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- Volume 29, Issue 8, 2022
Current Medicinal Chemistry - Volume 29, Issue 8, 2022
Volume 29, Issue 8, 2022
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Biogenic Gas Vesicles for Ultrasound Imaging and Targeted Therapeutics
Authors: Rui Wang, Lufang Wang, Yihan Chen, Yuji Xie, Mengrong He, Ye Zhu, Lingling Xu, Zhengyang Han, Dandan Chen, Qiaofeng Jin, Li Zhang and Mingxing XieUltrasound is not only the most widely used medical imaging mode for diagnostics owing to its real-time, non-radiation, portable and low-cost merits, but also a promising targeted drug/gene delivery technique by producing a series of powerful bioeffects. The development of micron-sized or nanometer-sized ultrasound agents or delivery carriers further makes ultrasound a distinctive modality in accurate diagnosis and effective treatment. In this review, we introduce one kind of unique biogenic gas-filled protein nanostructures called gas vesicles, which present some unique characteristics beyond the conventional microbubbles. Gas vesicles can not only serve as ultrasound contrast agent with innovative imaging methods such as cross-amplitude modulation harmonic imaging, but also can further be adjusted and optimized via genetic engineered techniques. Moreover, they could not only serve as acoustic gene reporters, acoustic biosensors to monitor the cell metabolism, but also serve as cavitation nuclei and drug carrier for therapeutic purpose. We focus on the latest development and applications in the area of ultrasound imaging and targeted therapeutics, and also give a brief introduction to the corresponding mechanisms. In summary, these biogenic gas vesicles show some advantages over conventional MBs that deserve making more efforts to promote their development.
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Liposomes-based Nanoplatform Enlarges Ultrasound-related Diagnostic and Therapeutic Precision
Authors: Ying Zhang and Brian FowlkesUltrasound (US) is recognized in the medical field as a safe and effective imaging modality due to its lack of ionizing radiation, non-invasive approach, and real-time monitoring capability. Accompanying recent progress in nanomedicine, US has been providing hope of theranostic capability not only for imaging-based diagnosis but also for US-based therapy by taking advantage of the bioeffects induced by US. Cavitation, sonoporation, thermal effects, and other cascade effects stimulated by acoustic energy conversion have contributed to medical problem-solving in the past decades, although to varying degrees of efficacy in comparison to other methods. Recently, the usage of liposomesbased nanoplatform fuels the development of nanomedicine and provides novel clinical strategies for antitumor, thrombolysis, and controlled drug release. The merging of novel liposome-based nanoplatforms and US-induced reactions has promise for a new blueprint for future medicine. In the present review article, the value of liposome-based nanoplatforms in US-related diagnosis and therapy will be discussed and summarized along with potential future directions for further investigations.
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Ultrasound-Based Drug Delivery System
Authors: Wei-Wei Ren, Shi-Hao Xu, Li-Ping Sun and Kun ZhangCancer still represents a leading threat to human health worldwide. The effective usage of anti-cancer drugs can reduce patients’ clinical symptoms and extend life-span survival time. Current anti-cancer strategies include chemotherapy, traditional Chinese medicine, biopharmaceuticals, and the latest targeted-therapy. However, due to the complexity and heterogeneity of tumor, serious side effects may result from the direct use of anti-cancer drugs. Besides, the current therapeutic strategies failed to effectively alleviate metastasized tumors. Recently, ultrasound-mediated nano-drug delivery system has become an increasingly important treatment strategy. Due to its abilities to enhance the efficacy and reduce toxic and side effects, it has become a research hotspot in the field of biomedicine. In this review, we introduced the latest research progress of the ultrasound-responsive nano-drug delivery systems, and the possible mechanisms of ultrasound acting on the carrier to change the structure or conformation, as well as to realize the controlled release. In addition, the progress in ultrasound responsive nano-drug delivery systems will also be briefly summarized.
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Polymer-Based Materials and their Applications in Image-Guided Cancer Therapy
Authors: Yang Sun, Haitao Ran and Fan LiuBackground: Advances in nanotechnology have enabled the combination of disease diagnosis and therapy into a single nano package that has tremendous potential for the development of new theranostic strategies. The variety of polymer-based materials has grown exponentially over the past several decades. Such materials have great potential as carriers in disease detection imaging and image monitoring and in systems for the precise delivery of drugs to specific target sites. Objective: In the present article, we review recent key developments in the synthesis of polymer- based materials for various medical applications and their clinical trials. Conclusion: There is a growing range of multi-faceted, polymer-based materials with various functions. These functions include carriers for image contrast agents, drug delivery systems, and real-time image-guided systems for noninvasive or minimally invasive therapeutic procedures for cancer therapy.
