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Pharmaceuticals, Volume 15, Issue 5

2022 May - 154 articles

Cover Story: The depth and versatility of siRNA technologies enable their use in disease targets that cannot be drugged using small molecules. Major extracellular barriers enzymatically degrade siRNAs through several pathways, such as endonucleases and serum RNAases, renal clearance of the siRNA delivery system, and capillary endothelium crossing. To overcome the intrinsic difficulties of using siRNA molecules, therapeutic applications require nanometric delivery carriers to protect double strands and deliver molecules to target cells. This review discusses the history of siRNAs, siRNA design, and delivery strategies, with a focus on progress made regarding siRNA molecules in clinical trials and how siRNA has become a valuable asset for biopharmaceutical companies. View this paper
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Articles (154)

  • Systematic Review
  • Open Access
18 Citations
5,079 Views
14 Pages

Mono or Dual Antiplatelet Therapy for Treating Patients with Peripheral Artery Disease after Lower Extremity Revascularization: A Systematic Review and Meta-Analysis

  • Shang-Yu Tsai,
  • Ying-Sheng Li,
  • Che-Hsiung Lee,
  • Shion-Wei Cha and ,
  • Yao-Chang Wang,
  • Ta-Wei Su,
  • Sheng-Yueh Yu and
  • Chi-Hsiao Yeh
  • + 3 authors+ 0 author

The efficacy of dual antiplatelet therapy (DAPT) for patients with peripheral artery disease (PAD) after lower-limb intervention remains controversial. Currently, the prescription of DAPT after an intervention is not fully recommended in guidelines d...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
17 Citations
4,823 Views
12 Pages

Biodistribution of Intra-Arterial and Intravenous Delivery of Human Umbilical Cord Mesenchymal Stem Cell-Derived Extracellular Vesicles in a Rat Model to Guide Delivery Strategies for Diabetes Therapies

  • Junfeng Li,
  • Hirotake Komatsu,
  • Erasmus K. Poku,
  • Tove Olafsen and ,
  • Kelly X. Huang,
  • Lina A. Huang,
  • Junie Chea,
  • Nicole Bowles,
  • Betty Chang and
  • Fouad R. Kandeel
  • + 9 authors+ 4 authors

Umbilical cord mesenchymal stem cell-derived extracellular vesicles (UC-MSC-EVs) have become an emerging strategy for treating various autoimmune and metabolic disorders, particularly diabetes. Delivery of UC-MSC-EVs is essential to ensure optimal ef...

(This article belongs to the Special Issue In Vivo Nuclear Molecular Imaging in Drug Development and Pharmacological Research)
  • Article
  • Open Access
12 Citations
4,919 Views
13 Pages

Safety and Tolerability of Ivermectin and Albendazole Mass Drug Administration in Lymphatic Filariasis Endemic Communities of Tanzania: A Cohort Event Monitoring Study

  • Adam M. Fimbo,
  • Omary Mashiku Minzi,
  • Bruno P. Mmbando,
  • Parthasarathi Gurumurthy and ,
  • Appolinary A. R. Kamuhabwa and
  • Eleni Aklillu
  • + 1 author+ 0 author

Ivermectin and albendazole (IA) combination preventive chemotherapy to all at-risk populations is deployed to eliminate lymphatic filariasis. Although safety monitoring is imperative, data from Sub-Saharan Africa is scarce. We conducted a large-scale...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
23 Citations
4,953 Views
16 Pages

Nobiletin Ameliorates Cellular Damage and Stress Response and Restores Neuronal Identity Altered by Sodium Arsenate Exposure in Human iPSCs-Derived hNPCs

  • Sadaf Jahan,
  • Uzair Ahmad Ansari,
  • Arif Jamal Siddiqui,
  • Danish Iqbal and ,
  • Johra Khan,
  • Saeed Banawas,
  • Bader Alshehri,
  • Mohammed Merae Alshahrani,
  • Suliman A. Alsagaby and
  • Aditya Bhushan Pant
  • + 6 authors+ 1 author

Environmental exposure to arsenic has been profoundly associated with chronic systemic disorders, such as neurodegeneration, in both experimental models and clinical studies. The neuronal cells of the brain and the nervous system have a limited regen...

(This article belongs to the Special Issue Drug Screening or Drug Designing Based on Stem Cell Models)
  • Article
  • Open Access
17 Citations
5,636 Views
20 Pages

Mangifera indica ‘Namdokmai’ Prevents Neuronal Cells from Amyloid Peptide Toxicity and Inhibits BACE-1 Activities in a Drosophila Model of Alzheimer’s Amyloidosis

  • Piya Temviriyanukul,
  • Suwapat Kittibunchakul,
  • Piyapat Trisonthi,
  • Thanit Kunkeaw and ,
  • Woorawee Inthachat,
  • Dalad Siriwan and
  • Uthaiwan Suttisansanee
  • + 2 authors+ 0 author

Alzheimer’s disease (AD) is a progressive neurological illness with few effective treatments. Thus, ameliorating the effects of AD using natural products has attracted global attention with promising efficacy and safety. In this study, ten trop...

