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Current Topics in Medicinal Chemistry

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https://www.readbyqxmd.com/read/28056746/innovative-approaches-for-controlling-clinically-relevant-biofilms-current-trends-and-future-prospects
#1
Kristina Ivanova, Eva Ramon, Javier Hoyo, Tzanko Tzanov
Bacteria that colonize and form biofilms on living tissues and medical devices are a global healthcare concern. They cause life threatening infections and are associated with increased mortality and morbidity in the hospitals. Although antibiotics have been successfully applied for treatment of bacterial diseases, the adaptive and genetic changes of the microorganisms within the biofilms make them inherently resistant to all known antibacterial agents. Therefore, novel antimicrobial strategies that do not exert selective pressure on bacterial population and minimize the risk of resistance occurrence have been sought to prevent and treat biofilm related infections...
January 5, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056745/exploiting-quorum-sensing-inhibition-for-the-control-of-pseudomonas-aeruginosa-and-acinetobacter-baumannii-biofilms
#2
Israel Castillo-Juarez, Luis Esaú López-Jácome, Gloria Soberón-Chávez, María Tomás, Jintae Lee, Paulina Castañeda-Tamez, Iván Ángelo Hernández-Bárragan, Martha Yumiko Cruz-Muñiz, Toshinari Maeda, Thomas K Wood, Rodolfo García-Contreras
Pseudomonas aeruginosa and Acinetobacter baumannii are two of the main bacteria responsible for nosocomial infections; both organisms are resistant to several classes of antibiotics making their infections very difficult to treat. Moreover, they possess a remarkable ability to form biofilms, which further enhances their antimicrobial resistance. Both organisms coordinate their formation of biofilms and their expression of virulence factors through quorum sensing, a system that regulates gene expression at high cell densities and that plays a key role in the establishment of bacterial infections...
January 5, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056744/nucleotide-second-messenger-signaling-as-a-target-for-the-control-of-bacterial-biofilm-formation
#3
Alberto J Martín-Rodríguez, Ute Römling
Bacterial biofilm formation and associated phenotypes are the major cause of chronic infection in humans. The major regulator of biofilm formation in Gram-negative and Gram-positive bacteria are nucleotide-based second messenger signaling pathways. Nucleotide-based signaling is a ubiquitous signal transduction mechanism in all domains of life that relay changes in the extracellular or intracellular milieu to protein or RNA effectors, leading to adaptive physiological responses. To date, six bona fide nucleotide signaling pathways, (p)ppGpp, cAMP, cGMP, c-di-AMP, c-di-GMP and cGAMP, have been characterized with respect to basic pathway modules and phenotypic and physiological output...
January 5, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056743/antimicrobial-peptides-for-the-control-of-biofilm-formation
#4
Mercedes González Moreno, Lisa Lombardi, Mariagrazia Di Luca
Antimicrobial peptides (AMPs) are an abundant and varied group of molecules recognized as the most ancient components of the innate immune system. They are found in a wide group of organisms including bacteria, plants and animals as a defense mechanism against different kinds of infectious pathogens. Over the past two decades, a fast-growing number of AMPs have been identified/designed and their wide-spectrum antimicrobial activity has been deeply investigated. In recent years, there has been an increasing interest in the use of AMPs as alternative anti-biofilm molecules for the control of biofilm-related infections...
January 5, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056742/fungal-biofilm-a-real-obstacle-against-an-efficient-therapy-lessons-from-candida
#5
Thaís Pereira de Mello, Lívia de Souza Ramos, Lys Adriana Braga-Silva, Marta Helena Branquinha, André Luis Souza Dos Santos
The past decades have witnessed a dramatic increase in invasive fungal infections, especially caused by different species belonging to the Candida genus. Nowadays, even after many improvements in several medical procedures, Candida infections (candidiasis) still account for an unacceptable high rate of morbimortality in hospital settings. Corroborating this statement, fungal biofilms formed on both abiotic and living surfaces are responsible for an important medical and economic burden, since biofilm lifestyle confers numerous advantages to the pathogens, including high tolerance to environmental stresses such as antimicrobials and host immune responses...
