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Future Medicinal Chemistry

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https://www.readbyqxmd.com/read/28097893/probing-the-cholinergic-system-to-understand-neurodegenerative-diseases
#1
Pierre-Yves Renard, Ludovic Jean
No abstract text is available yet for this article.
January 18, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28097887/pseudokinases-update-on-their-functions-and-evaluation-as-new-drug-targets
#2
Dominic P Byrne, Daniel M Foulkes, Patrick A Eyers
The pseudokinase complement of the human kinase superfamily consists of approximately 60 signaling proteins, which lacks one or more of the amino acids typically required to correctly align ATP and metal ions, and phosphorylate protein substrates. Recent studies in the pseudokinase field have begun to expose the biological relevance of pseudokinases, which are now thought to perform a diverse range of physiological roles and are connected to a multitude of human diseases, including cancer. In this review, we discuss how and why members of the 'pseudokinome' represent important new targets for drug discovery, and describe how knowledge of protein structure and function provides informative clues to help guide the rational chemical design or repurposing of inhibitors to target pseudokinases...
January 18, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28097880/practical-applications-of-matched-series-analysis-sar-transfer-binding-mode-suggestion-and-data-point-validation
#3
Peter Hunt, Matthew Segall, Noel O'Boyle, Roger Sayle
AIM: The assumption in scaffold hopping is that changing the scaffold does not change the binding mode and the same structure-activity relationships (SARs) are seen for substituents decorating each scaffold. Results/methodology: We present the use of matched series analysis, an extension of matched molecular pair analysis, to automate the analysis of a project's data and detect the presence or absence of comparable SAR between chemical series. CONCLUSION: The presence of SAR transfer can confirm the perceived binding mode overlay of different chemotypes or suggest new arrangements between scaffolds that may have gone unnoticed...
January 18, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27874288/n-heterocyclic-carbene-complexes-of-silver-and-gold-as-novel-tools-against-breast-cancer-progression
#4
Carmela Saturnino, Ines Barone, Domenico Iacopetta, Annaluisa Mariconda, Maria Stefania Sinicropi, Camillo Rosano, Antonella Campana, Stefania Catalano, Pasquale Longo, Sebastiano Andò
AIM: Metal carbenic complexes have received considerable attention in both the catalysis and biological fields for their potential applications in cancer and antimicrobial therapies. RESULTS: A small series of new silver and gold N-heterocyclic carbene complexes has been designed and synthesized. Among the tested complexes, one compound was particularly active in inhibiting anchorage-dependent and -independent breast cancer proliferation, and inducing cell apoptosis via a mitochondria-related process...
November 22, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27874285/modern-tools-for-the-chemical-ligation-and-synthesis-of-modified-peptides-and-proteins
#5
Luca Gentilucci, Pierluigi Tosi, Adriano Bauer, Rossella De Marco
The ability to improve nature's capacity by introducing modification of biological interest in proteins and peptides (P&P) is one of the modern challenges in synthetic chemistry. Due to the unfavorable pharmacokinetic properties, many native P&P are of little use as therapeutic agents. Today, few methods for the preparation of modified proteins are available. Initially introduced to realize the ligation between two standard peptidic sequences, and hence to afford native proteins, the modern chemical methodologies, in other words native chemical ligation, expressed ligation, Staudinger ligation, auxiliary mediated ligation, aldehyde capture, etc...
November 22, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27874280/a-survey-of-the-mechanisms-of-action-of-anticancer-transition-metal-complexes
#6
Mickaël Marloye, Gilles Berger, Michel Gelbcke, François Dufrasne
Metal complexes have been the subject of numerous investigations in oncology but, despite the plethora of newly synthesized compounds, their precise mechanisms of action remain generally unknown or, for the best, incompletely determined. The continuous development of efficient and sensitive techniques in analytical chemistry and molecular biology gives scientists new tools to gather information on how metal complexes can be effective toward cancer. This review focuses on recent findings about the anticancer mechanism of action of metal complexes and how the ligands can be used to tune their pharmacological and physicochemical properties...
November 22, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27845593/target-identification-and-lead-discovery-by-functional-lipidomics
#7
Andreas Koeberle
No abstract text is available yet for this article.