(This article belongs to the Special Issue Bioactive Compounds from Plants and Foods with Pharmaceutical Interest 2022)
  • Review
  • Open Access
13 Citations
9,481 Views
24 Pages

Targeting the Hematopoietic Stem Cell Niche in β-Thalassemia and Sickle Cell Disease

  • Annamaria Aprile,
  • Silvia Sighinolfi,
  • Laura Raggi and
  • Giuliana Ferrari

In the last decade, research on pathophysiology and therapeutic solutions for β-thalassemia (BThal) and sickle cell disease (SCD) has been mostly focused on the primary erythroid defect, thus neglecting the study of hematopoietic stem cells (HSC...

(This article belongs to the Special Issue Drug Design and Development for Rare Hematologic Diseases)
  • Article
  • Open Access
16 Citations
4,820 Views
13 Pages

[99mTc]Tc-iFAP Radioligand for SPECT/CT Imaging of the Tumor Microenvironment: Kinetics, Radiation Dosimetry, and Imaging in Patients

  • Luis Coria-Domínguez,
  • Paola Vallejo-Armenta,
  • Myrna Luna-Gutiérrez,
  • Blanca Ocampo-García and ,
  • Brenda Gibbens-Bandala,
  • Francisco García-Pérez,
  • Gerardo Ramírez-Nava,
  • Clara Santos-Cuevas and
  • Guillermina Ferro-Flores
  • + 4 authors+ 0 author

Tumor microenvironment fibroblasts overexpress the fibroblast activation protein (FAP). We recently reported the preclinical evaluation of [99mTc]Tc-iFAP as a new SPECT radioligand capable of detecting FAP. This research aimed to evaluate the kinetic...

(This article belongs to the Special Issue Tumor-Targeting Radioligands for Molecular Imaging and Therapy)
  • Review
  • Open Access
25 Citations
5,514 Views
27 Pages

Effect of Statins on Lung Cancer Molecular Pathways: A Possible Therapeutic Role

  • Gianmarco Marcianò,
  • Caterina Palleria,
  • Alessandro Casarella,
  • Vincenzo Rania and ,
  • Emanuele Basile,
  • Luca Catarisano,
  • Cristina Vocca,
  • Luigi Bianco,
  • Corrado Pelaia and
  • Luca Gallelli
  • + 9 authors+ 4 authors

Lung cancer is a common neoplasm, usually treated through chemotherapy, radiotherapy and/or surgery. Both clinical and experimental studies on cancer cells suggest that some drugs (e.g., statins) have the potential to improve the prognosis of cancer....

(This article belongs to the Special Issue Statins Use and Cancer)
  • Article
  • Open Access
10 Citations
4,717 Views
15 Pages

Synthesis and Antioxidant/Anti-Inflammatory Activity of 3-Arylphthalides

  • María J. Ortega,
  • Belén Parra-Torrejón,
  • Fátima Cano-Cano,
  • Laura Gómez-Jaramillo and ,
  • M. Carmen González-Montelongo and
  • Eva Zubía
  • + 1 author+ 0 author

Phthalides are a group of compounds with relevant biological activities in different areas such as cytotoxicity, anti-stroke activity, neuroprotection, and inflammation, among others. In this study we designed and synthesized a series of 3-arylphthal...

(This article belongs to the Section Natural Products)
  • Article
  • Open Access
5 Citations
3,939 Views
14 Pages

Isotopic Radiolabeling of the Antiretroviral Drug [18F]Dolutegravir for Pharmacokinetic PET Imaging

  • Marion Tisseraud,
  • Sébastien Goutal,
  • Thomas Bonasera,
  • Maud Goislard and ,
  • Delphine Desjardins,
  • Roger Le Grand,
  • Chris M. Parry,
  • Nicolas Tournier,
  • Bertrand Kuhnast and
  • Fabien Caillé
  • + 5 authors+ 0 author

Deciphering the drug/virus/host interactions at infected cell reservoirs is a key leading to HIV-1 remission for which positron emission tomography (PET) imaging using radiolabeled antiretroviral (ARV) drugs is a powerful asset. Dolutegravir (DTG) is...

(This article belongs to the Section Radiopharmaceutical Sciences)
  • Article
  • Open Access
10 Citations
4,703 Views
22 Pages

Promising Antibacterial and Antifungal Agents Based on Thiolated Vitamin K3 Analogs: Synthesis, Bioevaluation, Molecular Docking

  • Hatice Yıldırım,
  • Mahmut Yıldız,
  • Nilüfer Bayrak,
  • Emel Mataracı-Kara and ,
  • Mohamed Osman Radwan,
  • Ayse Tarbin Jannuzzi,
  • Masami Otsuka,
  • Mikako Fujita and
  • Amaç Fatih TuYuN
  • + 4 authors+ 0 author

In the present study, we designed and synthesized thiolated VK3 analogs (VK3a–g) along with an extensive antimicrobial study. After the evaluation of the antibacterial and antifungal activity against various bacterial and fungal strains, we pre...

