journal
MENU ▼
Read by QxMD icon Read
search

Current Topics in Medicinal Chemistry

journal
https://www.readbyqxmd.com/read/28137208/c-elegans-as-model-for-drug-discovery
#1
Maria Carretero, Gregory M Solis, Michael Petrascheck
Small molecule screens using C. elegans as a model are becoming increasingly popular as the number of high-throughput methodologies has steadily increased over the years. Here we focus on the biology that underlies this increased popularity and outline the reasons that make C. elegans an attractive model for drug discovery. We discuss successful C. elegans based drug discovery projects in the literature and future challenges ahead.
January 31, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137239/targeted-theranostics-against-solid-cancer-using-metal-bond-milk-protein-and-aptamers
#2
Suman Chaudhary, Rupinder Kaur Kanwar, Jagat Rakesh Kanwar
Targeted therapeutics is a new generation therapy that can increase the efficacy of chemotherapeutic drugs, by facilitating site-specific delivery with minimum off-target effects. Amongst the targeted therapy, nucleic-acid based aptamers are increasingly gaining interest due to their small size, long shelf-life and ease in synthesis. Further, lactoferrin, a milk protein belonging to the transferrin family is now an established multi-functional iron-binding protein. Its applicability as an immunomodulator, antimicrobial and an anti-cancer agent has made this protein highly valuable...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137238/a-practical-guide-to-molecular-docking-and-homology-modelling-for-medicinal-chemists
#3
Anna E Lohning, Stephan M Levonis, Billy Williams-Noonan, Stephanie S Schweiker
Elucidating details of the relationship between molecular structure and a particular biological end point is essential for successful rationally-based drug discovery. Molecular docking is a widely accepted tool for lead identification however navigating the intricacies of the software can be daunting. Our objective was therefore to provide a step-by-step guide for those interested in incorporating contemporary basic molecular docking and homology modelling into their design strategy. Three molecular docking programs, AutoDock4, SwissDock and Surflex-Dock, were compared in the context of a case study where a set of steroidal and non-steroidal ligands were docked into the human androgen receptor (hAR) using both rigid and flexible target atoms...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137237/model-systems-for-pulmonary-infectious-diseases-paradigms-of-anthrax-and-tuberculosis
#4
Gunjan Arora, Richa Misra, Andaleeb Sajid
Robert Koch utilized animal model systems to put forward his postulates while discovering the etiological agents of anthrax and tuberculosis, Bacillus anthracis and Mycobacterium tuberculosis, respectively. After more than 130 years, we have achieved limited success towards understanding these two pestilences, which have propagated as scourge against humans. B. anthracis and M. tuberculosis are diverse organisms, which share a common evolutionary path in tropics. They adapt unique strategies to overcome unfavorable conditions and surpass the host defense mechanisms...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137236/the-use-of-the-zebrafish-model-to-aid-in-drug-discovery-and-target-validation
#5
Prusothman Yoganantharjah, Yann Gibert
The zebrafish is fast becoming a leading and prominent model organism used by researchers for developmental biology, and research in modeling human diseases in zebrafish is being undertaken at a fast pace. Many therapeutic areas, including oncology and cardiovascular diseases to name a few all have zebrafish models based on known disease mechanisms that are translatable to modes of action in humans. Many novel assays have been and are continuing to be developed to study human disease in zebrafish. Prominent methods to identify novel drug targets within the organism include, chemical mutagenesis, insertional mutagenesis and high throughput small molecule screens...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137235/calcium-dependent-protein-kinases-cdpks-key-to-malaria-eradication
#6
Kavita Kadian, Yash Gupta, Prakasha Kempaiah, Nikesh Gupta, Arun Sharma, Manmeet Rawat
The family of calcium-dependent protein kinases (CDPKs) carries a kinase domain fused to a calmodulin-like domain. The presence of protein kinases devoid of clear mammalian eukaryotic protein kinase orthologues makes them potential targets for therapeutic development. Recent studies on CDPKs have inspired an important primary regulator of calcium (intracellular Ca2+ signaling), which is extensively reported to play a critical role in various stages of the apicomplexan life cycle such as microneme secretion of adhesions, cell invasion, gamete maturation, gliding motility and egress of Plasmodium Spp...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137234/mycobacterial-dna-replication-as-a-target-for-antituberculosis-drug-discovery
#7
Renata Płocińska, Małgorzata Korycka-Machała, Przemysław Płociński, Jarosław Dziadek
Mycobacterium tuberculosis (M. tuberculosis), the causative agent of tuberculosis, is a leading infectious disease organism, causing millions of deaths each year. This serious pathogen has been greatly spread worldwide and recent years have observed an increase in the number of multi-drug resistant and totally drug resistant M. tuberculosis strains (WHO report, 2014). The danger of tuberculosis becoming an incurable disease has emphasized the need for the discovery of a new generation of antimicrobial agents...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137233/antimalarials-molecular-drug-targets-and-mechanism-of-action
#8
Angela O Achieng, Manmeet Rawat, Bernhards Ogutu, Bernard Guyah, John Michael Ong Echa, Douglas J Perkins, Prakasha Kempaiah
