Modern Approaches for the Discovery of Anti-Infectious Drugs for the Treatment of Neglected Diseases.

abstract：:The increase of pathogens being resistant to antibiotics represents a global health problem and therefore it is a pressing need to develop antibiotics with novel mechanisms of action. Host defense peptides, which have direct antimicrobial activity (also termed antimicrobial peptides) or immune modulating activity, are...

journal_title：Current topics in medicinal chemistry

authors： Lohner K

更新日期：2017-01-01 00:00:00

abstract：:Of the tropical diseases, trypanosomiases and leishmaniases should most concern the pharmaceutical community because of their high prevalence in developing countries and the lack of effective drug treatments. Despite this, they have not historically received much attention in terms of investment and research effort, n...

journal_title：Current topics in medicinal chemistry

authors： Bolognesi ML

更新日期：2011-11-01 00:00:00

abstract：:The genetic material in humans contains approximately 6 billion base pairs in the nuclear genome and 16,569 base pairs in the mitochondrial genome [1-3]. In some cases the difference between a healthy and a sick individual consists in only one nucleotide. Thus, it is evident that the pristine replication of the genome...

journal_title：Current topics in medicinal chemistry

authors： Brieba LG

更新日期：2008-01-01 00:00:00

abstract：:One of the main goals of in silico Caco-2 cell permeability models is to identify those drug substances with high intestinal absorption in human (HIA). For more than a decade, several in silico Caco-2 models have been made, applying a wide range of modeling techniques; nevertheless, their capacity for intestinal absor...

journal_title：Current topics in medicinal chemistry

authors： Pham-The H,Cabrera-Pérez MÁ,Nam NH,Castillo-Garit JA,Rasulev B,Le-Thi-Thu H,Casañola-Martin GM

更新日期：2018-01-01 00:00:00

abstract：:Penile erection is a complex physiologic event resulting from the interactions of the nervous system on a highly specialized vascular organ. Activation of central nervous system melanocortinergic (MC) receptors with either endogenous or synthetic melanotropic ligands may initiate and/or facilitate spontaneous penile e...

journal_title：Current topics in medicinal chemistry

authors： King SH,Mayorov AV,Balse-Srinivasan P,Hruby VJ,Vanderah TW,Wessells H

更新日期：2007-01-01 00:00:00

abstract：:Cancer cells alter their metabolism to support the uninterrupted supply of biosynthetic molecules required for continuous proliferation. Glucose metabolism is frequently reprogrammed in several tumors in addition to fatty acid, amino acid and glutamine metabolism. Pyruvate Dehydrogenase Kinase (PDK) is a gatekeeper en...

journal_title：Current topics in medicinal chemistry

authors： Sradhanjali S,Reddy MM

更新日期：2018-01-01 00:00:00

abstract：:Alzheimer's Disease (AD) once considered a rare disorder emerges as a major health concern in recent times. The disease pathogenesis is very complex and yet to be understood completely. However, "Amyloid Cascade" is the central event in disease pathogenesis. Several proteins of the amyloid cascade are currently being ...

journal_title：Current topics in medicinal chemistry

authors： Chakraborty S

更新日期：2017-01-01 00:00:00

abstract：:Increasing evidence has shown that chemokine receptors may form functional dimers with unique pharmacological profiles. A common practice to characterize such G protein-coupled receptor dimerization processes is to apply bivalent ligands as chemical probes which can interact with both receptors simultaneously. Current...

journal_title：Current topics in medicinal chemistry

authors： Arnatt CK,Zhang Y

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:Glycogen synthase kinase-3 (GSK-3) is involved in the phosphorylation and inactivation of glycogen synthase. GSK-3 inhibitors have been associated with a variety of diseases, including Alzheimer´s disease (AD), diabetes type II, neurologic disorders, and cancer. The inhibition of GSK-3β isoforms is likely to...

journal_title：Current topics in medicinal chemistry

authors： Francisco CS,Javarini CL,de S Barcelos I,Morais PAB,de Paula H,de S Borges W,Neto ÁC,Lacerda V

更新日期：2020-01-01 00:00:00

abstract：:Choline kinase (CK) is a homodimeric enzyme that catalyses the transfer of the ATP γ-phosphate to choline, generating phosphocholine and ADP in the presence of magnesium. Several isoforms of CK are present in humans but only the HsCKα has been associated with cancer and validated as a drug target to treat this disease...

journal_title：Current topics in medicinal chemistry

authors： Serran-Aguilera L,Nuti R,López-Cara LC,Ríos-Marco P,Carrasco MP,Marco C,Entrena A,Macchiarulo A,Hurtado-Guerrero R

