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Current Medicinal Chemistry

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https://www.readbyqxmd.com/read/28201970/highlights-in-endocytosis-of-nanostructured-systems
#1
Aline Raquel Voltan, Kaila Medina Alarcon, Ana Marisa Fusco-Almeida, Christiane Piena Soares, Maria José Soares Mendes-Giannini, Marlus Chorilli
The focus of this review is the cellular internalisation mechanism of nanostructured systems (NSs) and their endosomal escape for targeted drug delivery. Endocytosis is a cellular process of internalisation of different molecules and foreign microorganisms. It is currently being studied for drug delivery through nanostructured systems. The most commonly studied routes of cellular uptake are phagocytosis, macro-pinocytosis, clathrin-mediated endocytosis, caveolin-mediated endocytosis, and clathrin and caveolin-independent endocytosis...
February 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28201969/vitamin-d-and-cancer-stem-cells-in-the-gastrointestinal-tract
#2
Ming-Xing Li, Long-Fei Li, Lin Zhang, Zan-Gang Xiao, Jing Shen, Wei Hu, Qiang Zeng, Chi-Hin Cho
Vitamin D has been widely used as a dietary supplement for the prevention and treatment of bone disorders. Epidemiological and preclinical studies demonstrated the anticancer action of vitamin D in a variety of cancers including those in the gastrointestinal (GI) tract. In these studies the inhibitory action of vitamin D on cancer stem cells (CSCs) has been a focus and is also an important subject to revolutionize the therapeutic potential of vitamin D on cancer treatment. Here, we summarize the involvement of CSC markers and factors and also their signaling pathways in the development of cancers in the esophagus, stomach, colon, pancreas and also liver...
February 14, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28183261/lactate-dehydrogenase-inhibition-biochemical-relevance-and-therapeutical-potential
#3
Giuseppina Laganà, Davide Barreca, Antonella Calderaro, Ersilia Bellocco
Lactate dehydrogenase (LHD) is a key enzyme of anaerobic metabolism in almost all living organisms and it is also a functional checkpoint for glucose restoration during gluconeogenesis and single-stranded DNA metabolism. This enzyme has a well preserved structure during evolution and among the species, with little, but sometimes very useful, changes in the amino acid sequence, which makes it an attractive target for the design and construction of functional molecules able to modulate its catalytic potential and expression...
February 8, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28183260/current-challenges-and-opportunities-for-chemoprevention-of-pancreatic-cancer
#4
Altaf Mohammed, Naveena B Janakiram, Venkateshwar Madka, Min Li, Adam S Asch, Chinthalapally V Rao
The incidence of pancreatic cancer (PC) is rising in parallel with the deaths caused by this malignant disease largely due to limited improvement in current treatment strategies. In spite of aggressive PC research, for the past three decades, there has been no significant improvement in the five-year survival for this cancer. Like many other cancers, it takes several years for normal pancreatic cells to transform into pancreatic precursor lesions and to further progress into invasive carcinoma. Hence there is a scope for development of chemoprevention strategies to inhibit/delay/prevent progression of this disease into an advanced stage cancer...
February 8, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28183259/targeting-melatonin-mt2-receptors-a-novel-pharmacological-avenue-for-inflammatory-and-neuropathic-pain
#5
Luca Posa, Danilo De Gregorio, Gabriella Gobbi, Stefano Comai
Melatonin (MLT) has been implicated in several pathophysiological states, including pain. MLT mostly activates two G-protein coupled receptors, MT1 and MT2. In this review, we present the analgesic properties of MLT in preclinical and clinical studies, giving particular emphasis to the effects mediated by MT2 receptors and to recent investigations demonstrating the analgesic effects of MT2 receptor partial agonists in chronic and acute/inflammatory pain conditions. MT2 receptors are localized in specific brain areas, including the reticular and the ventromedial nuclei of the thalamus (part of the ascending nociceptive pathway) and the ventrolateral periaqueductal grey matter (vlPAG) (part of the descending antinociceptive pathway)...
February 8, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28183258/progress-in-the-discovery-of-macrocyclic-histone-deacetylase-inhibitors-for-the-treatment-of-cancer
#6
Kai Cheng, Siyu Li, Chenzhong Liao
Histone deacetylases (HDACs) play key roles in many biological phenomena and HDAC inhibition has been proved to be an effective strategy in cancer therapy. Over the last few decades, a plethora of structurally diverse HDAC inhibitors have been reported for a broad range of tumor indications. Among them, macrocyclic HDAC inhibitors, including cyclic peptides, depsipeptides and peptidomimetics, etc., have drawn lots of interests because of the fact that macrocyclic HDAC inhibitors have the potential for member or isoform selective inhibition...
February 8, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28183257/molecular-players-in-tuberculosis-drug-development-another-break-in-the-cell-wall
#7
Flavia Squeglia, Maria Romano, Alessia Ruggiero, Rita Berisio
Tuberculosis is a leading killer, especially for people living with HIV. It is a real medical need to tackle this disease, which is made difficult to treat due to the increasing spread of multi-drug-resistant and extensively drug-resistant bacterial strains. Cases of tuberculosis that are resistant to virtually all drugs currently available are increasing at an alarming rate around the world. Here, we review the current knowledge in the field of drug development against tuberculosis with a focus on the mechanisms of action of drugs and the targeted bacterial cell processes involved...
