Khawla Nuseir,
  • Allyssa Ha,
  • Warren Phan and ,
  • Ilias Marmouzi,
  • Shalini Shah and
  • Olivier Civelli
  • + 2 authors+ 0 author

12 October 2021

The opioid epidemic was triggered by an overprescription of opioid analgesics. In the treatment of chronic pain, repeated opioid administrations are required which ultimately lead to tolerance, physical dependence, and addiction. A possible way to ov...

(This article belongs to the Section Natural Products)
  • Article
  • Open Access
3 Citations
3,552 Views
20 Pages

12 October 2021

Combinations of platinum-based compounds with doxorubicin in free and/or in liposomal form for improved safety are currently being evaluated in the neoadjuvant setting on patients with advanced triple-negative breast cancer (TNBC). However, TNBC may...

(This article belongs to the Special Issue Potential Molecular Targets and Therapeutics in Triple-Negative Breast Cancer)
  • Article
  • Open Access
7 Citations
3,224 Views
10 Pages

Folium Sennae Increased the Bioavailability of Methotrexate through Modulation on MRP 2 and BCRP

  • Chung-Ping Yu,
  • Yu-Hsuan Peng,
  • Ching-Ya Huang,
  • Yow-Wen Hsieh and ,
  • Yu-Chi Hou and
  • Shiuan-Pey Lin
  • + 1 author+ 0 author

12 October 2021

Folium Sennae (FS), a popular laxative (Senna), contains polyphenolic anthranoids, whose conjugation metabolites are probable modulators of multidrug resistance-associated proteins (MRPs) and breast cancer resistance protein (BCRP). We suspected that...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
8 Citations
3,478 Views
17 Pages

Thermodynamic Study of Oxidovanadium(IV) with Kojic Acid Derivatives: A Multi-Technique Approach

  • Rosita Cappai,
  • Guido Crisponi,
  • Daniele Sanna,
  • Valeria Ugone and ,
  • Andrea Melchior,
  • Eugenio Garribba,
  • Massimiliano Peana,
  • Maria Antonietta Zoroddu and
  • Valeria Marina Nurchi
  • + 4 authors+ 0 author

12 October 2021

The good chelating properties of hydroxypyrone (HPO) derivatives towards oxidovanadium(IV) cation, VIVO2+, constitute the precondition for the development of new insulin-mimetic and anticancer compounds. In the present work, we examined the VIVO2+ co...

(This article belongs to the Special Issue Applications of Medicinal Bioinorganic Chemistry)
  • Article
  • Open Access
21 Citations
5,033 Views
19 Pages

12 October 2021

The difficulties in developing novel classes of antibacterials is leading to a resurgence of interest in bacteriophages as therapeutic agents, and in particular engineered phages that can be optimally designed. Here, pre-clinical microbiology assessm...

(This article belongs to the Special Issue Bacteriophages as Therapeutic Delivery Vehicles)
  • Systematic Review
  • Open Access
11 Citations
4,811 Views
12 Pages

Somatostatin Analogue Therapy in MEN1-Related Pancreatic Neuroendocrine Tumors from Evidence to Clinical Practice: A Systematic Review

  • Anna La Salvia,
  • Franz Sesti,
  • Chiara Grinzato,
  • Rossella Mazzilli and ,
  • Maria Grazia Tarsitano,
  • Elisa Giannetta and
  • Antongiulio Faggiano
  • + 2 authors+ 0 author

12 October 2021

Neuroendocrine neoplasms (NENs) are relatively rare and complex tumors that can be sporadic or hereditary, as in the context of multiple endocrine neoplasia type 1 (MEN1) where patients display a 70% lifelong risk of developing a pancreatic NENs (pNE...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
4 Citations
3,887 Views
13 Pages

11 October 2021

Sickness behavior, characterized by on overall reduction in behavioral activity, is commonly observed after bacterial infection. Sickness behavior can also be induced by the peripheral administration of Gram-negative bacterial lipopolysaccharide (LPS...

(This article belongs to the Special Issue Cerebral Production and Action of Pro-inflammatory Cytokines)
  • Review
  • Open Access
14 Citations
6,347 Views
23 Pages

The Cross Talk between Underlying Mechanisms of Multiple Sclerosis and Epilepsy May Provide New Insights for More Efficient Therapies

  • Atefeh Rayatpour,
  • Sahar Farhangi,
  • Ester Verdaguer,
  • Jordi Olloquequi and ,
  • Jesus Ureña,
  • Carme Auladell and
  • Mohammad Javan
  • + 2 authors+ 0 author

11 October 2021

Despite the significant differences in pathological background of neurodegenerative diseases, epileptic seizures are a comorbidity in many disorders such as Huntington disease (HD), Alzheimer’s disease (AD), and multiple sclerosis (MS). Regarding the...