更新日期：2014-01-01 00:00:00

abstract：:The structure-activity relationships of azetidine-based DPP IV inhibitors will be discussed in detail in the following review. The azetidine-based DPP IV inhibitors can be divided into three main subtypes, the 2-cyanoazetidines, 3-fluoroazetidines and 2-ketoazetidines. These subtypes have been explored and structure-a...

journal_title：Current topics in medicinal chemistry

authors： Ferraris D,Belyakov S,Li W,Oliver E,Ko YS,Calvin D,Lautar S,Thomas B,Rojas C

更新日期：2007-01-01 00:00:00

abstract：:The sol-gel process provides a robust and versatile technology for the immobilization of biologicals. A wide range of inorganic, composites and hybrid materials can be prepared to encapsulate molecular drugs, proteins, antibodies/antigens, enzymes, nucleic acids, prokaryotic and eukaryotic cells into bulk gels, partic...

journal_title：Current topics in medicinal chemistry

authors： Wang X,Ahmed NB,Alvarez GS,Tuttolomondo MV,Hélary C,Desimone MF,Coradin T

更新日期：2015-01-01 00:00:00

abstract：:In recent times, the novel concept of generating hybrid molecules by pharmacophoric hybridisation approach is fast becoming an alternative to other existing strategies of drug development. These hybrids also known as 'dual drugs' or 'double drugs' are especially found to be effective in overcoming drug resistance prob...

journal_title：Current topics in medicinal chemistry

authors： Manohar S,Tripathi M,Rawat DS

更新日期：2014-01-01 00:00:00

abstract：:Identifying drug binding sites and elucidating drug action mechanisms are important components in a drug discovery process. In this review, we briefly compared three different approaches (sequence- based methods, structure-based methods and probe-based molecular dynamics (MD) methods) to identifying drug binding sites...

journal_title：Current topics in medicinal chemistry

authors： Wang Y,Lupala CS,Liu H,Lin X

更新日期：2018-01-01 00:00:00

abstract：:Machine learning (ML) computational methods for predicting compounds with pharmacological activity, specific pharmacodynamic and ADMET (absorption, distribution, metabolism, excretion and toxicity) properties are being increasingly applied in drug discovery and evaluation. Recently, machine learning techniques such as...

journal_title：Current topics in medicinal chemistry

authors： Dobchev DA,Pillai GG,Karelson M

更新日期：2014-01-01 00:00:00

abstract：:The introduction of biochemical biomarkers in the evaluation of patients with cardiovascular disease has led to practice-changing advancements in the way these patients are diagnosed and managed. Measurements of cardiac troponins or brain-type natriuretic peptide (BNP) and its precursor, N-terminal brain-type natriure...

journal_title：Current topics in medicinal chemistry

authors： Giannopoulos G,Deftereos S,Panagopoulou V,Kossyvakis C,Kaoukis A,Bouras G,Pyrgakis V,Cleman MW

更新日期：2013-01-01 00:00:00

abstract：:This review highlights the biological importance of many polysubstituted nitro-prolines and -pyrrolidines. Their preparation using asymmetric 1,3-dipolar cycloadditions of azomethine ylides with nitroalkenes using diastereoselective and enantioselective strategies is described remarking the scope and main features of ...

journal_title：Current topics in medicinal chemistry

authors： Nejera C,Sansano JM

更新日期：2014-01-01 00:00:00

abstract：:Interest in the chemistry and biological properties of non-nucleoside N-glycosidic compounds has gathered pace over the past several years; the occurrence of the N-glycoside moiety in glycoproteins and a range of active natural products has prompted the synthesis of a diverse spectrum of related materials with promisi...

journal_title：Current topics in medicinal chemistry

authors： Norris P

更新日期：2008-01-01 00:00:00

abstract：:Iron chelators may be of value as therapeutic agents in the treatment of cancer. They may act by depleting iron, a necessary nutrient, and limiting tumor growth. Alternatively or additionally, they may form redox-active metal complexes that cause oxidative stress via production of reactive oxygen species, damaging cri...

journal_title：Current topics in medicinal chemistry

authors： Buss JL,Greene BT,Turner J,Torti FM,Torti SV

更新日期：2004-01-01 00:00:00

abstract：:In the late 1970s and the early 1980s the initial p38 chemotype, the triaryl imidazoles, was discovered as an off-target effect during the development of cyclooxygenase and 5-lipoxygenase inhibitors long before the identity of the p38 kinase was known. During the last 10 years a number of novel p38 chemotypes were dis...

journal_title：Current topics in medicinal chemistry

authors： Diller DJ,Lin TH,Metzger A

更新日期：2005-01-01 00:00:00

abstract：:Kynurenic acid (KYNA), one of the metabolites belonging to the kynurenine pathway, has been described as an important neuroprotective compound, its unbalancing being associated with several pathological conditions. In human brain, the majority of KYNA production is sustained by kynurenine aminotransferase II (KAT II)....

