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    Daropeptide natural products
    Cyclophane-containing peptides comprise an important group of macrocyclic peptides with unique structural properties and pharmaceutical relevance. Darobactin A is a ribosomally synthesized and post-...
    Suze Ma ... Qi Zhang
    Published: April 19, 2024 Explor Drug Sci. DOI: 10.37349/eds.2024.00042
    Viewed:37
    Downloaded:4
    Open Access
    Review
    Stapled peptides: targeting protein-protein interactions in drug development
    Protein-protein interactions (PPIs) impersonate a significant role in many biological processes and are potential therapeutic targets in numerous human diseases. Stapled peptides, as the most promis...
    Qian Zhang ... Chunqiu Zhang
    Published: April 18, 2024 Explor Drug Sci. DOI: 10.37349/eds.2024.00041
    Viewed:47
    Downloaded:8
    Open Access
    Perspective
    Clinical studies with drugs and biologics aimed at slowing or reversing normal aging processes—emerging results and future perspectives
    Five families of investigational products are in clinical investigation to slow or reverse normal aging processes [longevity candidates, mesenchymal stem cells, senolytics drugs, sirtuin activators,...
    Ricardo P. Garay
    Published: April 10, 2024 Explor Drug Sci. DOI: 10.37349/eds.2024.00040
    Viewed:86
    Downloaded:5
    Open Access
    Review
    Glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide agonists for the treatment of obesity and diabetes mellitus
    Pharmaceutical interventions play a vital role in managing various conditions, including weight-related issues such as obesity. In this context, lifestyle changes are often challenging to maintain, ...
    Alexander C. Martins ... Fernando Albericio
    Published: April 03, 2024 Explor Drug Sci. DOI: 10.37349/eds.2024.00039
    Viewed:193
    Downloaded:13
    Open Access
    Review
    Influenza A virus hemagglutinin: from classical fusion inhibitors to proteolysis targeting chimera-based strategies in antiviral drug discovery
    The influenza virus glycoprotein hemagglutinin (HA) participates in critical steps of the attachment of viral particles to the host cell membrane receptor and membrane fusion. Due to its crucial inv...
    Francisco Javier Hermoso-Pinilla ... Francisco Javier Luque
    Published: February 29, 2024 Explor Drug Sci. DOI: 10.37349/eds.2024.00037
    Viewed:361
    Downloaded:22
    Open Access
    Mini Review
    Mini-review on the antimicrobial potential of actinobacteria associated with seagrasses
    The search for novel therapeutic agents to combat the crisis of antimicrobial resistance has spanned from terrestrial to unique, marine environments. Currently, most of the drugs available for usage...
    Galana Siro, Atanas Pipite
    Published: February 29, 2024 Explor Drug Sci. DOI: 10.37349/eds.2024.00038
    Viewed:327
    Downloaded:18
    Open Access
    Review
    Seaweed: a sustainable solution for greening drug manufacturing in the pursuit of sustainable healthcare
    The environmental impact of drug manufacturing raises concerns about sustainability in healthcare. To address this, exploring alternative approaches to drug production is crucial. This review focuse...
    Leonel Pereira, João Cotas
    Published: February 27, 2024 Explor Drug Sci. DOI: 10.37349/eds.2024.00036
    Viewed:1041
    Downloaded:31
    Open Access
    Review
    Revisiting 310-helices: biological relevance, mimetics and applications
    310-Helices represent the third most abundant secondary structure proteins. Although understandably overshadowed by α-helices for decades, the 310-helix structure is slowly regaining certain releva...
    Diego Núñez-Villanueva
    Published: February 01, 2024 Explor Drug Sci. DOI: 10.37349/eds.2024.00034
    Viewed:540
    Downloaded:26
    Open Access
    Review
    Effect of the size of nucleic acid delivery systems on their fate in cancer treatment
    Nucleic acid therapeutics are emerging as a promising class of medicines, offering unique therapeutic options for cancer at the gene level. However, the druggability of nucleic acid therapeutics is ...
