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Current Medicinal Chemistry

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https://www.readbyqxmd.com/read/29231134/plant-made-antibodies-properties-and-therapeutic-applications
#1
Tatianamsu Ru V Komarova, Ekaterina V Sheshukova, Yuri L Dorokhov
A cost-effective plant platform for therapeutic monoclonal antibody production is both flexible and scalable. In addition, plant-made antibodies (PMAbs) could be advantageous compared to those produced in animal cells due to the absence of a risk of contamination from nucleic acids or proteins of animal origin. In this review, the various platforms of PMAbs production are described, and the widely used transient expression system based on Agrobacterium-mediated delivery of genetic material into plant cells is discussed in detail...
December 11, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210643/adipokines-and-myokines-a-pivotal-role-in-metabolic-and-cardiovascular-disorders
#2
Hye Soo Chung, Kyung Mook Choi
Obesity induces an imbalance in the expression and secretion of several cytokines, which contributes to the development of metabolic and cardiovascular disorders. On the contrary, skeletal muscle is known to have a role in reversing the detrimental impact of obesity. It has been established that adipose tissue acts as an endocrine organ that secretes proinflammatory and anti-inflammatory adipokines. Similarly, skeletal muscle produces secretory molecules, called myokines, from contracting muscle fibers. Myokines were recently recognized as beneficial modulators of obesity, metabolic syndrome, and type 2 diabetes...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210642/antidiabetics-structural-diversity-of-molecules-with-a-common-aim
#3
Jelena B Popovic-Dordevic, Ivana I Jevtic, Tatjana P Stanojkovic
BACKGROUND: Diabetes mellitus type 2 (DMT2) is an endocrine disease of global proportions which is currently affecting 1 in 12 adults in the world, with still increasing prevalence. World Health Organization (WHO) declared this worldwide health problem, as an epidemic disease, to be the only non-infectious disease with such categorization. People with DMT2 are at increased risk of various complications and have shorter life expectancy. The main classes of oral antidiabetic drugs accessible today for DMT2 vary in their chemical composition, modes of action, safety profiles and tolerability...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210641/dynamic-localization-of-hepatocellular-transporters-role-in-biliary-excretion-and-impairment-in-cholestasis
#4
Marcelo Gabriel Roma, Ismael R Barosso, Gisel S Miszczuk, Fernando A Crocenzi, Enrique J Sanchez Pozzi
Bile flow generation is driven by the vectorial transfer of osmotically active compounds from sinusoidal blood into a confined space, the bile canaliculus. Hence, localization of hepatocellular transporters relevant to bile formation is crucial for bile secretion. Hepatocellular transporters are localized either in the plasma membrane or in recycling endosomes, from where they can be relocated to the plasma membrane on demand, or endocytosed when the demand decreases. The balance between endocytic internalization/exocytic targeting to/from this recycling compartment is therefore the main determinant of the hepatic capability to generate bile, and to dispose endo- and xenobiotics...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210640/fine-tuning-of-micrornas-in-type-2-diabetes-mellitus
#5
Juan A Rosado, Raquel Diez-Bello, Gines Maria Salido, Gines Maria Salido
Type 2 diabetes mellitus is a metabolic disease widely spread across industrialized countries. Sedentary lifestyle and unhealthy alimentary habits lead to obesity, boosting both glucose and fatty acid in the bloodstream and eventually, insulin resistance, pancreas inflammation and faulty insulin production or secretion, all of them very well-defined hallmarks of type 2 diabetes mellitus. miRNAs, are small sequences of non-coding RNA that may regulate several processes within the cells, fine-tuning protein expression, with an unexpected and subtle precision and in time-frames ranging from minutes to days...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210639/guanylate-cyclase-c-a-current-hot-target-from-physiology-to-pathology