January 5, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056740/novel-colchicine-derivatives-and-their-anti-cancer-activity
#6
Lorelei Johnson, Ing Swie Goping, Aja Rieger, Jonathan Y Mane, Torin Huzil, Asok Banerjee, Richard Luduena, Bashar Hassani, Philip Winter, Jack A Tuszynski
In this paper we provide an overview of the status of various colchicine derivatives in pre-clinical development with special focus on their anti-cancer activity. We discuss several groups of compounds that have been designed to differentially bind with specific affinities for tubulin β isotypes, especially in regard to βIII, which is commonly over-expressed in cancer. Computational prediction, protein-based and cell-based assays are summarized as well as some animal tests conducted on these compounds. It is concluded that an untapped potential exists for exploiting the colchicine scaffold as a pharmacophore with the possibility of increasing its affinity for tubulin isotypes over-expressed in cancer and decreasing it for normal cells thereby widening the therapeutic window...
January 4, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056739/from-natural-products-to-designer-drugs-development-and-molecular-mechanisms-of-action-of-novel-anti-microtubule-breast-cancer-therapeutics
#7
Tejashree Mahaddalkar, Manu Lopus
Microtubule-targeted drugs (MTDs) have been on the forefront of breast cancer chemotherapy. Classic MTDs, such as paclitaxel and their semisynthetic derivatives, have achieved considerable success in the clinical management of breast neoplasms. In order to improve the specificity and to reduce undesirable, dose-limiting toxicities of these drugs, a plethora of novel compounds are being synthesized and investigated in laboratories worldwide. Due to their crucial roles during cell division, and to the fact that the suppression of their innate 'dynamic instability' can arrest cell cycle progression, microtubules formed an attractive target for cancer chemotherapy...
4, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056738/microtubule-targeting-agents-as-cancer-chemotherapeutics-an-overview-of-molecular-hybrids-as-stabilising-and-destabilising-agents
#8
Anjana Devi Tangutur, Dinesh Kumar, Kommalapati Vamsi Krishna, Srinivas Kantevari, Anjana Devi Tangutur, Dinesh Kumar, Kommalapati Vamsi Krishna, Srinivas Kantevari
Microtubules form crucial dynamic structural cellular components of the cell and are composed of the alpha beta tubulin heterodimers. Microtubules are involved in a wide variety of functions in the cell such as attribution to cell shape, motility, intracellular trafficking and mitotic spindle formation. Owing to these reasons, tubulin and microtubules have gained significant interest as important targets for cancer therapy. A review of the existing microtubule targeting drugs specifies that these agents can be categorised into two of the major categories: Microtubule stabilising agents such as paclitaxel, docetaxel, epothilones, and discodermolide which bind to the tubulin polymer and stabilize the microtubules, microtubule destabilising agents such as vinca alkaloids, colchicine and combretastatins which bind to tubulin dimers and cause destabilisation...
January 4, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056737/elucidation-of-the-tubulin-targeted-mechanism-of-action-of-9-3-pyridyl-noscapine
#9
Swagat Pradhan, Tejashree Mahaddalkar, Sinjan Choudhary, Naresh Manhcukonda, Praveen Reddy Nagireddy, Srinivas Kantevari, Manu Lopus
We have recently reported the synthesis and antiproliferative potential of a series of biaryl type α-noscapine congeners. Among them, 9-(3-pyridyl) noscapine 3f (9-PyNos, henceforth), which was synthesized by adding pyridine unit to the tetrahydroisoquinoline part of natural α-noscapine core, was found to be the most effective one to inhibit proliferation of a variety of cancer cell lines. However, details of its interactions with its cellular target, tubulin, remain poorly understood. In this report, we examined the nature of interactions of 9-PyNos with tubulin based on the methodologies of spectrofluorimetry, circular dichroism, and turbidimetry techniques...
4, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28049405/inhibition-of-bacterial-carbonic-anhydrases-as-a-novel-approach-to-escape-drug-resistance
#10
Clemente Capasso, Claudiu Supuran
BACKGROUND: Clinically used antibiotics act through one of these four mechanisms: cell wall biosynthesis inhibition, inhibition of protein biosynthesis, interference with DNA and RNA synthesis and the folate pathway. OBJECTIVE: The metalloenzymes carbonic anhydrases (CAs, EC 4.2.1.1) widespread in microorganisms and present as three genetically distinct families may be considered for the design of antiinfective agents with a different mechanism of action compared to the clinically used antibiotics...