    Mengyun Ye ... Dandan Zhu
    Published: February 01, 2024 Explor Drug Sci. DOI: 10.37349/eds.2024.00035
    Viewed:321
    Downloaded:15
    Open Access
    Case Report
    Histological diagnosis of primary biliary cholangitis in one patient without cholestasis alterations: a case report that escaped guidelines
    Primary biliary cholangitis (PBC) is an autoimmune cholangiopathy that affects mainly women and, if untreated, can evolve into biliary cirrhosis. Its prevalence varies worldwide, depending on race, ...
    Matteo Biagi ... Pietro Andreone
    Published: January 22, 2024 Explor Drug Sci. DOI: 10.37349/eds.2024.00033
    Viewed:276
    Downloaded:12
    Open Access
    Review
    Harnessing the power of seaweed: unveiling the potential of marine algae in drug discovery
    Seaweeds, also known as marine algae, have gained attention as a promising source of bioactive compounds with potential applications in drug discovery. This review explores the emerging field of sea...
    Leonel Pereira, Ana Valado
    Published: December 28, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00032
    Viewed:1379
    Downloaded:43
    Open Access
    Original Article
    Rational design of novel phenol ether derivatives as non-covalent proteasome inhibitors through 3D-QSAR, molecular docking and ADMET prediction
    Aim: The purpose of this paper is to use different structures and ligand-based drug design methods properly to provide theoretical guidance for the design of novel non-covalent proteasome inhibit...
    Miao Yuan ... Ping Cheng
    Published: December 27, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00029
    Viewed:399
    Downloaded:13
    Open Access
    Review
    Electrospun short fibers: a new platform for cancer nanomedicine applications
    With the continuous development of nanomaterials, nanofibers prepared by electrospinning have gradually occupied people’s vision because of their unique advantages, such as crisscross network and ...
    Yifan Huang ... Xiangyang Shi
    Published: December 27, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00030
    Viewed:407
    Downloaded:17
    Open Access
    Case Report
    Reactivation of latent hepatitis B infection during immunosuppressive therapy with guselkumab for plaque psoriasis: a case report
    Reactivation of hepatitis B virus (HBV; RHBV) is a significant concern during immunosuppressive therapy, as it can lead to severe hepatitis and liver failure. The article reports a case of RHBV duri...
    Elena Franchi ... Pietro Andreone
    Published: December 27, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00031
    Viewed:367
    Downloaded:10
    Open Access
    Original Article
    Hybrid azole-based conjugates as upcoming anticancer and antimicrobial agents
    Aim: This study discloses the synthesis and the antimicrobial and anticancer activities of four molecules of structural basis saccharin-thiadiazolyl (4), saccharin-pyridyl (6, 8), and tetrazole-t...
    Luís M. T. Frija ... Patrícia Rijo
    Published: November 23, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00028
    Viewed:566
    Downloaded:33
    Open Access
    Original Article
    Insights into the binding selectivity of harzianoic acids A and B to tetraspanin CD81
    Aim: Harzianoic acids A and B (Hz-A/B) are two rare cyclobutene-containing sesquiterpenes isolated from a marine strain of the sponge-associated fungus Trichoderma harzianum. They display anticancer and antiviral effects, reducing the entry of hepatitis C virus (HCV) into hepatocarcinoma cells. The large extracellular loop (LEL) of the tetraspanin protein CD81 represents a molecular target for both Hz-A and Hz-B. Methods: The interaction of Hz-A/B with CD81 has been modeled, using structures of the cholesterol-bound full-length protein and a truncated protein corresponding to the LEL portion. The models mimicked the closed and open conformations of the LEL. Results: The best ligand Hz-B can form stable complexes with the open LEL structure, whereas binding to the closed form is drastically reduced. Key H-bonds between the acid groups of Hz-B and the CD81-LEL domain stabilize the ligand-protein complex. A comparison of the interaction with the homologous tetraspanin CD9, which also presents a dynamic open/closed equilibrium, underlined the marked selectivity of Hz-A/B for CD81 over CD9. The cyclobutane-containing monoterpene grandisol, an insect pheromone, has been identified as a fragment that could be modulated to improve its modest interaction with CD81-LEL. Conclusions: The modeling docking analysis suggests that Hz-B is a robust CD81 binder, better interacting with the LEL portion of CD81 compared to CD9-LEL. The docking study paves the way to the design of small molecules targeting CD81. The study has implications for a better understanding of CD81 binding properties and the regulation of its activities....
