Non peptidic alphavbeta3 antagonists: recent developments.

abstract：: ...

journal_title：Current medicinal chemistry

authors： Mandraffino G,Saitta A

更新日期：2018-01-01 00:00:00

abstract：:The need for innovation in research is leading to an increased use of imaging biomarkers, which have shown to reduce timings and increase productivity, thus saving costs. PET and SPECT neurotransmission imaging has shown usefulness in the discovery and development of drugs for the central nervous system, providing uni...

journal_title：Current medicinal chemistry

authors： Catafau AM,Bullich S

更新日期：2013-01-01 00:00:00

abstract：:Since the discovery of penicillin, natural and synthetic β-lactams have aroused great interest not only as sources of effective antibacterial agents but also as specific inhibitors of proteases responsible for various non-bacterial pathological processes. This interest was reflected in our review published in Current ...

journal_title：Current medicinal chemistry

authors： Veinberg G,Potorocina I,Vorona M

更新日期：2014-01-01 00:00:00

abstract：:In recent years there has been a growing interest in computer-based screening. One of the driving forces has been the increased efficiency of protein crystallography leading to the real possibility of using structure-based design as a significant contributor to the discovery of novel ligands. In 1957 after 22 years of...

journal_title：Current medicinal chemistry

authors： Glen RC,Allen SC

更新日期：2003-05-01 00:00:00

abstract：:Diabetes mellitus (DM) is a significant healthcare concern worldwide that affects more than 165 million individuals leading to cardiovascular disease, nephropathy, retinopathy, and widespread disease of both the peripheral and central nervous systems. The incidence of undiagnosed diabetes, impaired glucose tolerance, ...

journal_title：Current medicinal chemistry

authors： Maiese K,Chong ZZ,Shang YC

更新日期：2007-01-01 00:00:00

abstract：:Diabetes mellitus (DM) is characterized by hyperglycemia, resulting from defects in insulin secretion, insulin action or both. There are several factors such as hyperlipidemia and oxidative stress (OS), namely the production of reactive oxygen/nitrogen species (ROS/RNS), that actively contribute to the development and...

journal_title：Current medicinal chemistry

authors： Sousa A,Ribeiro D,Fernandes E,Freitas M

更新日期：2020-05-24 00:00:00

abstract：:Whilst knowledge of basic biology, diagnosis and prognosis of glioblastoma (GB - WHO grade IV) are steadily improving, advancements of therapy are discouragingly slow, with the only significant novelty during last ten years represented by introduction of temozolomide in chemotherapy. In order to analyze the current st...

journal_title：Current medicinal chemistry

authors： Frosina G

更新日期：2015-01-01 00:00:00

abstract：:Mammalian ecto ADP-ribosyltransferases (ARTs) constitute a family of structurally related proteins expressed on the cell surface or secreted in the extracellular compartment. Using NAD+ as substrate, they transfer ADP-ribose groups onto target proteins. In contrast to intracellular poly(ADP-ribosyl)transferases (PARPs...

journal_title：Current medicinal chemistry

authors： Seman M,Adriouch S,Haag F,Koch-Nolte F

更新日期：2004-04-01 00:00:00

abstract：:Genetic, experimental and clinical studies have consistently confirmed that inhibition of Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) can result in significant lowering of LDL-C and two fully human PCSK9 monoclonal antibodies have received regulatory approval for use in highrisk patients. Co-administration o...

journal_title：Current medicinal chemistry

authors： Panagiotopoulou O,Chiesa ST,Tousoulis D,Charakida M

更新日期：2020-01-01 00:00:00

abstract：:Now cisplatin and its analogs are some of the most effective chemotherapeutic agents in clinical use as the first line of treatment in testicular and ovarian cancers. Unfortunately, they have several major drawbacks, such as cumulative toxicities of nephrotoxicity and ototoxicity, inherent or treatment-induced resista...

journal_title：Current medicinal chemistry

authors： Zhang J,Zhang F,Li H,Liu C,Xia J,Ma L,Chu W,Zhang Z,Chen C,Li S,Wang S

更新日期：2012-01-01 00:00:00

abstract：:COX-2, a key enzyme that catalyzed the rate-limiting steps in the conversion of arachidonic acid to prostaglandins, played a pivotal role in inflammatory process. Different from other family members, COX-2 was barely detectable in normal physiological conditions and highly inducible during acute inflammatory response ...