(This article belongs to the Special Issue Privileged Structures as Leads in Medicinal Chemistry)
  • Article
  • Open Access
6 Citations
4,235 Views
30 Pages

Design, Semisynthesis, and Estrogenic Activity of Lignan Derivatives from Natural Dibenzylbutyrolactones

  • Priscila López-Rojas,
  • Ángel Amesty,
  • Miguel Guerra-Rodríguez,
  • Yeray Brito-Casillas and ,
  • Borja Guerra,
  • Leandro Fernández-Pérez and
  • Ana Estévez-Braun
  • + 2 authors+ 0 author

Based on molecular docking studies on the ERα, a series of lignan derivatives (3–16) were designed and semisynthesized from the natural dibenzylbutyrolactones bursehernin (1) and matairesinol dimethyl ether (2). To examine their estrogeni...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
8 Citations
5,374 Views
20 Pages

Virtual Screening Based on Machine Learning Explores Mangrove Natural Products as KRASG12C Inhibitors

  • Lianxiang Luo,
  • Tongyu Zheng,
  • Qu Wang,
  • Yingling Liao and ,
  • Xiaoqi Zheng,
  • Ai Zhong,
  • Zunnan Huang and
  • Hui Luo
  • + 3 authors+ 0 author

Mangrove secondary metabolites have many unique biological activities. We identified lead compounds among them that might target KRASG12C. KRAS is considered to be closely related to various cancers. A variety of novel small molecules that directly t...

(This article belongs to the Special Issue In Silico Approaches in Drug Design)
  • Review
  • Open Access
12 Citations
8,495 Views
18 Pages

Future Prospects of Positron Emission Tomography–Magnetic Resonance Imaging Hybrid Systems and Applications in Psychiatric Disorders

  • Young-Don Son,
  • Young-Bo Kim,
  • Jong-Hoon Kim,
  • Jeong-Hee Kim and ,
  • Dae-Hyuk Kwon,
  • Haigun Lee and
  • Zang-Hee Cho
  • + 2 authors+ 0 author

A positron emission tomography (PET)–magnetic resonance imaging (MRI) hybrid system has been developed to improve the accuracy of molecular imaging with structural imaging. However, the mismatch in spatial resolution between the two systems hin...

(This article belongs to the Special Issue In Vivo Nuclear Molecular Imaging in Drug Development and Pharmacological Research)
  • Article
  • Open Access
14 Citations
3,597 Views
14 Pages

Purinoceptor Targeted Cytotoxicity of Adenosine Triphosphate-Conjugated Biogenic Selenium Nanoparticles in Human Colon Cancer Cells

  • Kandasamy Saravanakumar,
  • Anbazhagan Sathiyaseelan,
  • Xin Zhang,
  • Soyoung Park and
  • Myeong-Hyeon Wang

The adenosine triphosphate (ATP)-conjugated biogenic selenium nanoparticles (SeNPs) for P2 (purinoceptors) receptor-targeted anti-colon cancer activity were developed in this study. First, the SeNPs were synthesized using Trichoderma extracts (TE) an...

(This article belongs to the Special Issue Synthesis of Metal Nanoparticles and Their Pharmaceutical Applications)
  • Review
  • Open Access
65 Citations
7,537 Views
18 Pages

Advances in Research on Antiviral Activities of Sulfated Polysaccharides from Seaweeds

  • Qiang Wei,
  • Guoqiang Fu,
  • Ke Wang,
  • Qiong Yang and ,
  • Jiarui Zhao,
  • Yuan Wang,
  • Kai Ji and
  • Shuliang Song
  • + 3 authors+ 0 author

In recent years, various viral diseases have suddenly erupted, resulting in widespread infection and death. A variety of biological activities from marine natural products have gradually attracted the attention of people. Seaweeds have a wide range o...

(This article belongs to the Special Issue Polysaccharide-Based Nanoparticles for Theranostic Nanomedicine)
  • Article
  • Open Access
11 Citations
4,963 Views
20 Pages

Improving Antimicrobial Activity and Physico-Chemical Properties by Isosteric Replacement of 2-Aminothiazole with 2-Aminooxazole

  • Martin Juhás,
  • Andrea Bachtíková,
  • Daria Elżbieta Nawrot,
  • Paulína Hatoková and ,
  • Vinod Sukanth Kumar Pallabothula,
  • Adéla Diepoltová,
  • Ondřej Janďourek,
  • Pavel Bárta,
  • Klára Konečná and
  • Jan Zitko
  • + 7 authors+ 2 authors

Antimicrobial drug resistance is currently one of the most critical health issues. Pathogens resistant to last-resort antibiotics are increasing, and very few effective antibacterial agents have been introduced in recent years. The promising drug can...

(This article belongs to the Section Medicinal Chemistry)
  • Article
  • Open Access
11 Citations
3,489 Views
14 Pages

Effects of the Prior Use of Statins on Head and Neck Cancer Risk: A Hospital-Based Case–Control Study

  • Constanza Saka-Herrán,
  • Enric Jané-Salas,
  • Antonio Mano-Azul,
  • Aina Torrejón-Moya and ,
  • Albert Estrugo-Devesa and
  • José López-López
  • + 1 author+ 0 author

Mechanisms related to the potential beneficial effects of statins on cancer are mainly related to the inhibition of the mevalonate pathway. The purpose of this study was to assess the association between prior use of statins and the risk of head and...