#6
Jose Antonio Uranga, Marta Castro, Raquel Abalo
Guanylate cyclase C (GC-C) receptor is a transmembrane receptor, predominantly expressed in intestinal epithelial cells, that plays a main role in homeostasis and function of the digestive tract. The endogenous ligands for this receptor are the paracrine hormones uroguanylin and guanylin. The heat-stable enterotoxin, produced by enterotoxigenic bacteria, is also a natural ligand of this receptor. Upon ligand binding, GC-C receptors increase the second messenger cyclic guanosine monophosphate (cGMP) levels, regulating a variety of key cell-type specific processes such as chloride and bicarbonate secretion (which increases luminal fluid and intestinal motility), epithelial cell growth, regulation of intestinal barrier integrity and visceral sensitivity...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210638/medical-applications-of-collagen-and-collagen-based-materials
#7
Anatoly Borisovich Shekhter, Alexey Leonidovich Fayzullin, Marina Nikolaevna Vukolova, Tatyana Georgiyevna Rudenko, Varvara Dmitriyevna Osipycheva, Petr Francevich Litvitsky
Collagen and collagen-based materials have been successfully used in medicine for over 50 years. The number of scientific articles about the role of collagen in the construction of scaffolds for tissue engineering has risen precipitously in recent years. The review contains materials about historic and modern applications of collagen in medicine such as soluble collagen injections, solid constructs reconstructed from solution, and decellularized collagen matrices. The analysis of published data proves the efficacy of collagen material in the treatment of chronic wounds, burns, venous and diabetic ulcers, in plastic, reconstructive and general surgery, urology, proctology, gynecology, ophthalmology, otolaryngology, neurosurgery, dentistry, cardiovascular and bone and cartilage surgery, as well as in cosmetology...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210637/metallopharmaceuticals-in-therapy-a-new-horizon-for-scientific-research
#8
Agnieszka Chylewska, Małgorzata Biedulska, Przemyslaw Sumczynski, Mariusz Makowski
Coordination chemistry offers much scope for the design of novel and therapeutic agents, including metallopharmaceuticals. The widespread use of metal complexes as effective pharmaceuticals, e.g. cancer therapeutic, anti-inflammatory, antidiabetic drugs or antimicrobial and diagnostic agents, demonstrates that the cytotoxicity of metal ions can be finely controlled via the appropriate choice of ligands. The successful targeting of radioisotopes again depends on the ligand design and metal oxidation state. The complexes of platinum, ruthenium, cobalt, copper and other d-block metal ions have been used in medicine for a long time but only recent advances have been made in understanding the molecular basis of mechanism of their action...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210636/new-insights-into-adipokines-as-potential-biomarkers-for-type-2-diabetes-mellitus
#9
Marta Olivera-Santa Catalina, Pedro C Redondo, Carlos Cantonero-Chamorro, Maria P Granados, Jose Sanchez-Collado, Letizia Albarran, Jose Lopez
A large number of studies have been focused on investigating serum biomarkers associated with risk or diagnosis of type-2 diabetes mellitus. In the last decade, promising studies have shown that circulating levels of adipokines could be used as a relevant biomarker for diabetes mellitus progression as well as therapeutic future targets. Here we discuss the possible use of recent described adipokines, including apelin, omentin-1, resistin, FGF-21, neuregulin-4 and visfatin, as early biomarkers for diabetes. In addition, we also include recent findings of other well know adipokines such as leptin and adiponectin...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210635/potential-drug-targets-in-the-pentose-phosphate-pathway-of-trypanosomatids
#10
Ines Loureiro, Joana Faria, Nuno Santarem, Terry K Smith, Joana Tavares, Anabela Cordeiro-da-Silva
