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Current Medicinal Chemistry

Xinyu He, Xianzhu Yang, Dongdong Li, Ziyang Cao
Red and NIR light-responsive polymeric nanocarriers capable of on-demand drug delivery have gained tremendous attention for their great potential in cancer therapy. Various strategies have been applied to fabricate such nanocarriers, and they have demonstrated significant therapeutic efficacy and minimal toxicity to normal tissues. Here, we will review the current developments in various red and NIR light-responsive polymeric nanocarriers with respect to their use in on-demand drug delivery, including facilitation of drug internalization and boosting of drug release at targeted sites...
February 14, 2019: Current Medicinal Chemistry
Yixing Qiu, Huanghe Yu, Rong Zeng, Shiyin Guo, Muhammad Daniyal, Zeyu Deng, Aibing Wang, Wei Wang
Obesity, associated with a series of complications such as diabetes, hypertension, and heart disease, is a great threat to human health and leads to increased morbidity and mortality. In spite of the presence of anti-obesity agents on the market, the application of these drugs is limited because of their typical side effects. More effective and safe weight-loss drugs are being pursued by many researchers, correspondingly, growing small molecules and natural products with anti-obesity effects have been identified and the molecular mechanisms underlying the action of novel and known compounds have at least partially been revealed...
February 14, 2019: Current Medicinal Chemistry
U S Swapna Sasi, G Sindhu, P Salin Raj, K G Raghu
MAMs, the physical association between the endoplasmic reticulum (ER) and mitochondria are functional domains, performing a significant role in the maintenance of cellular homeostasis. It is evolving as an important signaling center that coordinates nutrient and hormonal signaling for the proper regulation of hepatic insulin action and glucose homeostasis. Moreover, MAMs can be considered as hot spots for the transmission of stress signals from ER to mitochondria. The altered interaction between ER and mitochondria results in the amendment of several insulin-sensitive tissues, revealing the role of MAMs in glucose homeostasis...
February 12, 2019: Current Medicinal Chemistry
Jiyin Zhou, Zuo Zhang, Hongli Zhou, Guisheng Qian
Type 2 diabetes increases the risk of developing cognitive dysfunction in the elderly in the form of short-term memory and executive function impairment. Genetic and diet-induced models of type 2 diabetes further support this link, displaying deficits in working memory, learning, and memory performance. The risk factors for diabetic cognitive dysfunction include vascular disease, hypoglycaemia, hyperlipidaemia, adiposity, insulin resistance, lifestyle factors, and genetic factors. Using neuronal imaging technologies, diabetic patients with cognitive dysfunction show atrophy of the whole brain, particularly the grey matter, hippocampus and amygdala; increased volume of the ventricular and white matter; brain infarcts; impaired network integrity; abnormal microstructure; and reduced cerebral blood flow and amplitude of low-frequency fluctuations...
February 6, 2019: Current Medicinal Chemistry
Xin Jin, Meng-Lin Jiang, Zhao-Hui Wu, Yu Fan
BACKGROUND: Gastric cancer is a major malignancy that has high incidence rates worldwide. Approximately 30% of patients with gastric cancer have progressed into advanced stages at the time of diagnosis. Chemotherapy is the standard-of-care for most advanced gastric cancer and elicits variable responses among patients. Personalized chemotherapy based on genetic information of individual patients with gastric cancer has gained increasing attention among oncologists for guiding chemotherapeutic regimens...
February 4, 2019: Current Medicinal Chemistry
Ashutosh Dash, Tapas Das, F F Russ Knapp
Bone pain arising from secondary skeletal malignancy constitutes one of the most common types of chronic pain among patients with cancer which can lead to rapid deterioration in quality of life. Radionuclide therapy using bone-seeking radiopharmaceuticals based on the concept of localization of the agent at the bone metastases sites to deliver focal cytotoxic levels of radiation emerged as an effective treatment modality for the palliation of symptomatic bone metastases. Bone-seeking radiopharmaceuticals not only provide palliative benefit but also improve clinical outcomes in term of overall and progression-free survival...