February 8, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28176636/discovery-of-species-selective-and-resistance-breaking-anticholinesterase-insecticides-for-the-malaria-mosquito
#8
Paul R Carlier, Jeffrey R Bloomquist, Max Totrov, Jianyong Li
Great reductions in malaria mortality have been accomplished in the last 15 years, in part due to the widespread roll-out of insecticide-treated bednets across sub-Saharan Africa. To date, these nets only employ pyrethroids, insecticides that that target the voltage-gated sodium ion channel of the malaria vector, Anopheles gambiae. Due to the growing emergence of An. gambiae strains that are resistant to pyrethroids, there is an urgent need to develop new public health insecticides that engage a different target and possess extremely low mammalian toxicity...
February 6, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28176635/modes-of-action-resistance-and-toxicity-of-insecticides-targeting-nicotinic-acetylcholine-receptors
#9
Makoto Ihara, Steven D Buckingham, Kazuhiko Matsuda, David B Sattelle
Nicotinic acetylcholine receptors (nAChRs) are members of the cys-loop superfamily of ligand-gated ion channels (cys-loop LGICs) and mediate fast cholinergic synaptic transmission in the nervous system of insects. The completion of many insect genome projects has greatly enhanced our understanding of the individual subunits that make up nAChR gene families from an insect genetic model organism (Drosophila melanogaster), crop pests, disease vectors and beneficial (pollinator) species. In addition to considerable insect nAChR subunit diversity, individual subunits can be subject to alternative splicing and RNA editing and these post-transcriptional modifications can add significantly to the diversity of nAChR receptor subtypes...
February 6, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28176634/targeting-the-akt-pi3k-signaling-pathway-as-a-potential-therapeutic-strategy-for-the-treatment-of-pancreatic-cancer
#10
Safieh Ebrahimi, Mina Hosseini, Soodabeh Shahidsales, Mina Maftouh, Gordon A Ferns, Majid Ghayour-Mobarhan, Seyed Mahdi Hassanian, Amir Avan
The phosphoinositide 3 kinase AKT mammalian target of rapamycin (PI3K-AKT-mTOR) signaling pathway is an important signaling pathway in pancreatic cancer (PC). It is frequently activated in PC and is associated with worse outcome. Aberrant activation of this pathway is involved in cell metabolism and survival, cell cycle progression, regulation of apoptosis, protein synthesis, and genomic instability. Several agents have been developed to target Akt/PI3K pathways, including PI3K inhibitors, (e.g. LY294002, Wortmannin), PI3K/mTOR inhibitors (e...
February 6, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28164762/regulation-of-ion-channels-cellular-carriers-and-na-k-atpase-by-janus-kinase-3
#11
Mentor Sopjani, Shpëtim Thaçi, Berat Krasniqi, Miranda Selmonaj, Mark Rinnerthaler, Miribane Dërmaku-Sopjani
Janus kinase-3 (JAK3), a tyrosine kinase, is expressed in a variety of tissues, including the brain, and is involved in the signaling of cytokine receptors. JAK3 participates in numerous functions, among other the cell survival and proliferation, neuroprotection, apoptosis, as well as cellular response to hypoxia and ischemia-reperfusion. This kinase further contributes in the signaling of hematopoietic cell cytokine receptors, dendritic cells activation, maturation, and immune suppression as well as to cell volume regulation...
February 3, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28164761/mitogen-activated-protein-kinase-mapk-interacting-kinases-1-and-2-mnk1-and-mnk2-as-targets-for-cancer-therapy-recent-progress-in-the-development-of-mnk-inhibitors
#12
Agnieszka Dreas, Maciej Mikulski, Mariusz Milik, Charles-Henry Fabritius, Krzysztof Brzózka, Tomasz Rzymski
BACKGROUND: MNK1 and MNK2 are MAP kinase-interacting serine/threonine kinases, which are activated by RAS and MAPK signaling pathways and are involved in regulation of protein translation. Both kinases phosphorylate translation initiation factor eIF4E on a conserved serine 209. Overactivated eIF4E can act as an oncogene and contribute to the transformation both in vitro and in vivo and is highly expressed in diverse types of cancer. Interestingly, knockout mice that lack both Mnk1 and Mnk2 do not have any apparent phenotype...
February 3, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28164760/the-typical-metabolic-modifiers-conferring-improvement-in-cancer-resistance
#13
Wen Tan, Zhangfeng Zhong, Shengpeng Wang, Hui Liu, Hua Yu, Rui Tan, Xiaodong Hu, Tingrui Pan, Yitao Wang
BACKGROUND: Cancer metabolic reprogramming rekindles enthusiasm for the research of metabolic regulation in cancer drug resistance. A growing number of metabolic modifiers combined with cancer drugs obtain the expected efficacy in in vitro or in vivo studies, also in clinical trial studies, indicating a good potential of enhancing efficacy and reducing resistance. Hence, a comprehensive review on the attenuations of metabolic modifiers in cancer drug resistance is necessary for rational drug design and clinical cancer drug research...