(This article belongs to the Special Issue Statins Use and Cancer)
  • Article
  • Open Access
11 Citations
4,457 Views
17 Pages

Food-Derived β-Carboline Alkaloids Ameliorate Lipid Droplet Accumulation in Human Hepatocytes

  • Dya Fita Dibwe,
  • Saki Oba,
  • Nire Takeishi,
  • Toshihiro Sakurai and ,
  • Takayuki Tsukui,
  • Hitoshi Chiba and
  • Shu-Ping Hui
  • + 2 authors+ 0 author

Lipid droplet accumulation (LDA) in hepatocytes is the initial stage of nonalcoholic fatty liver disease (NAFLD). In the search for natural compounds for the prevention of NAFLD, a series of β-carboline alkaloid derivatives, inspired by flazin a...

(This article belongs to the Special Issue Bioactive Compounds from Plants and Foods with Pharmaceutical Interest 2022)
  • Article
  • Open Access
8 Citations
4,215 Views
15 Pages

Report of Exosomes Isolated from a Human Uterine Leiomyoma Cell Line and Their Impact on Endometrial Vascular Endothelial Cells

  • Antonia Navarro,
  • Maria Victoria Bariani,
  • Hang-Soo Park,
  • Ami R. Zota and
  • Ayman Al-Hendy

Uterine leiomyomas are the most common pelvic tumor in women of reproductive age; they cause irregular heavy menstrual bleeding leading to anemia and subsequent negative effects on quality of life. Exosomes have arisen as main players of disease prog...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
41 Citations
5,444 Views
19 Pages

New Quinoline–Urea–Benzothiazole Hybrids as Promising Antitubercular Agents: Synthesis, In Vitro Antitubercular Activity, Cytotoxicity Studies, and In Silico ADME Profiling

  • Rashmika Moodley,
  • Chakes Mashaba,
  • Goitsemodimo H. Rakodi,
  • Nomagugu B. Ncube and ,
  • Mabuatsela V. Maphoru,
  • Mohammed O. Balogun,
  • Audrey Jordan,
  • Digby F. Warner,
  • Rene Khan and
  • Matshawandile Tukulula
  • + 5 authors+ 0 author

A series of 25 new benzothiazole–urea–quinoline hybrid compounds were synthesized successfully via a three-step synthetic sequence involving an amidation coupling reaction as a critical step. The structures of the synthesized compounds were confirmed...

(This article belongs to the Special Issue Heterocyclic Compounds and Their Application in Therapy)
  • Review
  • Open Access
30 Citations
12,287 Views
21 Pages

Biotechnological Evolution of siRNA Molecules: From Bench Tool to the Refined Drug

  • Danielle de Brito e Cunha,
  • Ana Beatriz Teixeira Frederico,
  • Tamiris Azamor,
  • Juliana Gil Melgaço and ,
  • Patricia Cristina da Costa Neves,
  • Ana Paula Dinis Ano Bom,
  • Tatiana Martins Tilli and
  • Sotiris Missailidis
  • + 3 authors+ 0 author

The depth and versatility of siRNA technologies enable their use in disease targets that are undruggable by small molecules or that seek to achieve a refined turn-off of the genes for any therapeutic area. Major extracellular barriers are enzymatic d...

(This article belongs to the Special Issue siRNA Therapeutics: From Bench Lab to Clinics)
  • Article
  • Open Access
25 Citations
5,943 Views
13 Pages

Activation of Host-NLRP3 Inflammasome in Myeloid Cells Dictates Response to Anti-PD-1 Therapy in Metastatic Breast Cancers

  • Isak W. Tengesdal,
  • Suzhao Li,
  • Nicholas E. Powers,
  • Makenna May and ,
  • Charles P. Neff,
  • Leo A. B. Joosten,
  • Carlo Marchetti and
  • Charles A. Dinarello
  • + 3 authors+ 0 author

Tumor-associated inflammation leads to dysregulated cytokine production that promotes tumor immune evasion and anti-tumor immunity dysfunction. In advanced stage breast cancer, the proinflammatory cytokine IL-1β is overexpressed due to large pro...

(This article belongs to the Special Issue Novel Therapeutic Targets in Cancer)
  • Article
  • Open Access
3 Citations
3,751 Views
14 Pages

Substituted Purines as High-Affinity Histamine H3 Receptor Ligands

  • Christian Espinosa-Bustos,
  • Luisa Leitzbach,
  • Tito Añazco,
  • María J. Silva and ,
  • Andrea del Campo,
  • Alejandro Castro-Alvarez,
  • Holger Stark and
  • Cristian O. Salas
  • + 3 authors+ 0 author

Continuing with our program to obtain new histamine H3 receptor (H3R) ligands, in this work we present the synthesis, H3R affinity and in silico studies of a series of eight new synthetically accessible purine derivatives. These compounds are designe...