February 1, 2019: Current Medicinal Chemistry
E Pappa, M Elisaf, C Kostara, E Bairaktari, V Tsimihodimos
BACKGROUND: As Mendelian randomization (MR) studies showed no efficacy of variants altering HDL-cholesterol (HDL-C) levels concerning cardiovascular disease (CVD) and novel therapeutic interventions aiming to raise HDL-C resulted to futility, the usefulness of HDL-C is unclear. OBJECTIVE: As the role of HDL-C is currently doubtful, it is suggested that the atheroprotective functions of HDLs can be attributed to the number of HDL particles,and their characteristicsincludingtheir lipid and protein components...
February 1, 2019: Current Medicinal Chemistry
Muhammad Daniyal, Bin Liu, Wei Wang
Motivated by the accomplishment of carbon nano tubes (CNTs), graphene and graphene oxide (GO) have been widely investigated in the previous quite a long while as an innovative medication nanocarrier for the stacking of a variety of therapeutics as well as anti-cancer medications, ineffectively dissolvable medications, anti-microbials, antibodies, peptides, DNA, RNA and genes. The greatly huge surface region of graphene, with each molecule uncovered on its two sides, is took into consideration ultra-high medication stacking effectiveness...
February 1, 2019: Current Medicinal Chemistry
Thais A Sales, Silvana Marcussic Teodorico, C Ramalho
The inflammatory process is a natural self-defense response of the organism to damage agents and its action mechanism involves a series of complex reactions. However, in some cases, this process can become chronic , causing much harm to the body. Therefore, over the years, many anti-inflammatory drugs have been developed aiming to decrease the concentrations of inflammatory mediators in the organism, which is a way of controlling these abnormal chain reactions. The main target of conventional anti-inflammatory drugs is the cyclooxygenase (COX) enzyme, but its use implies several side effects...
February 1, 2019: Current Medicinal Chemistry
Vasco Branco, José Pimentel, Maria Alexandra Brito, Cristina Carvalho
BACKGROUND: Central Nervous System (CNS) tumors have a poor survival prognosis due to their invasive and heterogeneous nature, in addition to the resistance to multiple treatments. OBJECTIVE: In this paper, the main aspects of brain tumor biology and pathogenesis are reviewed both for primary tumors of the brain, (i.e. gliomas) and for metastasis from other malignant tumors, namely lung cancer, breast cancer and malignant melanoma which account for a high percentage of overall malignant brain tumors...
January 31, 2019: Current Medicinal Chemistry
Miroslav Pohanka
Two cholinesterases exist: acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). While AChE plays a crucial role in neurotransmissions, BChE has no specific function apart of the detoxification of some drugs and secondary metabolites from plants. Thus both AChE and BChE can serve as biochemical markers of various pathologies. Poisoning by nerve agents like sarin, soman, tabun, VX, novichok and overdosing by drugs used in some neurodegenerative disorders like Alzheimer´s disease and myasthenia gravis, as well as poisoning by organophosphorus pesticides are relevant to this issue...
January 30, 2019: Current Medicinal Chemistry
Mário Fernandes, Ivo Lopes, José Teixeira, Cláudia Botelho, Andreia C Gomes
Nanoparticles are one of the most used systems for imaging or therapeutic drug delivery. Exosomes are nanovesicular carriers that transport cargo for intercellular communication. These nanovesicles are linked to the pathology of some major diseases, in some cases with a central role in their progression. The use of these carriers to transport therapeutic drugs is a recent and promising approach to treat diseases such as cancer and Alzheimer disease. The physiological production of these structures is limited impairing its collection and subsequent purification...
January 29, 2019: Current Medicinal Chemistry
Carlo Gabriele Tocchetti
No abstract text is available yet for this article.
January 28, 2019: Current Medicinal Chemistry
Jan Tauchen
BACKGROUND: Migraine may be described as a headache with moderate to extreme pain that is often accompanied by incapacitating neurological symptoms. It is estimated that 12% of the world population suffers from migraine. Although a number of drugs have been used for treatment of migraine, most of these are not effective for every patient and may have undesirable side-effects. Thus there is an enormous unmet need in current migraine therapy for discovering safer and more effective agents...