journal_title：Current medicinal chemistry

authors： Cui J,Jia J

更新日期：2020-09-17 00:00:00

abstract：:Homocysteine is a thiol aminoacid synthesized during the metabolism of methionine. Increased plasma levels of homocysteine can be the result of mutations in the enzymes responsible for homocysteine metabolism, particularly cystathionine-beta synthase (CBS) and 5,10-methylenetetrahydrofolate reductase (MTHFR). Addition...

journal_title：Current medicinal chemistry

authors： Pezzini A,Del Zotto E,Padovani A

更新日期：2007-01-01 00:00:00

abstract：:Frontotemporal Lobar Degeneration (FTLD) is characterized by behavioral changes, executive dysfunctions, and language impairment, sustained by different neuropathological patterns. The collective efforts of clinical, pathological and genetic studies have recently opened new insights into the underpinnings of pathologi...

journal_title：Current medicinal chemistry

authors： Bigni B,Premi E,Pilotto A,Padovani A,Borroni B

更新日期：2012-01-01 00:00:00

abstract：:Advanced enteropancreatic (EP) neuroendocrine tumors (NETs) can be treated with several different therapies, including chemotherapy, biotherapy, and locoregional treatments. Over the last few decades, impressive progress has been made in the biotherapy field. Three main druggable molecular targets have been studied an...

journal_title：Current medicinal chemistry

authors： Fazio N,Scarpa A,Falconi M

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:Pregnancy specific β1-glycoproteins (PSGs) have long been recognized as trophoblast quality and embryo viability markers. However, biological roles of PSGs remain obscure, and structure/function relationships to other feto-placental proteins as well as implications for drug design have not been reviewed. Thi...

journal_title：Current medicinal chemistry

authors： Moldogazieva NT,Mokhosoev IM,Terentiev AA

更新日期：2017-01-01 00:00:00

abstract：:Angiotensin converting enzyme (ACE) 2 is a homologue of ACE that catalyzes the conversion of Angiotensin (Ang) II into Ang1-7, which induces vasodilation, anti-fibrotic, anti-proliferative and anti-inflammatory effects. Given that ACE2 counterbalances the effects of Ang II, it has been proposed as a biomarker in kidne...

journal_title：Current medicinal chemistry

authors： Anguiano L,Riera M,Pascual J,Soler MJ

更新日期：2017-01-01 00:00:00

abstract：:Diabetic patients have a two- to four-fold increased risk for the development of microvascular (renal, neuronal and retinal) and macrovascular complications. Unfortunately, these complications may develop in both Type 1 and Type 2 diabetic patients even with careful glycaemic, blood pressure and lipid control. With th...

journal_title：Current medicinal chemistry

authors： Soro-Paavonen A,Forbes JM

更新日期：2006-01-01 00:00:00

abstract：:Among the strategies that can lead to the discovery of new drugs, the identification and use of privileged structures, molecular fragments that are able to interact with more than one target, gained particular attention, in an attempt to find new drugs in a shorter time with respect to other strategies. These structur...

journal_title：Current medicinal chemistry

authors： Costantino L,Barlocco D

更新日期：2006-01-01 00:00:00

abstract：:Inosine 5'-monophosphate dehydrogenase (IMPDH) catalyzes the first committed step of guanosine 5'-monophosphate (GMP) biosynthesis, and thus regulates the guanine nucleotide pool, which in turn governs proliferation. Human IMPDHs are validated targets for immunosuppressive, antiviral and anticancer drugs, but as yet m...

journal_title：Current medicinal chemistry

authors： Hedstrom L,Liechti G,Goldberg JB,Gollapalli DR

更新日期：2011-01-01 00:00:00

abstract：:Semicarbazide-sensitive amine-oxidase (SSAO) is present in various human tissues and in plasma. Oxidative deamination of short-chain aliphatic amines is catalyzed by this enzyme to afford the corresponding aldehydes, ammonia and hydrogen peroxide. Methylamine and aminoacetone have been recognized to be physiological s...