The trypanosomatids, Trypanosoma brucei, Trypanosoma cruzi and Leishmania spp, are causative agents of important human diseases such African sleeping sickness, Chagas' disease and Leishmaniasis, respectively. The high impact of these diseases on human health and economy worldwide, the unsatisfactory available chemotherapeutic options and the absence of human effective vaccines, strongly justifies the search for new drugs. The pentose phosphate pathway has been proposed to be a viable strategy to defeat several infectious diseases, including those from trypanosomatids, as it includes an oxidative branch, important in the maintenance of cell redox homeostasis, and a non-oxidative branch in which ribose 5-phosphate and erythrose 4-phosphate, precursors of nucleic acids and aromatic amino acids, are produced...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210634/preventive-and-therapeutic-potentials-of-anthocyanins-in-diabetes-and-associated-complications
#11
Swathi Putta, Nagendra Sastry Yarla, Eswar K Kumar, Dhananjaya Bhadrapura Lakkappa, Mohammad A Kamal, Luciana Scotti, Marcus T Scotti, Ghulam Md Ashraf, George E Barreto, B Sasi Bhusana Rao, D Sarala Kumari, Gorla V Reddy, Vadim V Tarasov, Sarat Babu Imandi, Gjumrakch Aliev
Diet is an essential factor affecting the development of and risk for diabetes mellitus. In search of preventative and therapeutic strategies, it is to be considering the potential role of certain foods and their bioactive compounds to prevent the pathogenesis associated with metabolic diseases. Human consumption of anthocyanins is among the highest of all flavonoids. Epidemiological studies have suggested that the consumption of anthocyanins lowers the risk of diabetes and diabetic complications. Anthocyanins are important natural bioactive pigments responsible for red to blue colour of fruits, leaves, seeds, stems and flowers, which are present in a variety of plant species particularly in berries and cherries...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210632/role-of-matrix-metalloproteinases-in-degenerative-kidney-disorders
#12
Shifa Narula, Chanderdeep Tandon, Simran Tandon
Matrix metalloproteinases (MMPs) are members of calcium dependent-zinc containing endopeptidases that play a pivotal role in extracellular matrix (ECM) remodeling. MMPs are also known to cleave non-matrix proteins, including cell surface receptors, TNF-α, angiotensin-II, growth factors, (especially transforming growth factor-β1, ΤGF-β1) plasminogen, endothelin and other bioactive molecules. The tissue inhibitors of metalloproteinases (TIMPs) inhibit the activity of MMPs and decrease ECM degradation. Various patho-physiological conditions have been linked with the imbalance of ECM synthesis and degradation...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210631/uterine-function-from-normal-to-polycystic-ovarian-syndrome-alterations
#13
Silvana Rocio Ferreira, Alicia Beatriz Motta
BACKGROUND: The endometrium is one of the most important female reproductive organs. Polycystic ovarian syndrome (PCOS) is a reproductive and endocrine pathology that affect women of reproductive age. PCOS negatively affects the endometrium, leading to implantation failure and proliferative aberrations. METHODS: We conducted a search at the http://www.ncbi.nlm.nhi.gov/pubmed/electronic database using the following key words: endometrial steroid receptors, endometrium, uterine function, endometrium and PCOS, implantation window, implantation and PCOS, implantation markers, inflammation, oxidative stress...
December 5, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210644/carboxylesterase-inhibitors-an-update
#14
Li-Wei Zou, Qiang Jin, Dan-Dan Wang, Qing-Kai Qian, Da-Cheng Hao, Guang-Bo Ge, Ling Yang
Mammalian carboxylesterases are key serine hydrolases that catalyze the hydrolysis of a wide variety of ester compounds into the corresponding carboxylic acids and alcohols. In human, two major carboxylesterases, CES1 and CES2, have been identified and well-studied over the past decade. CES1 inhibitors have potential applications in the treatment of hypertriglyceridaemia, obesity and type 2 diabetes, owing to that this enzyme plays prominent role in the metabolism of cholesteryl esters. CES2 plays crucial roles in the metabolic activation of many prodrugs including anticancer agents capecitabine and CPT-11...