(This article belongs to the Special Issue Epilepsy and Neurodegeneration: Current Therapeutic Implications 2021)
  • Article
  • Open Access
9 Citations
3,462 Views
30 Pages

Mechanistic Insights into Binding of Ligands with Thiazolidinedione Warhead to Human Histone Deacetylase 4

  • Markus Schweipert,
  • Niklas Jänsch,
  • Neha Upadhyay,
  • Kalpana Tilekar and ,
  • Ewelina Wozny,
  • Sidra Basheer,
  • Eva Wurster,
  • Marlene Müller,
  • Ramaa C S and
  • Franz-Josef Meyer-Almes
  • + 5 authors+ 0 author

11 October 2021

Recently, we have reported that non-hydroxamate thiazolidinedione (TZD) analogs are capable of inhibiting human deacetylase 4 (HDAC4). This study aims at the dissection of the molecular determinants and kinetics of the molecular recognition of TZD li...

(This article belongs to the Special Issue Drug Insight: Histone Deacetylase (HDAC) Inhibitors)
  • Article
  • Open Access
13 Citations
4,457 Views
16 Pages

In Silico Studies of Potential Selective Inhibitors of Thymidylate Kinase from Variola virus

  • Danielle R. Garcia,
  • Felipe R. Souza,
  • Ana P. Guimarães,
  • Martin Valis and ,
  • Zbyšek Pavelek,
  • Kamil Kuca,
  • Teodorico C. Ramalho and
  • Tanos C. C. França
  • + 3 authors+ 0 author

9 October 2021

Continuing the work developed by our research group, in the present manuscript, we performed a theoretical study of 10 new structures derived from the antivirals cidofovir and ribavirin, as inhibitor prototypes for the enzyme thymidylate kinase from...

(This article belongs to the Special Issue In Silico Approaches in Drug Design)
  • Article
  • Open Access
14 Citations
3,426 Views
9 Pages

Graft Preservation Solution DuraGraft® Alleviates Vascular Dysfunction Following In Vitro Ischemia/Reperfusion Injury in Rats

  • Sevil Korkmaz-Icöz,
  • Belinda Ballikaya,
  • Jasmin Soethoff,
  • Patricia Kraft and ,
  • Alex Ali Sayour,
  • Tamás Radovits,
  • Sivakkanan Loganathan,
  • Matthias Karck,
  • Gábor Szabó and
  • Gábor Veres
  • + 5 authors+ 0 author

9 October 2021

Vascular ischemia/reperfusion injury (IRI) in patients undergoing coronary artery bypass grafting can result in graft failure and the need for repeat revascularization procedures. DuraGraft® has been shown to protect structure and function in sapheno...

(This article belongs to the Section Pharmacology)
  • Review
  • Open Access
8 Citations
5,971 Views
15 Pages

1,6-Naphthyridin-2(1H)-ones: Synthesis and Biomedical Applications

  • Juan Marcos Oliveras,
  • Raimon Puig de la Bellacasa,
  • Roger Estrada-Tejedor,
  • Jordi Teixidó and
  • José I. Borrell

9 October 2021

Naphthyridines, also known as diazanaphthalenes, are a group of heterocyclic compounds that include six isomeric bicyclic systems containing two pyridine rings. 1,6-Naphthyridines are one of the members of such a family capable of providing ligands f...

(This article belongs to the Special Issue Heterocyclic Compounds and Their Application in Therapy)
  • Review
  • Open Access
24 Citations
6,211 Views
17 Pages

8 October 2021

Common pathophysiological mechanisms have emerged for different neurological and neuropsychiatric conditions. In particular, mechanisms of oxidative stress, immuno-inflammation, and altered metabolic pathways converge and cause neuronal and non-neuro...