(This article belongs to the Special Issue Heterocyclic Compounds and Their Application in Therapy)
  • Review
  • Open Access
549 Citations
51,957 Views
33 Pages

Network Pharmacology Approach for Medicinal Plants: Review and Assessment

  • Fatima Noor,
  • Muhammad Tahir ul Qamar,
  • Usman Ali Ashfaq,
  • Aqel Albutti and ,
  • Ameen S. S. Alwashmi and
  • Mohammad Abdullah Aljasir
  • + 1 author+ 0 author

Natural products have played a critical role in medicine due to their ability to bind and modulate cellular targets involved in disease. Medicinal plants hold a variety of bioactive scaffolds for the treatment of multiple disorders. The less adverse...

(This article belongs to the Special Issue Systems Biology and Network Pharmacology in Phytotherapy of Stress-Induced Disorders)
  • Review
  • Open Access
3 Citations
6,424 Views
36 Pages

Radiotracers for the Central Serotoninergic System

  • Reynald Mangeant,
  • Emmanuelle Dubost,
  • Thomas Cailly and
  • Valérie Collot

This review lists the most important radiotracers described so far for imaging the central serotoninergic system. Single-photon emission computed tomography and positron emission tomography radiotracers are reviewed and critically discussed for each...

(This article belongs to the Special Issue Alliance of PET/SPECT Imaging and Drug Design/Discovery for the Development of Novel Diagnostic or Therapeutic Tools)
  • Article
  • Open Access
24 Citations
6,285 Views
13 Pages

Carbonic Anhydrase IX-Targeted α-Radionuclide Therapy with 225Ac Inhibits Tumor Growth in a Renal Cell Carcinoma Model

  • Robin I. J. Merkx,
  • Mark Rijpkema,
  • Gerben M. Franssen,
  • Annemarie Kip and ,
  • Bart Smeets,
  • Alfred Morgenstern,
  • Frank Bruchertseifer,
  • Eddie Yan,
  • Michael P. Wheatcroft and
  • Sandra Heskamp
  • + 7 authors+ 2 authors

In this study, we compared the tumor-targeting properties, therapeutic efficacy, and tolerability of the humanized anti-CAIX antibody (hG250) labeled with either the α-emitter actinium-225 (225Ac) or the β--emitter lutetium-177 (177Lu) in...

(This article belongs to the Special Issue Targeted Radionuclide Therapy (TRNT) in Modern Cancer Management)
  • Brief Report
  • Open Access
21 Citations
4,915 Views
10 Pages

Microglia play pivotal roles in central nervous system development, homeostasis, responses to trauma, and neurodegenerative and neuropsychiatric disorders with significant sex-bias in their symptoms and prevalence. Survival of the microglia in adult...

(This article belongs to the Topic Compounds with Medicinal Value)
  • Article
  • Open Access
54 Citations
8,304 Views
31 Pages

Development of Dapagliflozin Solid Lipid Nanoparticles as a Novel Carrier for Oral Delivery: Statistical Design, Optimization, In-Vitro and In-Vivo Characterization, and Evaluation

  • Aziz Unnisa,
  • Ananda K. Chettupalli,
  • Turki Al Hagbani,
  • Mohammad Khalid and ,
  • Suresh B. Jandrajupalli,
  • Swarnalatha Chandolu and
  • Talib Hussain
  • + 2 authors+ 0 author

Controlling hyperglycemia and avoiding glucose reabsorption are significant goals in type 2 diabetes treatments. Among the numerous modes of medication administration, the oral route is the most common. Introduction: Dapagliflozin is an oral hypoglyc...

(This article belongs to the Special Issue Current Insights on Lipid-Based Nanosystems)
  • Article
  • Open Access
19 Citations
5,882 Views
20 Pages

Unassisted and Carbon Dioxide-Assisted Hydro- and Steam-Distillation: Modelling Kinetics, Energy Consumption and Chemical and Biological Activities of Volatile Oils

  • Sara El-Kharraf,
  • Soukaïna El-Guendouz,
  • Farah Abdellah,
  • El Mestafa El Hadrami and ,
  • Alexandra M. Machado,
  • Cláudia S. Tavares,
  • Ana Cristina Figueiredo and
  • Maria Graça Miguel
  • + 3 authors+ 0 author

The demand for more suitable eco-friendly extraction processes has grown over the last few decades and driven research to develop efficient extraction processes with low energy consumption and low costs, but always assuring the quality of the volatil...

(This article belongs to the Special Issue Prospects of Essential Oils in Drug Discovery)
  • Article
  • Open Access
13 Citations
5,557 Views
18 Pages

Proteomic Network Analysis of Bronchoalveolar Lavage Fluid in Ex-Smokers to Discover Implicated Protein Targets and Novel Drug Treatments for Chronic Obstructive Pulmonary Disease

  • Manoj J. Mammen,
  • Chengjian Tu,
  • Matthew C. Morris,
  • Spencer Richman and ,
  • William Mangione,
  • Zackary Falls,
  • Jun Qu,
  • Gordon Broderick,
  • Sanjay Sethi and
  • Ram Samudrala
  • + 5 authors+ 0 author

Bronchoalveolar lavage of the epithelial lining fluid (BALF) can sample the profound changes in the airway lumen milieu prevalent in chronic obstructive pulmonary disease (COPD). We compared the BALF proteome of ex-smokers with moderate COPD who are...