November 15, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27845592/design-and-synthesis-of-a-new-series-of-highly-potent-raf-kinase-inhibiting-triarylpyrazole-derivatives-possessing-antiproliferative-activity-against-melanoma-cells
#8
Mohammad Ashrafuddin Khan, Mohammed I El-Gamal, Hamadeh Tarazi, Hong Seok Choi, Chang-Hyun Oh
BACKGROUND: Inhibition of V600E-B-RAF kinase represents a potential avenue for melanoma treatment. Herein, a series of 1,3,4-triarylpyrazoles possessing amide linker were designed, synthesized and evaluated for RAF kinase inhibition. RESULTS: Compounds 1d and 1f were more potent than sorafenib against A375 cell line, and their selectivity indexes toward A375 than HS27 fibroblasts were 25.43 and 45.83, respectively. Compound 1f was more potent against the melanoma cell lines with B-RAF V600E mutation than melanoma cells with NRAS mutation and normal skin epithelial cells...
November 15, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27845591/drug-target-interaction-kinetics-underutilized-in-drug-optimization
#9
Robert A Copeland
No abstract text is available yet for this article.
November 15, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27845575/hsp70-therapeutic-potential-in-acute-and-chronic-cardiac-disease-settings
#10
Bianca C Bernardo, Kate L Weeks, Natalie L Patterson, Julie R McMullen
Heat shock proteins are a family of proteins that are produced by cells in response to exposure to stressful conditions. The best studied heat shock protein is HSP70, which is known to act as a molecular chaperone to maintain cellular homeostasis and inhibit protein aggregation in response to stress. While early animal studies suggested that increasing HSP70 in the heart (using a transgenic, gene transfer or pharmacological approach) provided cardiac protection against acute cardiac stress, recent studies have found no benefit of increasing HSP70 in mouse models of chronic cardiac stress...
November 15, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27845570/anti-inflammatory-effect-of-novel-analogs-of-natural-enkephalinase-inhibitors-in-a-mouse-model-of-experimental-colitis
#11
Elżbieta Kamysz, Maciej Sałaga, Małgorzata Sobocińska, Artur Giełdoń, Jakub Fichna
AIM: The pharmacotherapy of inflammatory bowel disease is difficult and currently available treatments bring mostly poor and unsatisfactory results. RESULTS: The purpose of this work was the synthesis of opiorphin, sialorphin, spinorphin and a series of their analogs and the in vitro characterization of their effect on degradation of enkephalin by neutral endopeptidase and aminopeptidase N. Consequently, we investigated in vivo the anti-inflammatory effect of the most active inhibitors selected in the in vitro studies (Pal-KKQRFSR & Pal-KKQHNPR)...
November 15, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27845568/design-of-chalcogen-containing-norepinephrines-efficient-gpx-mimics-and-strong-cytotoxic-agents-against-hela-cells
#12
Azucena Marset, Paloma Begines, Óscar López, Inés Maya, Natalia García-Aranda, Simó Schwartz, Ibane Abasolo, José G Fernández-Bolaños
AIM: Numerous chronic diseases exhibit multifactorial etiologies, so focusing on a single therapeutic target is usually an inadequate treatment; instead, multi-target drugs are preferred. Herein, a panel of phenolic thioureas and selenoureas were designed as new prototypes against multifactorial diseases concerning antioxidation and cytotoxicity, as a pro-oxidant environment is usually found in such diseases. RESULTS: Selenoureas were excellent antiradical agents and biomimetic catalysts of glutathione peroxidase for the scavenging of H2O2...
November 15, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27774814/recent-progress-in-repositioning-alzheimer-s-disease-drugs-based-on-a-multitarget-strategy
#13
M Amélia Santos, Karam Chand, Sílvia Chaves
Alzheimer's disease (AD) is a serious progressive neurological disorder, characterized by impaired cognition and profound irreversible memory loss. The multifactorial nature of AD and the absence of a cure so far have stimulated medicinal chemists worldwide to follow multitarget drug-design strategies based on repositioning approved drugs. This review describes a summary of recently published works focused on tailoring new derivatives of US FDA-approved acetylcholinesterase inhibitors, in addition to huperzine (a drug approved in China), either by hybridization with other pharmacophore elements (to hit more AD targets), or by combination of two FDA-approved drugs...