    Gérard Vergoten, Christian Bailly
    Published: November 01, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00027
    Viewed:421
    Downloaded:19
    Open Access
    Original Article
    Creation and interpretation of machine learning models for aqueous solubility prediction
    Aim: Solubility prediction is an essential factor in rational drug design and many models have been developed with machine learning (ML) methods to enhance the predictive ability. However, most o...
    Minyi Su, Enric Herrero
    Published: October 30, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00026
    Viewed:749
    Downloaded:35
    Open Access
    Review
    Therapeutic proteins immunogenicity: a peptide point of view
    Protein therapeutics are extensively used in the treatment of autoimmune diseases, but a subset of patients appears to be refractory to these treatments, mainly due to the development of an immune r...
    Feliciana Real-Fernandez ... Paolo Rovero
    Published: October 26, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00025
    Viewed:991
    Downloaded:37
    Open Access
    Review
    Phytochemicals for mitigating the COVID-19 crisis: evidence from pre-clinical and clinical studies
    The outbreak of severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) infection in December 2019 quickly escalated to pandemic levels and had a severe impact on public health. There are 761 m...
    Atri Das ... Shantanabha Das
    Published: October 24, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00024
    Viewed:956
    Downloaded:47
    Open Access
    Original Article
    Late-stage diversification strategy for the synthesis of peptide acids and amides using hydrazides
    Aim: Modification of the C-terminus of a peptide to improve its properties, particularly after constructing the peptide chain, has great promise in the development of peptide therapeutics. This s...
    Shoko Tanaka ... Kohei Sato
    Published: October 09, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00023
    Viewed:818
    Downloaded:36
    Open Access
    Case Report
    Grade IV oral mucositis treatment with Brazilian green propolis mucoadherent gel
    Green propolis is collected by Apis mellifera from the flowers and buds of Baccharis dracunculifolia. It has several chemical compounds that confer anti-inflammatory, antimicrobial, healing, and ant...
    Diogo Alvarenga Silva ... Vagner Rodrigues Santos
    Published: October 9, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00022
    Viewed:1006
    Downloaded:22
    Open Access
    Original Article
    Electrochemical properties of hydroxyapatite immobilization material for potential cytosensor fabrication
    Aim: The biorecognition unit of an electrochemical biosensor requires molecules that are immobilised to serve as a bridge between the recognition unit and the transducing surface. Unique material...
    Dennis Adusei ... Elvis K. Tiburu
    Published: September 21, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00021
    Viewed:368
    Downloaded:21
    Open Access
    Commentary
    Could flavonoid aglycones prevent the absorption of flavonoid glycosides by inhibiting sodium-dependent glucose transporter-1 in the small intestine?
    Flavonoids present a large group of natural polyphenols with numerous important health benefits for preventing and treating a diverse variety of pathological conditions. However, the actual therapeu...
    Katrin Sak
    Published: August 30, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00019
    Viewed:406
    Downloaded:15
    Open Access
    Case Report
    Single or multiple treatments with lusutrombopag in subjects with thrombocytopenia and chronic liver disease needing an invasive procedure
    Thrombocytopenia is one of the most frequent implications of liver cirrhosis. This condition, when present in the severe form [platelet count (PLT) less than 50 × 109/L] correlates, with an increas...
    Davide Scalabrini ... Pietro Andreone
    Published: August 30, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00020
    Viewed:399
    Downloaded:17
    Open Access
    Original Article
    In silico study about β-amyloid’s role in Alzheimer’s disease and glaucoma and prediction of its interactions with glaucoma related proteins
    Aim: The significance of β-amyloid protein as a key player in neuro-degenerative disorders viz. Alzheimer’s disease (AD), Parkinson’s disease (PD) has been extensively researched and reporte...
    Nancy Maurya
    Published: August 29, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00018
    Viewed:574
    Downloaded:19
    Open Access
    Review
    The protective role of GLP-1 in neuro-ophthalmology
    Despite recent advancements in the field of neuro-ophthalmology, the rising rates of neurological and ophthalmological conditions, mismatches between supply and demand of clinicians, and an aging po...