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Phase-Changeable Nanoparticle-Mediated Energy Conversion Promotes Highly Efficient High-Intensity Focused Ultrasound Ablation
Authors: Zeng Zeng, Ji-Bin Liu and Cheng-Zhong PengThis review describes how phase-changeable nanoparticles enable highly-efficient high-intensity focused ultrasound ablation (HIFU). HIFU is effective in the clinical treatment of solid malignant tumors; however, it has intrinsic disadvantages for treating some deep lesions, such as damage to surrounding normal tissues. When phase-changeable nanoparticles are used in HIFU treatment, they could serve as good synergistic agents because they are transported in the blood and permeated and accumulated effectively in tissues. HIFU’s thermal effects can trigger nanoparticles to undergo a special phase transition, thus enhancing HIFU ablation efficiency. Nanoparticles can also carry anticancer agents and release them in the targeted area to achieve chemo-synergistic therapy response. Although the formation of nanoparticles is complicated and HIFU applications are still in an early stage, the potential for their use in synergy with HIFU treatment shows promising results.
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Triazolopyrimidine Nuclei: Privileged Scaffolds for Developing Antiviral Agents with a Proper Pharmacokinetic Profile
Viruses are a continuing threat to global health. The lack or limited therapeutic armamentarium against some viral infections and increasing drug resistance issues make the search for new antiviral agents urgent. In recent years, a growing literature highlighted the use of triazolopyrimidine (TZP) heterocycles in the development of antiviral agents, with numerous compounds that showed potent antiviral activities against different RNA and DNA viruses. TZP core represents a privileged scaffold for achieving biologically active molecules, thanks to: i) the synthetic feasibility that allows to variously functionalize TZPs in the different positions of the nucleus, ii) the ability of TZP core to establish multiple interactions with the molecular target, and iii) its favorable pharmacokinetic properties. In the present review, after mentioning selected examples of TZP-based compounds with varied biological activities, we will focus on those antivirals that appeared in the literature in the last 10 years. Approaches used for their identification, the hit-to-lead studies, and the emerged structure-activity relationship will be described. A mention of the synthetic methodologies to prepare TZP nuclei will also be given. In addition, their mechanism of action, the binding mode within the biological target, and pharmacokinetic properties will be analyzed, highlighting the strengths and weaknesses of compounds based on the TZP scaffold, which is increasingly used in medicinal chemistry.
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The Pivotal Role of Transient Receptor Potential Channels in Oral Physiology
Authors: Andreas Chalazias, Grigorios Plemmenos, Evangelos Evangeliou and Christina PiperiBackground: Transient Receptor Potential (TRP) Channels constitute a large family of non-selective permeable ion channels involved in the perception of environmental stimuli with a central and continuously expanding role in oral tissue homeostasis. Recent studies indicate the regulatory role of TRPs in pulp physiology, oral mucosa sensation, dental pain nociception and salivary gland secretion. This review provides an update on the diverse functions of TRP channels in the physiology of the oral cavity, with emphasis on their cellular location, the underlying molecular mechanisms and clinical significance. Methods: A structured search of bibliographic databases (PubMed and MEDLINE) was performed for peer-reviewed studies on the function of TRP channels on oral cavity physiology in the last ten years. A qualitative content analysis was performed of screened papers and a critical discussion on the main findings is provided. Results: TRPs expression has been detected in major cell types of the oral cavity, including odontoblasts, periodontal ligament, oral epithelial, salivary gland cells, and chondrocytes of temporomandibular joints, where they mediate signal perception and transduction of mechanical, thermal, and osmotic stimuli. They contribute to pulp physiology through dentin formation, mineralization, and periodontal ligament formation, along with alveolar bone remodeling in the dental pulp and periodontal ligament cells. TRPs are also involved in oral mucosa sensation, dental pain nociception, saliva secretion, swallowing reflex and temporomandibular joints' development. Conclusion: Various TRP channels regulate oral cavity homeostasis, playing an important role in the transduction of external stimuli to intracellular signals in a cell typespecific manner and presenting promising drug targets for the development of pharmacological strategies to manage oral diseases.
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Top 100 Most-Cited Publications on Breast Cancer and Machine Learning Research: A Bibliometric Analysis
Authors: Tengku M. Hanis, Md Asiful Islam and Kamarul Imran MusaBackground: Rapid advancement in computing technology and digital information leads to the possible use of machine learning on breast cancer. Objective: This study aimed to evaluate the research output of the top 100 publications and further identify a research theme of breast cancer and machine-learning studies. Methods: Databases of Scopus and Web of Science were used to extract the top 100 publications. These publications were filtered based on the total citation of each paper. Additionally, a bibliometric analysis was applied to the top 100 publications. Results: The top 100 publications were published between 1993 and 2019. The most productive author was Giger ML, and the top two institutions were the University of Chicago and the National University of Singapore. The most active countries were the USA, Germany, and China. Ten clusters were identified as both basic and specialised themes of breast cancer and machine learning. Conclusion: Various countries demonstrated comparable interest in breast cancer and machine-learning research. A few Asian countries, such as China, India and Singapore, were listed in the top 10 countries based on the total citation. Additionally, the use of deep learning and breast imaging data was trending in the past 10 years in the field of breast cancer and machine-learning research.