January 25, 2019: Current Medicinal Chemistry
Ana Cristina Fernandes
The search for new metal-efficient drugs has attracted considerable attention of the scientific community. Among them, ruthenium complexes have emerged as an excellent alternative of platinum complexes. This review presents a thorough and timely coverage of the synthesis, biological activity and medicinal applications of ruthenium complexes bearing carbohydrate ligands, allowing a large community of readers, in particularly the community that works in organic, inorganic, bioorganometallic and medicinal chemistry, ready access to the most relevant examples...
January 24, 2019: Current Medicinal Chemistry
Pan Jiang, Feng Yan
tiRNAs & tRFs are a class of small molecular noncoding tRNA derived from precise processing of mature or precursor tRNAs. Most tiRNAs & tRFs described originate from nucleus-encoded tRNAs, and only a few tiRNAs & tRFs have been reported. They have been suggested to play important roles in inhibiting protein synthesis, regulating gene expression, priming viral reverse transcriptases, and the modulation of DNA damage responses. However, the regulatory mechanisms and potential function of tiRNAs & tRFs remain poorly understood...
January 24, 2019: Current Medicinal Chemistry
Hayrettin Ozan Gulcan, Açelya Mavideniz, Mustafa Fethi Sahin, Ilkay Erdogan Orhan
Benzimidazole scaffold has been efficiently used for the design of various pharmacologically active molecules. Indeed, there are various drugs, available today, employed for the treatment of different diseases. Although, there is no benzimidazole moiety containing drug available today for the treatment of Alzheimer's Disease (AD), there have been many benzimidazole derivative compounds designed and synthesized to act on some of the validated and non-validated targets of AD. This paper has aimed to review the literature to describe these benzimidazole containing molecules designed for the treatment of AD...
January 24, 2019: Current Medicinal Chemistry
Cristina Agresti, Rosella Mechelli, Stefania Olla, Caterina Veroni, Cecilia Eleuteri, Giovanni Ristori, Marco Salvetti
BACKGROUND: MS is a chronic inflammatory disease of the CNS leading to demyelination and neurodegeneration, with a complex and still to be clarified aetiology. Several data, coming from patients' samples and from animal models, show that oxidative status (OS) plays an important role in MS pathogenesis. Overproduction of reactive oxidative species by macrophages/microglia can bring about cellular injury and ensuing cell death by oxidizing cardinal cellular components. Oxidized molecules are present in active MS lesions and are associated with neurodegeneration...
January 24, 2019: Current Medicinal Chemistry
Sara Paccosi, Barbara Cresci, Laura Pala, Carlo Maria Rorella, Astrid Parenti
BACKGROUND: Obesity represents the second preventable mortality cause worldwide, and is very often associated with type 2 diabetes mellitus (T2DM). The first line treatment is lifestyle modification to weight-loss, but for who fails the goal or has difficulty in maintaining achieved results, pharmacological treatment is needed. Few drugs are available up today, because of their side effects. OBJECTIVE: We aim to review actual pharmacological management of obese patients, highlighting differences between Food and Drug Administration - and European Medicine Agency-approved molecules, and pointing out on self-medications readily obtainable and widely distributed...
January 24, 2019: Current Medicinal Chemistry
Weslley Felix de Oliveira, Priscila Marcelino Dos Santos Silva, Luana Cassandra Breitenbach Barroso Coelho, Maria Tereza Dos Santos Correia
The discovery of new biomarkers associated with cancer, neurological and cardiovascular diseases is necessary, since these are common, recurrent diseases considered as leading causes of death in the human population. Molecular signatures of these disorders that can be identified at the outset of their pathogenesis leading to prompt and targeted treatment may increase patient survival. Cancer is a heterogeneous disease that can be expressed differently among individuals; in addition, treatments may have a differentiated approach according with the type of malignant neoplasm...
January 23, 2019: Current Medicinal Chemistry
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