    Sohum Sheth ... Brandon Lucke-Wold
    Published: August 28, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00015
    Viewed:1679
    Downloaded:58
    Open Access
    Review
    Iron depletion in “metabolic fatty liver syndromes”: a strong biological rationale with disappointing liver outcomes
    Nonalcoholic fatty liver disease (NAFLD), its more rapidly progressive steatohepatitic variant [nonalcoholic steatohepatitis, (NASH)], and the recently defined metabolic dysfunction-associated fatty...
    Amedeo Lonardo
    Published: August 28, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00016
    Viewed:438
    Downloaded:13
    Open Access
    Review
    Natural compounds from medicinal plants against COVID-19
    The severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), known to cause the coronavirus disease 2019 (COVID-19), was declared a pandemic in early 2020. During the past time, several infecti...
    Anton Kolodnitsky ... Vladimir Poroikov
    Published: August 28, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00017
    Viewed:842
    Downloaded:36
    Open Access
    Review
    Approved antibacterial drugs in the last 10 years: from the bench to the clinic
    Bacterial infections constitute one of the major cases of primary medical incidences worldwide. Historically, the fight against bacterial infections in humans has been an ongoing battle, due to the ...
    Miguel García-Castro ... Juan Manuel López-Romero
    Published: June 30, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00013
    Viewed:1121
    Downloaded:57
    Open Access
    Original Article
    A dextrorotatory residues-incorporated bioactive dodecapeptide against enterohemorrhagic Escherichia coli
    Aim: This study aims to report an engineered peptide zp39 with favorable bioactivity against enterohemorrhagic Escherichia coli (E. coli, EHEC). Its antibacterial mechanisms and application in a ...
    Ping Zeng ... Lanhua Yi
    Published: June 30, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00014
    Viewed:559
    Downloaded:25
    Open Access
    Original Article
    Identification of an inter-cysteine loop potentially involved in the activity of Opisthorchis viverrini-granulin-1
    Aim: Identification of small bioactive regions in proteins and peptides can be useful information in drug design studies. The current study has shown that an inter-cysteine loop of the N-terminal...
    Rozita Takjoo ... Norelle L. Daly
    Published: June 30, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00012
    Viewed:601
    Downloaded:13
    Open Access
    Review
    Nature-inspired and medicinally relevant short peptides
    Peptides constitute an important component of Nature’s pharmacy and they play a significant role in several signaling pathways acting as natural biological messengers. While nature has mastered th...
    Maria G. Ciulla ... Kamal Kumar
    Published: June 27, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00011
    Viewed:2114
    Downloaded:149
    Open Access
    Original Article
    Heterogeneous graph convolutional neural network for protein-ligand scoring
    Aim: Drug discovery is a long process, often taking decades of research endeavors. It is still an active area of research in both academic and industrial sectors with efforts on reducing time and...
    Kevin Crampon ... Luiz Angelo Steffenel
    Published: April 30, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00010
    Viewed:1076
    Downloaded:35
    Open Access
    Review
    Focused ultrasound for treatment of peripheral brain tumors
    Malignant brain tumors are the leading cause of cancer-related death in children and remain a significant cause of morbidity and mortality throughout all demographics. Central nervous system (CNS) t...
    Phillip Mitchell Johansen ... Brandon Lucke-Wold
    Published: April 28, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00009
    Viewed:1082
    Downloaded:34
    Open Access
    Review
    Nano theranostics involved in bladder cancer treatment
    Bladder cancer (BC) is a complex disease with multiple clinical manifestations and treatment challenges, and current standard-of-care therapies remain limited and unfavorable. Theranostics, the inte...
    Kunpeng Liu ... Qingsong Yu
    Published: April 28, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00008
    Viewed:939
    Downloaded:35
    Open Access
    Editorial
    Machine learning for drug science
    Walter F. de Azevedo Jr.
    Published: April 16, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00007
    Viewed:657
    Downloaded:26
    Open Access
    Original Article
    Levistolide A and periplogenin inhibit the growth of gastric cancer cells in vitro and in vivo
    Aim: In the present study, the natural products levistolide A (LA) and periplogenin (PPG) were studied for their growth inhibitory effects on the development of gastric cancer cells in vitro and, ...