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Epigenetics of Triple-Negative Breast Cancer via Natural Compounds
Triple-negative breast cancer (TNBC) is a highly resistant, lethal, and metastatic sub-division of breast carcinoma, characterized by the deficiency of estrogen receptor (ER), progesterone receptor (PR), and human epidermal growth factor receptor 2 (HER2). In women, TNBC shows a higher aggressive behavior with poor patient prognosis and a higher recurrence rate during reproductive age. TNBC is defined by the presence of epithelial- to-mesenchymal-transition (EMT), which shows a significant role in cancer progression. At the epigenetic level, TNBC is characterized by epigenetic signatures, such as DNA methylation, histone remodeling, and a host of miRNA, MiR-193, LncRNA, HIF- 2α, eEF2K, LIN9/NEK2, IMP3, LISCH7/TGF-β1, GD3s, KLK12, mediated regulation. These modifications either are silenced or activate the necessary genes that are prevalent in TNBC. The review is based on epigenetic mediated mechanistic changes in TNBC. Furthermore, Thymoquinone (TQ), Regorafenib, Fangjihuangqi decoction, Saikosaponin A, and Huaier, etc., are potent antitumor natural compounds extensively reported in the literature. Further, the review emphasizes the role of these natural compounds in TNBC and their possible epigenetic targets, which can be utilized as a potential therapeutic strategy in the treatment of TNBC.
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Anti-Proliferative Potential of Fluorinated Curcumin Analogues: Experimental and Computational Analysis and Review of the Literature
Background: Curcuminoids, flavoring, and coloring agents in food have potent antioxidant, anti-tumor activity, and anti-inflammatory effects. However, they are rapidly metabolized to lesser active metabolites. Therefore, various studies have been conducted to synthesize new and stable curcumin analogues with enhanced therapeutic activity. Methods: Fluorinated curcumin compounds (2a-2f) were synthesized by Knoevenagel condensation between fluorobenzaldehydes (1a-1f) with curcumin. Fluorinated demethoxycurcumin (3a) was synthesized by condensation between demethoxycurcumin and 3,4-difluorobenzaldehyde (1f). The structures of these compounds were confirmed by FTIR, 1H-NMR, 13C-NMR, 19FNMR, and mass spectroscopy. Antiproliferative activities of these synthetic compounds were evaluated against breast cancer cells (4T1), melanoma cancer cells (B16F10), and normal cell lines (NIH 3T3) using MTT assay. The interaction of curcumin, 2f and 3a with several proteins (1HCL, 2ZOQ, 3D94, 5EW3, 4WA9, 1XKK, 6CCY) was investigated. The structural preservation of the epidermal growth factor receptor (EGFR) was investigated by molecular dynamics simulation. Results: The spectroscopic data obtained confirmed the proposed structure of fluorinated analogues. The results showed that compounds 2f and 3a inhibited cancer cells proliferation significantly more than other compounds. Compounds 2f and 3a showed the highest affinity and lowest binding energy with EGFR. The binding energies were -7.8, -10, and - 9.8 kcal/mol for curcumin, 2f and 3a with EGFR, respectively. The molecular docking results demonstrated that compounds 2f and 3a were firmly bound in a complex with EGFR via the formation of a hydrogen bond. Conclusion: In summary, we found that fluorinated demethoxycurcumin and fluorinated curcumin induces cancer cell death and binds to EGFR with high affinity.
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Volumes & issues
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Volume 32 (2025)
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Volume 31 (2024)
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Volume 30 (2023)
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Volume 29 (2022)
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Volume 28 (2021)
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Volume 27 (2020)
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Volume 26 (2019)
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Volume 25 (2018)
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Volume 24 (2017)
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Volume 23 (2016)
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Volume 22 (2015)
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Volume 21 (2014)
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Volume 20 (2013)
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Volume 19 (2012)
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Volume 18 (2011)
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Volume 17 (2010)
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Volume 16 (2009)
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Volume 15 (2008)
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Volume 14 (2007)
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Volume 13 (2006)
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Volume 12 (2005)
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Volume 11 (2004)
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Volume 10 (2003)
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Volume 9 (2002)
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Volume 8 (2001)
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Volume 7 (2000)