(This article belongs to the Special Issue Lung Injury and Repair)
  • Article
  • Open Access
32 Citations
12,868 Views
17 Pages

A Focus on Abuse/Misuse and Withdrawal Issues with Selective Serotonin Reuptake Inhibitors (SSRIs): Analysis of Both the European EMA and the US FAERS Pharmacovigilance Databases

  • Stefania Chiappini,
  • Rachel Vickers-Smith,
  • Amira Guirguis,
  • John Martin Corkery and ,
  • Giovanni Martinotti and
  • Fabrizio Schifano
  • + 1 author+ 0 author

Despite increasing reports, antidepressant (AD) misuse and dependence remain underestimated issues, possibly due to limited epidemiological and pharmacovigilance evidence. Thus, here we aimed to determine available pharmacovigilance misuse/abuse/depe...

(This article belongs to the Special Issue Psychoactive Substances: Pharmacology and Toxicology)
  • Article
  • Open Access
34 Citations
6,720 Views
23 Pages

Antifungal Thiazolidines: Synthesis and Biological Evaluation of Mycosidine Congeners

  • Igor B. Levshin,
  • Alexander Y. Simonov,
  • Sergey N. Lavrenov,
  • Alexey A. Panov and ,
  • Natalia E. Grammatikova,
  • Alexander A. Alexandrov,
  • Eslam S. M. O. Ghazy,
  • Nikita A. Savin,
  • Peter V. Gorelkin and
  • Vladimir I. Polshakov
  • + 6 authors+ 1 author

Novel derivatives of Mycosidine (3,5-substituted thiazolidine-2,4-diones) are synthesized by Knoevenagel condensation and reactions of thiazolidines with chloroformates or halo-acetic acid esters. Furthermore, 5-Arylidene-2,4-thiazolidinediones and t...

(This article belongs to the Topic Compounds with Medicinal Value)
  • Review
  • Open Access
38 Citations
12,635 Views
94 Pages

Functionalized Nitroimidazole Scaffold Construction and Their Pharmaceutical Applications: A 1950–2021 Comprehensive Overview

  • Ria Gupta,
  • Sumit Sharma,
  • Rohit Singh,
  • Ram A. Vishwakarma and ,
  • Serge Mignani and
  • Parvinder Pal Singh
  • + 1 author+ 0 author

30 April 2022

Nitroimidazole represents one of the most essential and unique scaffolds in drug discovery since its discovery in the 1950s. It was K. Maeda in Japan who reported in 1953 the first nitroimidazole as a natural product from Nocardia mesenterica with an...

(This article belongs to the Special Issue Nitro Group Containing Drugs)
  • Article
  • Open Access
17 Citations
5,286 Views
16 Pages

Cathepsin B-Cleavable Polymeric Photosensitizer Prodrug for Selective Photodynamic Therapy: In Vitro Studies

  • Manish Jain,
  • Jordan Bouilloux,
  • Ines Borrego,
  • Stéphane Cook and ,
  • Hubert van den Bergh,
  • Norbert Lange,
  • Georges Wagnieres and
  • Marie-Noelle Giraud
  • + 3 authors+ 0 author

30 April 2022

Cathepsin B is a lysosomal cysteine protease that plays an important role in cancer, atherosclerosis, and other inflammatory diseases. The suppression of cathepsin B can inhibit tumor growth. The overexpression of cathepsin B can be used for the imag...

(This article belongs to the Special Issue Photodynamic Therapy 2022)
  • Review
  • Open Access
27 Citations
9,786 Views
16 Pages

30 April 2022

Induced pluripotent stem cells (iPSCs) are terminally differentiated somatic cells that differentiate into various cell types. iPSCs are expected to be used for disease modeling and for developing novel treatments because differentiated cells from iP...

(This article belongs to the Special Issue Drug Screening or Drug Designing Based on Stem Cell Models)
  • Article
  • Open Access
17 Citations
6,006 Views
18 Pages

Pulmonary Targeting of Levofloxacin Using Microsphere-Based Dry Powder Inhalation

  • Turki Al Hagbani,
  • Bhavya Vishwa,
  • Amr S. Abu Lila,
  • Hadil Faris Alotaibi and ,
  • El-Sayed Khafagy,
  • Afrasim Moin and
  • Devegowda V. Gowda
  • + 2 authors+ 0 author

30 April 2022

The objective of the current study was to develop poly (lactic-co-glycolic acid) (PLGA) microspheres loaded with the anti-tuberculosis (anti-TB) fluoroquinolone, Levofloxacin (LVX), in the form of dry powder inhalation (DPI). LVX-loaded microspheres...