    Jia Li Guo ... Ji Zhong Zhao
    Published: March 30, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00006
    Viewed:856
    Downloaded:25
    Open Access
    Systematic Review
    Utilizing the Ethereum blockchain for retrieving and archiving augmented reality surgical navigation data
    Aim: Conventional techniques to share and archive spinal imaging data raise issues with trust and security, with novel approaches being more greatly considered. Ethereum smart contracts present o...
    Sai Batchu ... Brandon Lucke-Wold
    Published: February 28, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00005
    Viewed:812
    Downloaded:26
    Open Access
    Original Article
    Surface functionalized mesoporous polydopamine nanocomposites for killing tumor cells through collaborative chemo/photothermal/chemodynamic treatment
    Aim: The development of a collaborative strategy with improved efficacy holds great promise in tumor treatment. This study aims to develop an effective collaborative strategy based on functionalized mesoporous polydopamine (MPDA) nanocomposites for killing tumor cells. Methods: MPDA nanoparticles were synthesized and functionalized with camptothecin (CPT) payload and manganese dioxide (MnO2) coating to construct MPDA-CPT-MnO2 nanocomposites. Results: When uptaken by tumor cells, the nanocomposites can degrade to produce O2, release CPT, and generate manganese (Mn2+) under the stimulation of hydrogen peroxide (H2O2) and acid. The released CPT and Mn2+ can act as chemotherapeutic drug and Fenton-like agent, respectively. Abundant reactive oxygen species (ROS) are generated in 4T1 tumor cells through an Mn2+-mediated Fenton-like reaction. After that, the generated Mn4+ can react with glutathione (GSH) through redox reaction to produce Mn2+ and deplete GSH, disrupting the reducing capacity and benefiting the production of ROS in tumor cells. Under laser irradiation, the nanocomposites can generate hyperthermia to promote the production of ROS. Conclusions: The developed MPDA-CPT-MnO2 nanocomposites can kill tumor cells through collaborative chemo/photothermal/chemodynamic therapy (CDT)....
    Yi Ouyang ... Hui Liu
    Published: February 27, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00003
    Viewed:1645
    Downloaded:108
    Open Access
    Review
    Essential functions, syntheses and detection of sialyl Lewis X on glycoproteins
    It is widely acknowledged that sialyl Lewis X (sLeX), the composition and linkage of which are N-acetylneuraminic acid (Neu5Ac) α2-3 galactose (Gal) β1-4 [fucose (Fuc) α1-3] N-acetylglucosamine, is usually attached to the cell surface. It presents as a terminal structure on either glycoproteins or glycolipids and has been demonstrated to be related to various biological processes, such as fertilization and selectin binding. Due to the vital role of sLeX, its synthesis as well as its determination approaches have attracted considerable attention from many researchers. In this review, the focus is sLeX on glycoproteins. The biological importance of sLeX in fertilization and development, immunity, cancers, and other aspects will be first introduced. Then the chemical and enzymatic synthesis of sLeX including the contributions from more than 15 international research groups will be described, followed by a brief view of the sLeX detection focusing on monosaccharides and linkages. This review is valuable for those readers who are interested in the chemistry and biology of sLeX....
    Qiushi Chen ... Xuechen Li
    Published: February 28, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00004
    Viewed:1534
    Downloaded:64
    Open Access
    Original Article
    Convenient estimation of oxytetracycline and polymyxin B by a novel high-performance liquid chromatography method: development and validation
    Aim: The aim of this research work was to develop a validated reversed-phase (RP)-high-performance liquid chromatography (HPLC) method for simultaneous estimation of oxytetracycline (OXY) and pol...
    Tanu Chaudhary ... Dilpreet Singh
    Published: February 24, 2023 Explor Drug Sci. DOI: 10.37349/eds.2023.00002
    Viewed:542
    Downloaded:21
    Open Access
    Editorial
    Drug discovery: a multifactorial ecosystem
    Fernando Albericio
    Published: January 01, 2023 Explor Drug Sci. DOI: 10.37349/eds.2022.00001
    Viewed:7015
    Downloaded:91