journal_title：Current medicinal chemistry

authors： Mátyus P,Dajka-Halász B,Földi A,Haider N,Barlocco D,Magyar K

更新日期：2004-05-01 00:00:00

abstract：BACKGROUND:Pollutants are diverse chemical entities, including gases such as ozone and particulate matter PM. PM contains toxic chemicals such as polycyclic aromatic hydrocarbons (PAHs). Some PAHs can induce strong oxidative stress under UVA exposure. Pollution aggravates some skin diseases such as atopy or eczema, but...

journal_title：Current medicinal chemistry

authors： Marrot L

更新日期：2018-01-01 00:00:00

abstract：:Universal stress proteins are ubiquitously expressed in bacteria, archaea and plants and other eukaryotes. A general property of USPs is their role in adaptation of bacteria to oxidative stress, high temperature, low pH and/or hypoxia. There is increasing evidence that these proteins facilitate the adaption of bacteri...

journal_title：Current medicinal chemistry

authors： O'Connor A,McClean S

更新日期：2017-11-24 00:00:00

abstract：:Essential oils constituents are a diverse family of low molecular weight organic compounds with comprehensive biological activity. According to their chemical structure, these active compounds can be divided into four major groups: terpenes, terpenoids, phenylpropenes, and "others". In addition, they may contain diver...

journal_title：Current medicinal chemistry

authors： Burčul F,Blažević I,Radan M,Politeo O

更新日期：2020-01-01 00:00:00

abstract：:Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT(1A) subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind...

journal_title：Current medicinal chemistry

authors： López-Rodríguez ML,Ayala D,Benhamú B,Morcillo MJ,Viso A

更新日期：2002-02-01 00:00:00

abstract：:Mammalian terminal deoxyribonucleotidyl transferase (TDT) catalyzes the non-template-directed polymerization of deoxyribonucleoside triphosphates and has a key role in V(D)J recombination during lymphocyte and repertoire development. Over 90% of leukemic cells in acute lymphocytic leukemia and approximately 30% of leu...

journal_title：Current medicinal chemistry

authors： Di Santo R,Maga G

更新日期：2006-01-01 00:00:00

abstract：:The utilization of graphene-based nanomaterials combined with magnetic nanoparticles offers key benefits in the modern biomedicine. In this minireview, we focus on the most recent advances in hybrids of magnetic graphene derivatives for biomedical applications. We initially analyze the several methodologies employed f...

journal_title：Current medicinal chemistry

authors： Alegret N,Criado A,Prato M

更新日期：2017-01-01 00:00:00

abstract：:The existence of functional NT/dopamine interactions in the central nervous system has been extensively documented. Among others, a possible molecular mechanism underlying the NT-induced modulation of dopamine release is a direct antagonistic NTS(1)/D(2) receptor interaction. More recently, neurochemical experiments a...

journal_title：Current medicinal chemistry

authors： Tanganelli S,Antonelli T,Tomasini MC,Beggiato S,Fuxe K,Ferraro L

更新日期：2012-01-01 00:00:00

abstract：:Specific noncovalent interactions that are indicative of attractive, directional intermolecular forces have always been of key interest to medicinal chemists in their search for the "glue" that holds drugs and their targets together. With the rapid increase in the number of solved biomolecular structures as well as th...

journal_title：Current medicinal chemistry

authors： Zhou P,Huang J,Tian F

更新日期：2012-01-01 00:00:00

abstract：:Chagas disease is one of the most important endemic diseases in Latin America, caused by Trypanosoma cruzi. The drugs used for the treatment of this disease, nifurtimox and benznidazole, are toxic and present severe side effects. The need of effective drugs, without adverse effects, has stimulated the search for new c...

journal_title：Current medicinal chemistry

authors： Salas CO,Faúndez M,Morello A,Maya JD,Tapia RA

更新日期：2011-01-01 00:00:00

abstract：:Although glial proliferation of the epileptic loci is recognized for more than a century in certain focal epilepsies, the role of astrocytes in epileptic conditions is receiving significant attention only in recent years. The present review will highlight current knowledge about the various ways astrocytes control neu...

journal_title：Current medicinal chemistry

authors： Héja L

更新日期：2014-01-01 00:00:00