Despite a reduction in the global burden of malaria, the disease remains responsible for 214 million cases and 438,000 deaths annually with 88% of the mortality occurring in sub-Saharan Africa. Malaria control largely depends on effective chemotherapy. However, the historic and current emergence and spread of multi-drug resistant parasite strains provides significant challenges to malaria control and consequently, reduction of malaria-associated morbidity and mortality. Combating parasite drug resistance requires pharmacological compounds that target both known and novel metabolic pathways that are crucial for parasite survival...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137232/synthesis-properties-and-mechanism-of-action-of-new-generation-of-polycyclic-glycopeptide-antibiotics
#9
Eugenia N Olsufyeva, Anna N Tevyashova
The increased resistance of glycopeptide based antibiotics has become a serious problem for the chemotherapy of infections triggered by resistant Gram-positive bacteria. This has motivated the urgent sincere efforts to develop potent glycopeptide-based antibiotics in both academy and industry research laboratories. Understanding of the mechanism of action of natural and modified glycopeptides is considered as the basis for the rational design of compounds with valuable properties to achieve the fundamental results...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137231/insp3-signaling-in-apicomplexan-parasites
#10
Celia R S Garcia, Eduardo Alves, Pedro H S Pereira, Paula J Bartlett, Andrew P Thomas, Katsuhiko Mikoshiba, Helmut Plattner, L David Sibley
Phosphoinositides (PIs) and their derivatives are essential cellular components that form the building blocks for cell membranes and regulate numerous cell functions. Specifically, the ability to generate myo-inositol 1,4,5-trisphosphate (InsP3) via phospholipase C (PLC) dependent hydrolysis of phosphatidylinositol 4,5-bisphosphate (PIP2) to InsP3 and diacylglycerol (DAG) initiates intracellular calcium signaling events representing a fundamental signaling mechanism dependent on PIs. InsP3 produced by PI turnover as a second messenger causes intracellular calcium release, especially from endoplasmic reticulum, by binding to the InsP3 receptor (InsP3R)...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137230/proteases-in-mosquito-borne-diseases-new-avenues-in-drug-development
#11
A Pant, R Pasupureddy, V Pande, S Seshadri, R Dixit, K C Pandey
Mosquito borne diseases continue to propagate and cause millions of deaths annually. They are caused either by protozoan parasites such as Plasmodium, Toxoplasma or by flaviviruses including Dengue and Zika. Among the proteome of such parasitic organisms, proteases play essential roles in events such as host invasion, hemoglobin hydrolysis, replication and immune evasion. Plasmepsin V (PMV), an endoplasmic reticulum resident aspartic protease of Plasmodium spp., is involved in the export of ~400 proteins containing the conserved Plasmodium Export Element motif (PEXEL)...
30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137229/challenges-with-mosquito-borne-viral-diseases-outbreak-of-the-monsters
#12
Renu Gautam, Sweta Mishra, Archana Milhotra, Ritika Nagpal, Mradul Mohan, Anchal Singhal, Pratibha Kumari
The viruses responsible for mosquito-borne diseases are on an exploring mode, expanding their horizon, adapting to the situation and comfortably making their presence felt globally, from South Africa to Asia, Europe and United States. The current global scenario and recent documentations indicate towards the real monsters, outbreak of Zika, dengue and chikungunya viruses. Zika, dengue and chikungunya viruses, all three are positive sense single-stranded RNA arbovirus and so their initial symptoms are almost 80% similar and all three are spread by mosquitos which bite during the day...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137228/an-overview-of-currently-available-antimalarials
#13
Nikolay Yu Gorobets, Yuriy V Sedash, Brajendra K Singh, Poonam, Brijesh Rathi
Background Despite the substantial progress over the time, malaria remains a major public health concern and causing hundreds of thousands of deaths. Resistance to the available antimalarial therapy increases threat to the global public health. Objective Overview of currently available antimalarials. Method Literary seaway. Results The summarized data about different types of antimalarial therapies and their efficiency and modes of action. Conclusion Despite the seemingly large number of the drugs currently available for malaria treatment, this arsenal is limited due to the narrow variation of their mechanism of action...
January 30, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28137240/ascidians-an-emerging-marine-model-for-drug-discovery-and-screening
#14
Rémi Dumollard, Ievgeniia Gazo, Isa D L Gomes, Lydia Besnardeau, Alex McDougall
Ascidians (tunicates; sea squirts) are marine animals which provide a source of diverse, bioactive natural products, and a model for toxicity screenings. Compounds isolated from ascidians comprise an approved anti-tumor drug and many others are potent drug leads. Furthermore, the use of invertebrate embryos for toxicological screening tests or analysis offers the possibility to image a large number of samples for high throughput screens. Ascidians are members of a sister clade to the vertebrates and make a vertebrate-like tadpole larva composed of less than 3000 cells in 18 hours...
January 29, 2017: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/28056746/innovative-approaches-for-controlling-clinically-relevant-biofilms-current-trends-and-future-prospects
#15
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
#16
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
#17
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
#18
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
#19
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
#20
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
journal
journal
39712
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"