(This article belongs to the Special Issue Repurposing Drug Strategies for CNS Disorders)
  • Article
  • Open Access
9 Citations
3,827 Views
29 Pages

Modular Synthesis and Antiproliferative Activity of New Dihydro-1H-pyrazolo[1,3-b]pyridine Embelin Derivatives

  • Pedro Martín-Acosta,
  • Ángel Amesty,
  • Miguel Guerra-Rodríguez,
  • Borja Guerra and ,
  • Leandro Fernández-Pérez and
  • Ana Estévez-Braun
  • + 1 author+ 0 author

8 October 2021

A set of new dihydro-1H-pyrazolo[1,3-b]pyridine and pyrazolo[1,3-b]pyridine embelin derivatives was synthesized through a multicomponent reaction from natural embelin, 3-substituted-5-aminopyrazoles and aldehydes. The synthesized compounds were evalu...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
2 Citations
3,882 Views
29 Pages

Identification of a Novel Neuropeptide S Receptor Antagonist Scaffold Based on the SHA-68 Core

  • Allison Zarkin,
  • Rajwana Jahan,
  • Rajendra Uprety,
  • Yanan Zhang and ,
  • Charles McElhinny,
  • Rodney Snyder,
  • Elaine Gay,
  • Gabriel Jewula,
  • Heather Bool and
  • Scott Runyon
  • + 6 authors+ 1 author

6 October 2021

Activation of the neuropeptide S receptor (NPSR) system has been shown to produce anxiolytic-like actions, arousal, and enhance memory consolidation, whereas blockade of the NPSR has been shown to reduce relapse to substances of abuse and duration of...

(This article belongs to the Special Issue Pharmacology of Neuropeptide S Receptor)
  • Review
  • Open Access
68 Citations
13,077 Views
30 Pages

New Frontiers in Cancer Imaging and Therapy Based on Radiolabeled Fibroblast Activation Protein Inhibitors: A Rational Review and Current Progress

  • Surachet Imlimthan,
  • Euy Sung Moon,
  • Hendrik Rathke,
  • Ali Afshar-Oromieh and ,
  • Frank Rösch,
  • Axel Rominger and
  • Eleni Gourni
  • + 2 authors+ 0 author

5 October 2021

Over the past decade, the tumor microenvironment (TME) has become a new paradigm of cancer diagnosis and therapy due to its unique biological features, mainly the interconnection between cancer and stromal cells. Within the TME, cancer-associated fib...

(This article belongs to the Special Issue Forward Thinking towards Theranostic (Radio)ligands Targeting the Tumor Microenvironment (TME))
  • Communication
  • Open Access
3 Citations
2,608 Views
7 Pages

Prophylactic Peripheral Blood Stem Cell Collection in Patients with Extensive Bone-Marrow Infiltration of Neuroendocrine Tumours Prior to Peptide Receptor Radionuclide Therapy with 177Lu-DOTATATE

  • Amir Sabet,
  • Nicolai Mader,
  • Jörg Thomas Bittenbring,
  • Fadi Khreish and ,
  • Frank Grünwald,
  • Hans Jürgen Biersack and
  • Samer Ezziddin
  • + 2 authors+ 0 author

5 October 2021

Peptide receptor radionuclide therapy (PRRT) of metastatic neuroendocrine tumors (NET) can be successfully repeated but may eventually be dose-limited. Since 177Lu-DOTATATE dose limitation may come from hematological rather than renal function, hemat...

(This article belongs to the Section Radiopharmaceutical Sciences)
  • Article
  • Open Access
10 Citations
3,798 Views
18 Pages

Anti-Proliferative, Anti-Angiogenic and Safety Profiles of Novel HDAC Inhibitors for the Treatment of Metastatic Castration-Resistant Prostate Cancer

  • Zohaib Rana,
  • Sarah Diermeier,
  • Fearghal P. Walsh,
  • Muhammad Hanif and ,
  • Christian G. Hartinger and
  • Rhonda J. Rosengren
  • + 1 author+ 0 author

4 October 2021

Metastatic castration-resistant prostate cancer (CRPC) has a five-year survival rate of 28%. As histone deacetylases (HDACs) are overexpressed in CRPC, the HDAC inhibitor suberoylanilide hydroxamic acid (SAHA) was trialled in CRPC patients but found...

(This article belongs to the Special Issue Drug Insight: Histone Deacetylase (HDAC) Inhibitors)
  • Article
  • Open Access
33 Citations
4,437 Views
29 Pages

Design and Synthesis of Newly Synthesized Acrylamide Derivatives as Potential Chemotherapeutic Agents against MCF-7 Breast Cancer Cell Line Lodged on PEGylated Bilosomal Nano-Vesicles for Improving Cytotoxic Activity

  • Islam Zaki,
  • Reham A. I. Abou-Elkhair,
  • Ali H. Abu Almaaty,
  • Ola A. Abu Ali and ,
  • Eman Fayad,
  • Ahmed Gaafar Ahmed Gaafar and
  • Mohamed Y. Zakaria
  • + 2 authors+ 0 author

4 October 2021

Cancer is a multifaceted disease. With the development of multi drug resistance, the need for the arousal of novel targets in order to avoid these drawbacks increased. A new series of acrylamide derivatives was synthesized from starting material 4-(f...