February 3, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28155603/advances-in-chemistry-and-pharmacology-of-triterpenoid-synthetic-dimers
#14
Barbara Bednarczyk-Cwynar, Andrzej Günther
The publication focuses on advances in chemistry and pharmacology of synthetic triterpenoid dimers, obtained from natural compounds. Synthetic triterpenoid dimers were divided into specific subgroups basing on the structure of main triterpenoid monomeric skeleton. Synthetic triterpenoid derivatives of dimeric structure can be obtained through the covalent linkage of the C-3 hydroxyl or another group, via the C-2 atom or the C-17 carboxyl group (mainly anhydrides, amides or esters). Some triterpenes can undergo chemical transformations leading to the formation of cyclic dimers or other types of dimers...
February 2, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28155602/displacement-of-drugs-from-human-serum-albumin-from-molecular-interactions-to-clinical-significance
#15
Hrvoje Rimac, Željko Debeljak, Mirza Bojić, Larisa Miller
BACKGROUND: Human serum albumin (HSA) is the most abundant protein in human serum. It has numerous functions, one of which is transport of small hydrophobic molecules, including drugs, toxins, nutrients, hormones and metabolites. HSA has the ability to interact with a wide variety of structurally different compounds. This promiscuous, nonspecific affinity can lead to sudden changes in concentrations caused by displacement, when two or more compounds compete for binding to the same molecular site...
February 2, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28137215/targeting-cancer-stem-cells-for-chemoprevention-of-pancreatic-cancer
#16
Dharmalingam Subramaniam, Gaurav Kaushik, Prasad Dandawate, Shrikant Anant
Pancreatic ductal adenocarcinoma is one of the deadliest cancers worldwide and the fourth leading cause of cancer-related deaths in United States. Regardless of the advances in molecular pathogenesis and consequential efforts to suppress the disease, this cancer remains a major health problem in United States. By 2030, the projection is that pancreatic cancer will be climb up to be the second leading cause of cancer-related deaths in the United States. Pancreatic cancer is a rapidly invasive and highly metastatic cancer, and does not respond to standard therapies...
January 26, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28120712/dna-damage-inducing-compounds-unraveling-their-pleiotropic-effects-using-high-throughput-sequencing
#17
Sebastian Müller
Compounds causing DNA damage have been used widely in molecular biology and some are used as therapeutic agents in cancer therapy. In most cases, their cellular response is pleiotropic, making it challenging to develop these agents efficiently for potential therapeutic use. Furthermore, this means that such compounds can also affect healthy tissues, which is a major drawback for the use in therapy. Thus, dissecting and understanding not only their molecular mode of action, but also identifying all their cellular targets is critical...
January 24, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28120711/lipoprotein-a-management-lifestyle-and-hormones
#18
Antonio Garcia-Rios, Ana Leon-Acuña, Jose Lopez-Miranda, Pablo Perez-Martinez
Cardiovascular disease (CVD) continues to be the first cause of mortality developed countries. Moreover, far from diminishing, the cardiovascular risk factors leading towards the development of CVD are on the rise. Therefore, the preventive and therapeutic management which is currently in place is clearly not enough to stop this pandemic. In this context, a major resurgence in interest in lipoprotein (a) [Lp(a)] has occurred in light of its association with CVD. This series aims to review the basic and clinical aspects of Lp(a) biology...
January 24, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28120710/the-role-of-universal-stress-proteins-in-bacterial-infections
#19
Andrew O Connor, Siobhán McClean
Universal stress proteins are ubiquitously expressed in bacteria, archaea and plants and other eukaryotes. A general property of USPs is their role in adaptation of bacteria to oxidative stress, high temperature, low pH and/or hypoxia. There is increasing evidence that these proteins facilitate the adaption of bacterial pathogens to the human host environment, thereby facilitating colonisation and pathogenicity. USPs in Mycobacterium tuberculosis are well studied and may play a role in latency of tuberculosis...
January 24, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28120709/dna-damaging-anticancer-drugs-a-perspective-for-dna-repair-oriented-therapy
#20
Janusz Blasiak
DNA-damaging drugs in cancer present two main problems: therapeutic resistance and side effects and both can associate with DNA repair, which can be targeted in cancer therapy. Bleomycin (BLM) induces complex DNA damages, including strand breaks, base loss and 3'-phosphoglycolate (3'PG) residues repaired by several pathways, but 3'PGs must be processed to the 3'-OH ends, usually by tyrosyl-DNA phosphodiesterase 1 (Tdp1). Therefore, targeting Tdp1 can improve anticancer therapy with BLM. Mitomycin C (MMC) produces a variety of adducts with DNA, including inter-strand cross-links (ICLs) and Xeroderma pigmentosum (XP) proteins, including XPG, XPE and XPF can be crucial for the initial stage of ICL repair, so they can be targeted by inhibitors to increase toxicity of MMC in cancer cells...
January 24, 2017: Current Medicinal Chemistry
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