Review
Pharmacology & Pharmacy
Mounir M. Salem-Bekhit, Abdullah M. E. Youssof, Fars K. Alanazi, Fadilah Sfouq Aleanizy, Alsuwyeh Abdulaziz, Ehab I. Taha, Amro Abd Al Fattah Amara
Summary: Bacterial ghosts, as empty cell envelopes of nonliving bacterial cells, have been tested as an advanced drug delivery system for various materials. They have diverse applications, including in vaccine and tumor therapy. The safety and stability aspects of using ghost bacteria as delivery systems are important considerations for further development.
Article
Chemistry, Multidisciplinary
Luca Ulfo, Andrea Cantelli, Annapaola Petrosino, Paolo Emidio Costantini, Michela Nigro, Francesco Starinieri, Eleonora Turrini, Suleman Khan Zadran, Giampaolo Zuccheri, Roberto Saporetti, Matteo Di Giosia, Alberto Danielli, Matteo Calvaresi
Summary: Using an orthogonal nanoarchitectonics approach, M13 bacteriophages were engineered to specifically target cancer cells with EGFR overexpression, and efficiently deliver photosensitizing molecules for photodynamic therapy at picomolar concentrations.
Review
Pharmacology & Pharmacy
Hanhee Cho, Seong Ik Jeon, Cheol-Hee Ahn, Man Kyu Shim, Kwangmeyung Kim
Summary: Albumin has the potential to improve the delivery of anticancer drugs by acting as a natural carrier. It can enhance the circulation time of the drugs and passively target tumors through enhanced permeability and retention. However, the delivery efficiency of exogenous albumin formulations is low, which increases the risk of systemic toxicity. Prodrugs that bind endogenous albumin have been investigated as a safer and more effective drug delivery option.
Article
Polymer Science
Kyungsene Lee, Taehyung Kim, Young Min Kim, Kyungjik Yang, Inseok Choi, Young Hoon Roh
Summary: Multifunctional DNA nanogels have been developed for potential cancer-targeted delivery and stimuli-responsive release of cancer therapeutics, exhibiting features such as temperature-induced disassembly, aptamer-mediated cancer cell targeting, and light-triggered temperature increase.
MACROMOLECULAR RAPID COMMUNICATIONS
(2021)
Article
Oncology
Rajeswari Raguraman, Dhaval Bhavsar, Dongin Kim, Xiaoyu Ren, Vassilios Sikavitsas, Anupama Munshi, Rajagopal Ramesh
Summary: Exosomes are small vesicles that can be used as drug delivery vehicles for cancer treatment due to their unique characteristics. Preclinical studies have shown that exosomes can effectively deliver chemotherapeutics, biologicals, and natural products with potent anticancer activity. However, challenges in large-scale production, storage, and stability have limited the number of exosome-based clinical trials.
Article
Chemistry, Multidisciplinary
Ying Huang, Lei Wang, Zhiyang Cheng, Biyu Yang, Jiahui Yu, Yi Chen, Wei Lu
Summary: The novel Mal-glu-SN38 prodrug showed selective delivery of SN38 to tumour sites and enhanced efficacy. With slower plasma clearance, increased drug exposure over time, and enhanced accumulation at the tumour site, Mal-glu-SN38 significantly delayed tumour growth after multiple doses, leading to an impressive reduction or even disappearance of tumours without observable side effects in 67% of mice.
JOURNAL OF CONTROLLED RELEASE
(2021)
Article
Chemistry, Multidisciplinary
Xiaoqing Li, Vamsidhara Vemireddy, Qi Cai, Hejian Xiong, Peiyuan Kang, Xiuying Li, Monica Giannotta, Heather N. Hayenga, Edward Pan, Shashank R. Sirsi, Celine Mateo, David Kleinfeld, Chris Greene, Matthew Campbell, Elisabetta Dejana, Robert Bachoo, Zhenpeng Qin
Summary: The study successfully synthesized gold nanoparticles for increasing blood-brain barrier permeability, demonstrating that transcranial picosecond laser stimulation can regulate BBB permeability, enabling drug delivery without disrupting the structure of the neurovascular unit.