journal_title：Current topics in medicinal chemistry

authors： Casazza V,Rossi F,Rizzi M

更新日期：2011-01-01 00:00:00

abstract：:This article focuses on the GDNF family of neurotrophic factors as a potential new class of therapeutics for neuropathic pain, with a particular emphasis on the ligands, artemin and GDNF. In vivo activity of the ligands, expression of ligands and receptors after peripheral nerve injury, and modulation of nerve injury-...

journal_title：Current topics in medicinal chemistry

authors： Sah DW,Ossipov MH,Rossomando A,Silvian L,Porreca F

更新日期：2005-01-01 00:00:00

abstract：:A major strategy used in drug design is the inhibition of enzyme activity. The ability to accurately measure the concentration of the inhibitor which is required to inhibit a given biological or biochemical function by half is extremely important in ranking compounds. Since the concept of the half maximal inhibitory c...

journal_title：Current topics in medicinal chemistry

authors： Caldwell GW,Yan Z,Lang W,Masucci JA

更新日期：2012-01-01 00:00:00

abstract：:Core histone acetylation is a key prerequisite for chromatin decondensation and plays a pivotal role in regulation of chromatin structure, function and dynamics. The addition of acetyl groups disturbs histone/DNA interactions in the nucleosome and alters histone/histone interactions in the same or adjacent nucleosomes...

journal_title：Current topics in medicinal chemistry

authors： Koprinarova M,Schnekenburger M,Diederich M

更新日期：2016-01-01 00:00:00

abstract：:Over activation of the NMDA receptor complex has been implicated in a number of neurological conditions. The use of NMDA antagonists as therapeutic agents has been limited by serious cognitive and motor side effects. Significant efforts have been reported in the development of NR2B subtype-selective antagonists, which...

journal_title：Current topics in medicinal chemistry

authors： Layton ME,Kelly MJ 3rd,Rodzinak KJ

更新日期：2006-01-01 00:00:00

abstract：:Release of somatostatin into the circulation from the activated TRPV1-expressing nociceptors revealed by antidromic stimulation of dorsal roots in the rat pinpointed to a novel potential drug target on these nociceptors. The review summarizes the functional, biochemical and pharmacological evidence for a novel somatos...

journal_title：Current topics in medicinal chemistry

authors： Szolcsányi J,Pintér E,Helyes Z,Petho G

更新日期：2011-01-01 00:00:00

abstract：:Melatonin was found to be a potent free radical scavenger in 1993. Since then over 800 publications have directly or indirectly confirmed this observation. Melatonin scavenges a variety of reactive oxygen and nitrogen species including hydroxyl radical, hydrogen peroxide, singlet oxygen, nitric oxide and peroxynitrite...

journal_title：Current topics in medicinal chemistry

authors： Tan DX,Reiter RJ,Manchester LC,Yan MT,El-Sawi M,Sainz RM,Mayo JC,Kohen R,Allegra M,Hardeland R

更新日期：2002-02-01 00:00:00

abstract：:Estrogens control a wide number of aspects of human physiology and play a key role in multiple diseases, including cancer. Estrogens act by binding to and activating the cognate receptor (ER), however numerous studies have revealed that the G protein-coupled receptor named GPR30/GPER mediates also estrogen signals. As...

journal_title：Current topics in medicinal chemistry

authors： Sinicropi MS,Lappano R,Caruso A,Santolla MF,Pisano A,Rosano C,Capasso A,Panno A,Lancelot JC,Rault S,Saturnino C,Maggiolini M

更新日期：2015-01-01 00:00:00

abstract：:Lipoic acid (LA) is an antioxidant able to produce its effects in aqueous or lipophilic environments. Lipoate is the conjugate base of lipoic acid, and the most prevalent form of LA under physiological conditions. It presents a highly negative reduction potential, increases the expression of antioxidant enzymes and pa...

journal_title：Current topics in medicinal chemistry

authors： Moura FA,de Andrade KQ,dos Santos JC,Goulart MO

更新日期：2015-01-01 00:00:00

abstract：AIMS:The need to find new antimicrobial agents to cope with this phenomenon increases. BACKGROUND:Infection diseases are illness caused by different microorganisms, such as bacteria, among those caused by resistant bacteria are associated with greater morbidity, mortality and cost of the treatment than those caused by...

journal_title：Current topics in medicinal chemistry

authors： Nocedo-Mena D,Garza-González E,González-Ferrara M,Del Rayo Camacho-Corona M

更新日期：2020-01-01 00:00:00