December 4, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29210633/recent-evidence-on-the-role-of-dietary-pufas-in-cancer-development-and-prevention
#15
Massimo D'Archivio, Beatrice Scazzocchio, Rosaria Vari, Carmela Santangelo, Claudio Giovannini, Roberta Masella
During the last decades a great bulk of scientific information has been accumulated about the metabolic effects of polyunsaturated fatty acids (PUFAs) that can impact human health. In particular, a growing body of evidence from in vitro, animal, and clinical studies supporting the use of n-3 PUFAs in cancer prevention has been collected. Furthermore, a considerable effort has recently been done to evaluate the hypothesis that n-3 PUFAs might improve the efficiency of currently used anticancer drugs. The role of n-6 PUFAs, in contrast, needs to be better assessed...
December 4, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29205109/new-treatments-for-allergy-advances-in-peptide-immunotherapy
#16
David Calzada, Selene Baos, Lucia Cremades, Blanca Olombrada Cardaba
BACKGROUND: Nowadays, allergen-specific immunotherapy (AIT) is the only treatment able to modulate the course of allergic diseases. Although it has been applied for the last 100 years, treatment with whole allergen extracts is not without its drawbacks: AIT can cause local and systemic adverse events and may produce new IgE sensitization against other allergens present in the extract. Furthermore, the lengthy treatment duration (3-5 years), frequent administration, and high cost of treatment are other disadvantages...
November 30, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29189126/recent-advances-for-the-synthesis-of-selenium-containing-small-molecules-as-potent-antitumor-agents
#17
Qi Miao, Jinyi Xu, Aijun Lin, Xiaoming Wu, Liang Wu, Weijia Xie
Selenium-containing small molecules have attracted considerable attention of chemical and medicinal researchers owing to their various biological activities, such as antitumor effects, cardiovascular protection, antibacterial or antiviral effects, immunoregulation and nerve protection, among which the most promising area is antineoplasm. In the past several decades, different kinds of organoselenium compounds, such as selenides, seleno(iso)cyanates, substituted selenoureas, selenious esters and Se-containing heterocycles have been reported as candidates of anti-cancer agents...
November 29, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29189125/use-of-antibiotic-loaded-biomaterials-for-the-management-of-bone-prosthesis-infections-rationale-and-limits
#18
Matilde Tschon, Maria Sartori, Deyanira Contartese, Gianluca Giavaresi, Nicolo Nicoli Aldini, Milena Fini
BACKGROUND: Periprosthetic joint infection still represents a challenging issue for the orthopedic community. In the United States approximately a million joint arthroplasties are performed each year, with infection rates ranging from 1 to 2%: revisions has significant implications in health care costs and appropriate resources management. The use of locally applied antibiotics as a prophylaxis measure or as a component of the therapeutic approach in primary or revision surgery is finalized at eliminating any microorganism and strengthening the effectiveness of systemic therapy...
November 29, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29189124/overview-on-anticancer-drug-design-and-development
#19
Sureyya Olgen
Many impediments of current anti-cancer therapies have urged scientists to discover new agents. As a result of growing spectrums of new targets and strategies and recent biological and biotechnological progresses, many anti-cancer agents such as monoclonal antibodies, small molecule tyrosine kinase inhibitors and epigenetic drugs have been reached to clinical trials. Addition to the traditional targets (mitosis, DNA synthesis, repairing systems, tumor growth, apoptosis, tumor vasculature and cell signaling mechanisms), other targets such as proteasome, heat shock proteins (HSPs), and epigenetics (HDACs, HATs, DNMT, PAD4, AID, and Tet1) are used to design new anti-cancer agents...
November 29, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29189123/anti-aging-drugs-prospect-of-longer-life
#20
Blanka Klimova, Michal Novotny, Kamil Kuca
BACKGROUND: Aging is a natural part of human life. However, recent discoveries indicate that pharmacological approaches used for the improvement and possibly, for the delay of the aging process, might shed a new light on this topic. This might obviously contribute to the extension of the active life of older people and maintenance of their quality of life, which could consequently reduce both social and economic burden of each country, especially the developed ones. OBJECTIVE: The purpose of this study is to explore pharmacological discoveries which may help to the delay or improvement of the aging process...
November 29, 2017: Current Medicinal Chemistry
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