Review
Pharmacology & Pharmacy
Richard B. Meagher, Zachary A. Lewis, Suresh Ambati, Xiaorong Lin
Summary: Combatting the increasing threat from invasive fungal pathogens faces challenges such as human exposure to species in the environment, immunocompromised individuals, unsatisfactory efficacy of current drugs, and barriers to new drug development. DectiSomes, a new drug delivery platform, enhance antifungal efficacy and reduce toxicity by targeting fungal ligands using pathogen receptor proteins. DectiSomes represent a leap forward for effective pan-antifungal therapy. The article discusses the problems of fungal diseases and the development of DectiSomes.
ADVANCED DRUG DELIVERY REVIEWS
(2023)
Article
Engineering, Biomedical
Sudipta Mallick, Ramadan Abouomar, David Rivas, Max Sokolich, Fatma Ceren Kirmizitas, Aditya Dutta, Sambeeta Das
Summary: Micro-sized magnetic particles, known as microrobots, have shown potential for biomedical applications such as drug delivery and cell manipulation. This study used microrobots to deliver anticancer drugs to cancer cells, resulting in cell death. The findings confirm the promise of microrobots as precise couriers for targeted delivery of therapeutic biomolecules for cancer therapy.
ADVANCED HEALTHCARE MATERIALS
(2023)
Article
Pharmacology & Pharmacy
Hanhee Cho, Man Kyu Shim, Suah Yang, Sukyung Song, Yujeong Moon, Jinseong Kim, Youngro Byun, Cheol-Hee Ahn, Kwangmeyung Kim
Summary: This study proposes a new approach for drug design in cancer therapy, utilizing a prodrug that can be activated by cathepsin B-overexpressed tumor cells. The prodrug selectively releases doxorubicin, a potent antitumor drug, in the tumor microenvironment, while minimizing toxicity to normal tissues. This promising strategy may have significant implications for effective and safe chemotherapy.
Review
Oncology
Jessica E. Holder, Christopher Ferguson, Elisabete Oliveira, Carlos Lodeiro, Carol M. Trim, Lee J. Byrne, Emilia Bertolo, Cornelia M. Wilson
Summary: Lung cancer is a global health problem, and non-small cell lung cancer is the most common form with conventional treatments often resulting in high rates of recurrence and adverse effects. Nanotechnology offers a potential solution by using nanoparticles to improve drug delivery and targeting to tumors, allowing for increased efficacy and reduced toxicity.
FRONTIERS IN ONCOLOGY
(2023)
Article
Chemistry, Multidisciplinary
Rossana Galassi, Lorenzo Luciani, Valentina Gambini, Silvia Vincenzetti, Giulio Lupidi, Augusto Amici, Cristina Marchini, Junbiao Wang, Stefania Pucciarelli
Summary: Phosphane gold(I) compounds were evaluated for screening on breast cancer cell panels, with compounds showing specific environments and components displaying activity. These compounds exhibited strong cytotoxicity, varying enzymatic activities, and binding properties in different cell lines.
FRONTIERS IN CHEMISTRY
(2021)
Review
Pharmacology & Pharmacy
Lu Tang, Jing Li, Qingqing Zhao, Ting Pan, Hui Zhong, Wei Wang
Summary: Nanotechnology plays a crucial role in cancer treatment, improving drug delivery efficiency and pharmacokinetics. Small molecule drugs and biological macromolecule drugs are the main types of anticancer agents, with nano-encapsulation technology playing a key role in their delivery.
Review
Chemistry, Multidisciplinary
Zhaomeng Wang, Jinbo Li, Guimei Lin, Zhonggui He, Yongjun Wang
Summary: Metal complex-based liposomes have attracted increasing interest in cancer diagnostics and therapeutics. They offer the potential to enhance therapeutic efficacy and reduce side effects. This review provides an overview of the latest advances in metal complex-based liposomal delivery systems, including encapsulation techniques, applications, and advantages.
JOURNAL OF CONTROLLED RELEASE
(2022)
Review
Polymer Science
Magdalena J. Bigaj-Jozefowska, Bartosz F. Grzeskowiak
Summary: Nanotechnology is a widely researched approach to improve cancer therapies, with polymeric nanocarriers playing a crucial role in delivering drugs and enhancing treatment outcomes. Biological membranes, such as those derived from red blood cells or cancer cells, have been extensively studied for their potential in improving biosafety and targeting properties. This review summarizes the development of biomimetic polymeric nanocarriers for efficient cancer treatment.