(This article belongs to the Section Pharmaceutical Technology)
  • Opinion
  • Open Access
204 Citations
14,009 Views
25 Pages

3 October 2021

Phage therapy is the use of bacterial viruses as antibacterial agents. A primary consideration for commercial development of phages for phage therapy is the number of different bacterial strains that are successfully targeted, as this defines the bre...

(This article belongs to the Special Issue Phage Therapy and Phage-Mediated Biological Control 2021)
  • Systematic Review
  • Open Access
6 Citations
4,966 Views
20 Pages

Pharmacometabolomics by NMR in Oncology: A Systematic Review

  • Nuria Gómez-Cebrián,
  • Pedro Vázquez Ferreiro,
  • Francisco Javier Carrera Hueso,
  • José Luis Poveda Andrés and ,
  • Leonor Puchades-Carrasco and
  • Antonio Pineda-Lucena
  • + 1 author+ 0 author

2 October 2021

Pharmacometabolomics (PMx) studies aim to predict individual differences in treatment response and in the development of adverse effects associated with specific drug treatments. Overall, these studies inform us about how individuals will respond to...

(This article belongs to the Special Issue High Field NMR and Ultra-High Field NMR in Medicinal Chemistry)
  • Technical Note
  • Open Access
7 Citations
3,478 Views
14 Pages

Optimization of Synthesis of the Amino Lipid ECO for Effective Delivery of Nucleic Acids

  • Andrew L. Schilb,
  • Josef H. Scheidt,
  • Amita M. Vaidya,
  • Zhanhu Sun and ,
  • Da Sun,
  • Sangjoon Lee and
  • Zheng-Rong Lu
  • + 2 authors+ 0 author

2 October 2021

Nucleic acids are promising for a variety of therapies, such as cancer therapy and the gene therapy of genetic disorders. The therapeutic efficacy of nucleic acids is reliant on the ability of their efficient delivery to the cytosol of the target cel...

(This article belongs to the Topic Compounds with Medicinal Value)
  • Communication
  • Open Access
21 Citations
5,696 Views
10 Pages

Withasomniferol D, a New Anti-Adipogenic Withanolide from the Roots of Ashwagandha (Withania somnifera)

  • Bum Soo Lee,
  • Min Jeong Yoo,
  • Heesun Kang,
  • Seoung Rak Lee and ,
  • Sil Kim,
  • Jae Sik Yu,
  • Jin-Chul Kim,
  • Tae Su Jang,
  • Changhyun Pang and
  • Ki Hyun Kim
  • + 5 authors+ 0 author

2 October 2021

Withania somnifera (Solanaceae), well-known as ‘Indian ginseng’ or ‘Ashwagandha’, is a medicinal plant that is used in Ayurvedic practice to promote good health and longevity. As part of an ongoing investigation for bioactive natural products with no...

(This article belongs to the Special Issue Searching for New Therapeutic Targets with Anti-obesity Potential)
  • Article
  • Open Access
27 Citations
5,385 Views
17 Pages

2 October 2021

The balsam poplar (Populus balsamifera L.) buds that grow in Lithuania are a polyphenol-rich plant material with a chemical composition close to that of propolis. In order to potentially adapt the extracts of this plant’s raw material for therapeutic...

(This article belongs to the Special Issue Bioactive Compounds from Plants and Foods with Pharmaceutical Interest 2022)
  • Article
  • Open Access
7 Citations
3,907 Views
18 Pages

Zinc Binding to NAP-Type Neuroprotective Peptides: Nuclear Magnetic Resonance Studies and Molecular Modeling

  • Ancuta-Veronica Lupaescu,
  • Cosmin Stefan Mocanu,
  • Gabi Drochioiu and
  • Catalina-Ionica Ciobanu

1 October 2021

Aggregation of amyloid-β peptides (Aβ) is a hallmark of Alzheimer’s disease (AD), which is affecting an increasing number of people. Hence, there is an urgent need to develop new pharmaceutical treatments which could be used to prevent the AD symptom...

(This article belongs to the Special Issue High Field NMR and Ultra-High Field NMR in Medicinal Chemistry)

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Pharmaceuticals - ISSN 1424-8247