January 3, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28049401/alzheimer-s-disease-and-natural-products-future-regimens-emerging-from-nature
#11
Md Asiful Islam, Shahad Saif Khandker, Fahmida Alam, Md Ibrahim Khalil, Mohammad Amjad Kamal, Siew Hua Gan
Alzheimer's disease (AD), which largely affects the elderly, has become a global burden. Patients with AD have both short- and long-term memory impairments. The neuronal loss in AD occurs due to abnormally folded amyloid beta proteins and aggregation of hyperphosphorylated tau proteins in the brain. Eventually, amyloid plaques and neurofibrillary tangles are formed, which subsequently disintegrate the neuronal transport system. There are several factors which are involved in AD pathogenesis, including oxidative stress, inflammation and the presence of metal ions...
January 3, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28049400/elucidating-treatment-of-alzheimer-s-disease-via-different-receptors
#12
Badar Ul Islam, Mohd Shahnawaz Khan, Nasimudeen R Jabir, Mohammad Amjad Kamal, Shams Tabrez
Alzheimer's disease (AD) is an irreversible multifaceted neurodegenerative disorder that gradually degrades neuronal cells. Presently, it is the most common reason for the memory loss and dementia in older individuals. It is patho-physiologically described by extracellular amyloid beta (Aβ) deposition, intracellular neurofibrillary tangles (NFTs) retention, neuronal decline, and neurotransmitter system derangement. Various receptors such as nicotinic acetylcholine, N-methyl-D-aspartate, insulin, serotonin, adenosine, and histamine are actively involved in the physiological progression of AD...
January 3, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28049399/gliomas-new-perspectives-in-diagnosis-treatment-and-prognosis
#13
Kemel A Ghotme, George E Barreto, Valentina Echeverria, Janneth Gonzalez, Rosa H Bustos, Magdy Sanchez, Jerzy Leszek, Nagendra Sastry Yarla, Rosa Margarita Gómez, Ghulam Md Ashraf, Gjumrakch Aliev
Gliomas are central nervous system tumors originated from glial cells, whose incidence and mortality is expected to rise in coming years, especially in developing countries. Diagnosis and classification of gliomas have largely relied on tumor histopathologic features that provide limited information regarding response to therapy or prognosis. Current treatment of gliomas is surgery combined with chemotherapy and/or radiotherapy. However, many tumors show a high resistance to these interventions, and recurrences are frequent since conventional therapies do not take into account the unique molecular features of different subtypes of glioma...
January 3, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28049398/infectious-agents-and-neurodegenerative-diseases-exploring-the-links
#14
Mohammad Zubair Alam, Qamre Alam, Mohammad Amjad Kamal, Asif Ahmad Jiman-Fatani, Esam I Azhar, Mohammad Azhar Khan, Absarul Haque
Recent studies have shown that bacterial and viral infections are risk factors for various neurodegenerative diseases such as Amyotrophic lateral sclerosis (ALS), Multiple Sclerosis (MS), Alzheimer's disease (AD), and Lyme disease (LD). However, it is still controversial how the infections play a role in neurological diseases progression. Infections in central nervous system may lead multiple damages in infected and neighboring cells. The infection leads to the activation of inflammatory processes and host immune responses, which acts as defense mechanism and also causes damage to the host neuronal functions and viability...
January 3, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28049397/insulin-resistance-in-alzheimer-disease-p53-and-micrornas-as-important-players
#15
Kazimierz Gąsiorowski, Barbara Brokos, Jerzy Leszek, Ghulam Md Ashraf, Gjumrakch Aliev
Glucose homeostasis is crucial for neuronal survival, synaptic plasticity, and is indispensable for learning and memory. Reduced sensitivity of cells to insulin and impaired insulin signaling in brain neurons participate in the pathogenesis of Alzheimer disease (AD). The tumor suppressor protein p53 coordinates with multiple cellular pathways in response to DNA damage and cellular stresses. However, prolonged stress conditions unveil deleterious effects of p53-evoked insulin resistance in neurons; enhancement of transcription of pro-oxidant factors, accumulation of toxic metabolites (e...