EUROPEAN POLYMER JOURNAL
(2022)
Article
Biochemistry & Molecular Biology
Marco Mellado, Cesar Gonzalez, Jaime Mella, Luis F. Aguilar, Ismail Celik, Fernanda Borges, Eugenio Uriarte, Giovanna Delogu, Dolores Vina, Maria J. Matos
Summary: Monoamine oxidases (MAOs) have been identified as attractive targets in drug design due to their role in modulating neurotransmitter levels and reactive oxygen species production. In this study, a comparative analysis was conducted to evaluate the inhibitory activity of two coumarin-based compounds (3-phenylcoumarin and trans-6-styrylcoumarin) on both MAO isoforms. Crystallographic structures, 3D-QSAR models, docking simulations, and molecular dynamics simulations were utilized to investigate the interaction mechanisms between these compounds and MAOs. Trans-6-styrylcoumarin exhibited significantly higher inhibitory activity on MAO-B compared to 3-phenylcoumarin and trans-resveratrol.
Editorial Material
Chemistry, Medicinal
Maria Joao Matos
Summary: Neurodegenerative diseases are a major cause of death, disability and dependency worldwide. Current therapeutic options only provide temporary relief of symptoms. Research on multitarget compounds for Alzheimer's and Parkinson's diseases offers potential therapeutic approaches.
FUTURE MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Josue Pozo-Martinez, Francisco Salgado, Ana Liempi, Ulrike Kemmerling, Raul Mera-Adasme, Claudio Olea-Azar, Mauricio Moncada-Basualto, Fernanda Borges, Eugenio Uriarte, Maria Joao Matos
Summary: The study demonstrated that a series of catechol-containing 3-arylcoumarins have moderate trypanocidal activity on the trypomastigote form of the parasite, with 3-(4'-bromophenyl)-6,7-dihydroxycoumarin (8) showing the highest activity but also the highest cytotoxicity in Vero cells. The inclusion in beta-cyclodextrins reduced the trypanocidal activity and cytotoxicity, but increased solubility. Compound 8 was found to act through the generation of oxidative stress, and the combination with BZN showed a synergistic effect, reducing the necessary dose of BZN and proving to be a promising alternative strategy for treating the disease.
ARABIAN JOURNAL OF CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Giovanna L. Delogu, Antonella Fais, Francesca Pintus, Chinmayi Goyal, Maria J. Matos, Benedetta Era, Amit Kumar
Summary: In this study, a combination of computational and biochemical techniques was used to modify the structure of benzofuran derivatives and identify relevant structural features for butyrylcholinesterase inhibitory activity and selectivity. By introducing a methylene spacer and substituents, a novel selective BChE inhibitor was discovered. 5-bromo-2-(4-hydroxybenzyl)benzofuran 9B exhibited the strongest inhibitory activity. Computational studies confirmed the correlation between the theoretical and experimental binding affinity of the compounds to the BChE protein.
Review
Biochemistry & Molecular Biology
Maria J. Matos, Lourdes Santana, Eugenio Uriarte, Fernanda Borges
Summary: This article provides a review of the synthesis and biological applications of thiocoumarins and their derivatives. It emphasizes their potential as drug candidates and highlights the research progress in the past 5 years. The information presented is based on data collected from multiple electronic databases.
Editorial Material
Chemistry, Medicinal
Maria Joao Matos, Maria-Jesus Blanco
ACS MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Chemistry, Medicinal
Maria Joao Matos, Eugenio Uriarte, Nuria Seoane, Aitor Picos, Jose Gil-Longo, Manuel Campos-Toimil
Summary: The newly synthesized nitrate-coumarins have been found to possess vasorelaxant activity on rat aorta rings, making them potential alternatives for the development of vasodilator drugs.
Article
Toxicology
Ana Paula Martins Castanha, Laiza Moura Almeida-Terassi, Estela Guardado-Yordi, Maria Joao Matos, Edson Luis Maistro
Summary: This study explored the safety and genotoxicity of a newly synthesized coumarin derivative, and found that the compound exhibited no cytotoxicity and protected cells from DNA damage at tested concentrations.