October 24, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27774798/opening-the-door-to-the-development-of-novel-abl-kinase-inhibitors
#14
Pedro Alves Bezerra Morais, Renata Dalmaschio Daltoé, Heberth de Paula
The discovery of the importance of kinase activity and its relationship to the emergence and proliferation of cancer cells, due to changes in normal physiology, opened a remarkable pathway for the treatment of chronic myelogenous leukemia through intense search of drug candidates. Six Abl kinase inhibitors have received the US FDA approval as chronic myelogenous leukemia treatment, and continuous efforts in obtaining new, more effective and selective molecules are being carried out. Herein we discuss the mechanisms of Abl inhibition, structural features and ligand/protein interactions that are important for the design of new Abl kinase inhibitors...
October 24, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27774795/recent-progress-of-cyclin-dependent-kinase-inhibitors-as-potential-anticancer-agents
#15
Tinghan Li, Tianwei Weng, Minzan Zuo, Zhihui Wei, Ming Chen, Zhiyu Li
Deregulation of the cell cycle is a common feature in human cancer. The inhibition of cyclin-dependent kinases (CDKs), which play a crucial role in control of the cell cycle, has always been one of the most promising areas in cancer chemotherapy. This review first summarizes the biology of CDKs and then focuses on the recent advances in both broad-range and selective CDK inhibitors during the last 5 years. The design rationale, structural optimization and structure-activity relationships analysis of these small molecules have been discussed in detail and the key interactions with the amino-acid residues of the most important compounds are highlighted...
October 24, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27774793/liposomal-drug-delivery-systems-for-targeted-cancer-therapy-is-active-targeting-the-best-choice
#16
Shaghayegh Fathi, Adegboyega K Oyelere
Liposomes are biodegradable and biocompatible self-forming spherical lipid bilayer vesicles. They can encapsulate and deliver one or more hydrophobic and hydrophilic therapeutic agents with poor therapeutic indices to tumor sites. Properties such as lipid bilayer fluidity, charge, size and surface hydration can be modified to extend liposome circulation time in the bloodstream and enhance efficacy. The focus of this review is on ligand-conjugated liposomes and their potential application in tumor-targeted delivery...
October 24, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/28001449/corrigendum
#17
(no author information available yet)
No abstract text is available yet for this article.
January 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27995811/discovery-of-novel-dual-vegfr2-and-src-inhibitors-using-a-multistep-virtual-screening-approach
#18
Shangying Chen, Chu Qin, Jia En Sin, Xuan Yang, Lin Tao, Xian Zeng, Peng Zhang, Chun Mei Gao, Yu Yang Jiang, Cheng Zhang, Yu Zong Chen, Wai Keung Chui
AIM: Simultaneous inhibition of VEGFR2 and Src may enhance the efficacy of VEGFR2-targeted cancer therapeutics. Hence, development of dual inhibitors on VEGFR2 and Src can be a useful strategy for such treatments. MATERIALS & METHODS: A multistep virtual screening protocol, comprising ligand-based support vector machines method, drug-likeness rules filter and structure-based molecular docking, was developed and employed to identify dual inhibitors of VEGFR2 and Src from a large commercial chemical library...
January 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27995810/a-comprehensive-look-of-poly-adp-ribose-polymerase-inhibition-strategies-and-future-directions-for-cancer-therapy
#19
Chandan Kumar, Nidhi Rani, Palanisamy Thanga Velan Lakshmi, Annamalai Arunachalam
The finding of promising drugs represents a huge challenge in cancer therapeutics, therefore it is important to seek out novel approaches and elucidate essential cellular processes in order to identify potential drug targets. Studies on DNA repair pathway suggested that an enzyme, PARP, which plays a significant role in DNA repair responses, could be targeted in cancer therapy. Hence, the efficacy of PARP inhibitors in cancer therapy has been investigated and has progressed from the laboratory to clinics, with olaparib having already been approved by the US FDA for ovarian cancer treatment...
January 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27995808/quercetin-and-derivatives-useful-tools-in-inflammation-and-pain-management
#20
Gabriele Carullo, Anna Rita Cappello, Luca Frattaruolo, Mariateresa Badolato, Biagio Armentano, Francesca Aiello
Inflammation represents a very frequent condition in humans; it is often underestimated, making the problem an increasingly alarming phenomenon. For these reasons, conventional therapies are losing their effectiveness, leaving room for innovative therapies. In this field, natural products showed their efficacy in various diseases; and flavonoids, in particular quercetin, is known for its broad range of activities. In this review, we have highlighted its efficacy in various models of inflammation, focusing also on the activity of its semisynthetic derivatives, and those naturally present in plant extracts...
January 2017: Future Medicinal Chemistry
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