January 3, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28049395/type-3-diabetes-mellitus-a-novel-implication-of-alzheimer-disease
#16
Jerzy Leszek, Elżbieta Trypka, Vadim V Tarasov, Ghulam Md Ashraf, Gjumrakch Aliev
The brain of patients with Alzheimer disease (AD) showed the evidence of reduced expression of insulin and neuronal insulin receptors, as compared with those of age-matched controls. This event gradually and certainly leads to a breakdown of the entire insulin-signaling pathway, which manifests insulin resistance. This in turn affects brain metabolism and cognitive functions, which are the best-documented abnormalities in AD. These observations led Dr. de la Monte and her colleagues to suggest that AD is actually a neuroendocrine disorder that resembles type 2 diabetes mellitus...
3, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28049396/oxidative-stress-and-antioxidant-potential-of-one-hundred-medicinal-plants
#17
Waseem Hassan, Hamsa Noreen, Shakila Rehman, Shehnaz Gul, Mohammad Amjad Kamal, Jean Paul Kamdem, Bakht Zaman, Joao B T da Rocha
Reactive species are produced in biological system because of redox reactions. The imbalance in pro-oxidant and antioxidant homeostasis leads to the production of toxic reactive oxygen and nitrogen species like hydrogen peroxide, organic peroxides, hydroxyl radicals, superoxide anion and nitric oxide. Inactivation of metabolic enzymes, oxidation of biomolecules and cellular damage are some of the prominent characteristics of reactive species. Similarly, oxidative stress has been associated with more than one hundred (100) pathologies such as atherosclerosis, diabetes, cardiovascular diseases, pancreatic and liver diseases, joint disorders, cardiac fibrosis, acute respiratory distress syndrome, neurological diseases (amyotrophic lateral sclerosis, Huntington's disorder, Parkinson's disease and Alzheimer's disease), ageing and cancer etc...
January 2, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28017154/advances-in-micelle-based-drug-delivery-cross-linked-systems
#18
İsmail Alper İşoğlu, Yıldız Özsoy, Sevil Dinçer İşoğlu
There are several barriers that drug molecules encounter in body beginning from kidney filtration and reticulo-endothelial system (RES) clearance to cellular trafficking. Multifunctional nanocarriers have a great potential for the delivery of drugs by enhancing therapeutic activity of existing methodologies. A variety of nanocarriers are constructed by different material types, which have unique physicochemical properties for drug delivery applications. Micelles formed by amphiphilic polymers are one of the most important drug/nanocarrier formulation products, in which the core part is suitable for encapsulation of hydrophobic agent whereas the outer shell can be utilized for targeting the drug to the disease area...
December 22, 2016: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28017153/template-synthesis-of-tubular-nanostructures-for-loading-biologically-active-molecules
#19
Ayşegül Karataş, Aslıhan Hilal Algan
The template synthesis is a low cost, simple and versatile nanofabrication method to produce cylindrical/tubular nanostructures with controllable dimensions such as length, diameter and aspect ratio. This method utilizes nanoporous membranes such as anodized aluminum oxide (AAO) or polycarbonate (PC) as templates which have nanosized specific, cylindrical and uniform inner pores to be coated with the desired material. Template synthesized nanotubular structures have been produced from variety of materials including ceramics, polymers and proteins for loading biologically active molecules...
December 22, 2016: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28017152/rdna-mediated-bioconjugates-fusion-proteins-and-their-intended-use-in-medicine
#20
Ayşe Göksu Kaya-Özsan, Ayşe Filiz Öner
Protein bioconjugates can be synthesized by using chemical reactions, enzymatic reactions or genetic engineering technologies. Naturally occurred protein fusion event is used on purpose in the development of better biopharmaceuticals by applying genetic engineering methodologies. This review will mainly focus on the types of fusion proteins produced with the use of recombinant DNA technology, by combining genes or parts of genes from the same or different organisms, in order to be used in pharmaceutical applications for several purposes...
December 22, 2016: Current Topics in Medicinal Chemistry
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