JOURNAL OF APPLIED TOXICOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Francesca Pintus, Sonia Floris, Antonella Fais, Benedetta Era, Amit Kumar, Gianluca Gatto, Eugenio Uriarte, Maria Joao Matos
Summary: This study investigates the inhibitory activity of certain compounds on enzymes involved in skin aging, such as tyrosinase, elastase, collagenase, and hyaluronidase. Several compounds were found to inhibit these enzymes, with five compounds acting as dual inhibitors. Compounds 1 and 2 showed the most promising anti-aging activity and also demonstrated a photo-protective effect.
Article
Chemistry, Medicinal
Maria J. Matos, Paula Novo, Lucia Mayan, Iria Torres, Eugenio Uriarte, Matilde Yanez, Jose Angel Fontenla, Francesco Ortuso, Stefano Alcaro, Francesca Procopio, Maria Isabel Rodriguez-Franco, Cristina Val, Maria I. Loza, Jose Brea, Fernanda Borges, Dolores Vina
Summary: Psychiatric and neurological disorders affect millions of people worldwide, and current treatments are limited in their effectiveness. New therapeutic solutions are urgently needed to improve the lives of patients.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
David Cabezas, Guido Mellado, Nicolas Espinoza, Jose Antonio Garate, Cesar Morales, Alejandro Castro-Alvarez, Maria J. Matos, Marco Mellado, Jaime Mella
Summary: Glycogen synthase kinase 3 (GSK-3) plays a role in various diseases and inhibiting GSK-3 could have pro-insulin effects. Aminopyrimidine derivatives have already proven to be promising GSK-3 inhibitors. In this study, CoMFA and CoMSIA models were developed to design new compounds with antidiabetic activity.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Review
Chemistry, Medicinal
Laura Fernandez-Pena, Maria Joao Matos, Enol Lopez
Summary: Coumarin and its derivatives are of great interest to medicinal chemists and chemical biologists due to their wide range of biological and pharmacological properties. Interesting families of coumarins have been discovered from marine sources, which have significantly accelerated the drug discovery process through inspiring innovation and identification of analogues with remarkable biological properties. This review aims to showcase the most interesting marine-derived coumarins from a medicinal chemistry perspective, as well as the novel and useful synthetic routes described to achieve these chemical structures. The references for this overview were collected from PubMed, Mendeley, and SciFinder.
Article
Chemistry, Medicinal
Aitor Carneiro, Lourdes Santana, Maria Joao Matos
Summary: The continuous symbiosis between chemical biology and drug discovery has led to the design of innovative bifunctional molecules for targeted and controlled drug delivery. Protein-drug and peptide-drug conjugates are popular approaches to achieve targeted delivery, selectivity, and efficacy. The selection of appropriate payloads and linkers is crucial for meeting the main goals of these bioconjugates, particularly in neurodegenerative diseases and certain cancer types where oxidative stress plays an important role. This mini-review covers the most relevant publications on oxidation-labile linkers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Chemistry, Medicinal
Antonella Fais, Francesca Pintus, Benedetta Era, Sonia Floris, Amit Kumar, Debapriyo Sarmadhikari, Valeria Sogos, Eugenio Uriarte, Shailendra Asthana, Maria Joao Matos
Summary: The coumarin scaffold shows promise in the development of bioactive agents, and this study focuses on the synthesis and evaluation of hydroxylated 3-arylcoumarins for their XO inhibition and antioxidant properties. Compound 11 is found to be the most potent XO inhibitor, and both compounds 11 and 5 show mixed-type inhibition and good antioxidant activity. Molecular docking studies correlate the theoretical and experimental binding affinity to the XO binding pocket.
Review
Chemistry, Medicinal
Aitor Carneiro, Eugenio Uriarte, Fernanda Borges, Maria Joao Matos
Summary: Propargylamine is widely used in medicinal chemistry and chemical biology due to its unique reactivity. This review discusses the applications and potential of propargylamine-based compounds in drug discovery, highlighting their impact in various therapeutic fields.
FUTURE MEDICINAL CHEMISTRY
(2023)