(This article belongs to the Special Issue Drug Delivery to the Lungs: Challenges and Opportunities)
  • Article
  • Open Access
4 Citations
4,048 Views
16 Pages

Bioassay-Guided Isolation of 2-[p-(2-Carboxyhydrazino)phenoxy]-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol from Oroxylum indicum and the Investigation of Its Molecular Mechanism Action of Apoptosis Induction

  • Asem Robinson Singh,
  • Salam Asbin Singh,
  • Thangjam Davis Singh,
  • Naorem Tarundas Singh and ,
  • Takhellambam Chanu Machathoibi,
  • Okram Mukherjee Singh and
  • Lisam Shanjukumar Singh
  • + 2 authors+ 0 author

30 April 2022

The leaf crude extract of Oroxylum indicum (L.) Kurz induces genomic DNA fragmentation, comet formation, and the inhibition of cell proliferation in the prostate cancer cell line PC3, as assessed by agarose gel electrophoresis, comet assay and MTT as...

(This article belongs to the Section Natural Products)
  • Article
  • Open Access
19 Citations
6,125 Views
14 Pages

Aptamer–Gemcitabine Conjugates with Enzymatically Cleavable Linker for Targeted Delivery and Intracellular Drug Release in Cancer Cells

  • Jianjun Qi,
  • Zihua Zeng,
  • Zhenghu Chen,
  • Cole Nipper and ,
  • Xiaohui Liu,
  • Quanyuan Wan,
  • Jian Chen,
  • Ching-Hsuan Tung and
  • Youli Zu
  • + 4 authors+ 0 author

30 April 2022

Gemcitabine is a chemotherapeutic used clinically to treat a variety of cancers. However, because it lacks tumor cell specificity, gemcitabine may cause off-target cytotoxicity and adversely impact patients. To impart cancer cell specificity to gemci...

(This article belongs to the Special Issue Potential of the Aptamers to Fill Therapeutic and Diagnostic Gaps)
  • Review
  • Open Access
8 Citations
3,667 Views
17 Pages

30 April 2022

Checkpoint inhibitors (CPI) represent a novel therapeutical strategy with a high efficacy both in solid and hematological cancers. They act by reactivating the immune system against neoplastic cells but may, in turn, cause immune-related adverse even...

(This article belongs to the Section Pharmacology)
  • Article
  • Open Access
11 Citations
4,179 Views
20 Pages

Identification of Potential RBPJ-Specific Inhibitors for Blocking Notch Signaling in Breast Cancer Using a Drug Repurposing Strategy

  • Mengjie Rui,
  • Min Cai,
  • Yu Zhou,
  • Wen Zhang and ,
  • Lianglai Gao,
  • Ke Mi,
  • Wei Ji,
  • Dan Wang and
  • Chunlai Feng
  • + 4 authors+ 0 author

29 April 2022

Notch signaling is a key parameter in regulating cell fate during tissue homeostasis, and an aberrant Notch pathway can result in mammary gland carcinoma and has been associated with poor breast cancer diagnosis. Although inhibiting Notch signaling w...

(This article belongs to the Special Issue Recent Progress of Nanomedicine and Targeted Drug Delivery for Cancer Treatment)
  • Article
  • Open Access
9 Citations
6,679 Views
15 Pages

Development of a Hospital Compounded, Taste-Masked, Temozolomide Oral Suspension and 5-Year Real-Life Experience in Treating Paediatric Patients

  • Maxime Annereau,
  • Mélanie Hinterlang,
  • Hugues Bienayme,
  • Gilles Vassal and ,
  • Antoine Pinon,
  • Mathieu Schmitt,
  • Lucas Denis,
  • Caroline Lemarchand,
  • Laurent Martin and
  • Lionel Tortolano
  • + 8 authors+ 3 authors

29 April 2022

The development of oral pediatric forms by pharmaceutical companies is still insufficient. In fact, many drugs used in paediatric oncology, such as temozolomide, are not labeled and adapted for paediatric use. Temozolomide (TMZ) is an alkylating agen...

(This article belongs to the Special Issue Recent Advance in Oral Drug Delivery Development)
  • Article
  • Open Access
6 Citations
3,865 Views
27 Pages

Substrate-Based Design of Cytosolic Nucleotidase IIIB Inhibitors and Structural Insights into Inhibition Mechanism

  • Dorota Kubacka,
  • Mateusz Kozarski,
  • Marek R. Baranowski,
  • Radoslaw Wojcik and ,
  • Joanna Panecka-Hofman,
  • Dominika Strzelecka,
  • Jerome Basquin,
  • Jacek Jemielity and
  • Joanna Kowalska
  • + 4 authors+ 0 author

29 April 2022

Cytosolic nucleotidases (cNs) catalyze dephosphorylation of nucleoside 5’-monophosphates and thereby contribute to the regulation of nucleotide levels in cells. cNs have also been shown to dephosphorylate several therapeutically relevant nucleo...

(This article belongs to the Special Issue Design of Enzyme Inhibitors as Potential Drugs 2022)
  • Article
  • Open Access
12 Citations
3,525 Views
10 Pages

Anti-Inflammatory Effects of (3S)-Vestitol on Peritoneal Macrophages

  • Bruno Bueno-Silva,
  • Manuela Rocha Bueno,
  • Dione Kawamoto,
  • Renato C. Casarin and ,
  • João Marcos Spessoto Pingueiro,
  • Severino Matias Alencar,
  • Pedro Luiz Rosalen and
  • Marcia Pinto Alves Mayer
  • + 3 authors+ 0 author

29 April 2022

The isoflavone (3S)-vestitol, obtained from red propolis, has exhibited anti-inflammatory, antimicrobial, and anti-caries activity; however, few manuscripts deal with its anti-inflammatory mechanisms in macrophages. The objective is to elucidate the...

(This article belongs to the Section Natural Products)
  • Review
  • Open Access
29 Citations
8,309 Views
12 Pages

Brain Glucose Hypometabolism and Iron Accumulation in Different Brain Regions in Alzheimer’s and Parkinson’s Diseases

  • Indira Y. Rao,
  • Leah R. Hanson,
  • Julia C. Johnson,
  • Michael H. Rosenbloom and
  • William H. Frey

29 April 2022

The aim of this study was to examine the relationship between the presence of glucose hypometabolism (GHM) and brain iron accumulation (BIA), two potential pathological mechanisms in neurodegenerative disease, in different regions of the brain in peo...

(This article belongs to the Special Issue New Drugs and Biologics For Treatment of Central Nervous Dysfunction)
  • Article
  • Open Access
23 Citations
3,867 Views
17 Pages

Galactosylated Prodrugs: A Strategy to Improve the Profile of Nonsteroidal Anti-Inflammatory Drugs

  • Federica Sodano,
  • Claudia Cristiano,
  • Barbara Rolando,
  • Elisabetta Marini and ,
  • Loretta Lazzarato,
  • Mariarosaria Cuozzo,
  • Stefania Albrizio,
  • Roberto Russo and
  • Maria Grazia Rimoli
  • + 4 authors+ 0 author

29 April 2022

Carbohydrates are one of the most abundant and important classes of biomolecules. The variety in their structures makes them valuable carriers that can improve the pharmaceutical phase, pharmacokinetics and pharmacodynamics of well-known drugs. D-gal...

(This article belongs to the Special Issue Carbohydrate-Based Drugs)
  • Review
  • Open Access
18 Citations
5,892 Views
21 Pages

Refining Glioblastoma Surgery through the Use of Intra-Operative Fluorescence Imaging Agents

  • Oluwakanyinsolami Netufo,
  • Kate Connor,
  • Liam P. Shiels,
  • Kieron J. Sweeney and ,
  • Dan Wu,
  • Donal F. O’Shea,
  • Annette T. Byrne and
  • Ian S. Miller
  • + 3 authors+ 0 author

29 April 2022

Glioblastoma (GBM) is the most aggressive adult brain tumour with a dismal 2-year survival rate of 26–33%. Maximal safe resection plays a crucial role in improving patient progression-free survival (PFS). Neurosurgeons have the significant chal...

(This article belongs to the Special Issue In Vivo Nuclear Molecular Imaging in Drug Development and Pharmacological Research)
  • Article
  • Open Access
24 Citations
3,787 Views
26 Pages

Mechanistic Insights on the In Vitro Antibacterial Activity and In Vivo Hepatoprotective Effects of Salvinia auriculata Aubl against Methotrexate-Induced Liver Injury

  • Nashwah G. M. Attallah,
  • Fatma Alzahraa Mokhtar,
  • Engy Elekhnawy,
  • Selim Z. Heneidy and ,
  • Eman Ahmed,
  • Sameh Magdeldin,
  • Walaa A. Negm and
  • Aya H. El-Kadem
  • + 3 authors+ 0 author

29 April 2022

Methotrexate (MTX) is widely used in the treatment of numerous malignancies; however, its use is associated with marked hepatotoxicity. Herein, we assessed the possible hepatoprotective effects of Salvinia auriculata methanol extract (SAME) against M...

(This article belongs to the Special Issue Botanicals: Bioactive Molecules and Therapeutic Properties for Human Health 2021)
  • Review
  • Open Access
50 Citations
16,896 Views
26 Pages

Therapeutic Targets in Allergic Conjunctivitis

  • Bisant A. Labib and
  • DeGaulle I. Chigbu

28 April 2022

Allergic conjunctivitis (AC) is a common condition resulting from exposure to allergens such as pollen, animal dander, or mold. It is typically mediated by allergen-induced crosslinking of immunoglobulin E attached to receptors on primed conjunctival...

(This article belongs to the Special Issue Advances in Ocular Pharmacology)
  • Article
  • Open Access
13 Citations
4,276 Views
17 Pages

Chromene Derivatives as Selective TERRA G-Quadruplex RNA Binders with Antiproliferative Properties

  • Roberta Rocca,
  • Francesca Scionti,
  • Matteo Nadai,
  • Federica Moraca and ,
  • Annalisa Maruca,
  • Giosuè Costa,
  • Raffaella Catalano,
  • Giada Juli,
  • Maria Teresa Di Martino and
  • Anna Artese
  • + 10 authors+ 5 authors

28 April 2022

In mammalian cells, telomerase transcribes telomeres in large G-rich non-coding RNA, known as telomeric repeat-containing RNA (TERRA), which folds into noncanonical nucleic acid secondary structures called G-quadruplexes (G4s). Since TERRA G4 has bee...

(This article belongs to the Special Issue In Silico Approaches in Drug Design)

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Pharmaceuticals - ISSN 1424-8247