Enzyme Inhibitors as the Attractive Targets for the Treatment of Various Diseases.

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：: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：:Inflammation plays a critical role in the atherosclerotic process in various vascular beds, starting from endothelial dysfunction and counting all stages of plaque development. The significant contribution of inflammation in the initiation and progression of atherosclerosis has been documented over many years but its ...

journal_title：Current medicinal chemistry

authors： Vavuranakis M,Kariori M,Vrachatis D,Siasos G,Kalogeras K,Bei E,Moldovan C,Lavda M,Aznaouridis K,Oikonomou E,Tousoulis D

更新日期：2015-01-01 00:00:00

abstract：:This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researc...

journal_title：Current medicinal chemistry

authors： Akhtar MJ,Yar MS,Sharma VK,Khan AA,Ali Z,Haider MDR,Pathak A

更新日期：2020-01-01 00:00:00

abstract：:Cancer is the world's second leading cause of death after heart diseases, and involves abnormal cell growth at a primary site and the potential to spread to other parts of the body. Tumors are highly heterogeneous and consist of subgroups of cells with distinct characteristics. Of these, the cancer stem cells (CSC) ni...

journal_title：Current medicinal chemistry

authors： Vizetto-Duarte C,Branco PC,Custódio L

更新日期：2020-03-20 00:00:00

abstract：:The serine protease thrombin is a key enzyme in the control of blood coagulation and displays numerous other effects on platelet, endothelial and smooth muscle cell function. The pre-eminence of thrombin in the coagulation cascade has made the enzyme a popular drug target in the search for more clinically acceptable a...

journal_title：Current medicinal chemistry

authors： Menear K

更新日期：1998-12-01 00:00:00

abstract：:Borderline Personality Disorder (BPD) is a common disorder in psychiatric practice and drugs are widely used in its treatment, targeting symptom clusters, such as affective dysregulation, impulsive-behavioural dyscontrol, and cognitive-perceptual symptoms. In last period, a growing number of studies on pharmacological...

journal_title：Current medicinal chemistry

authors： Bellino S,Rinaldi C,Bozzatello P,Bogetto F

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:Metabolic disorders comprise a set of different disorders varying from epidemic diseases such as diabetes mellitus to inborn metabolic orphan diseases such as phenylketonuria. Despite considerable evidence showing the importance of the computational methods in discovery and development of new pharmaceuticals...

journal_title：Current medicinal chemistry

authors： Janardhan S,Dubovskaja V,Lagunin A,Rao BV,Sastry GN,Poroikov V

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:Cholesterol efflux as a key event in reverse cholesterol transport (RCT) is considered now as both diagnostic tool and a promising target for the treatment of atherosclerosis. Radioactive in vitro cholesterol efflux assay (CEA) is the gold standard for determination of efflux at cellular level. Fluorescent t...

journal_title：Current medicinal chemistry

authors： Litvinov DY,Savushkin EV,Garaeva EA,Dergunov AD

更新日期：2016-01-01 00:00:00

abstract：:Gum resin extracts of Boswellia species have been traditionally applied in folk medicine for centuries to treat various chronic inflammatory diseases, and experimental data from animal models and studies with human subjects confirmed the potential of B. spec extracts for the treatment of not only inflammation but also...

journal_title：Current medicinal chemistry

authors： Poeckel D,Werz O

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：:Nitric oxide (NO) has been established as an important messenger molecule in various steps of brain physiology, from development to synaptic plasticity, learning and memory. However, NO has also been viewed as a major agent of neuropathology when, escaping controlled production it may directly or indirectly promote ox...

journal_title：Current medicinal chemistry

authors： Contestabile A,Monti B,Contestabile A,Ciani E

更新日期：2003-10-01 00:00:00

abstract：:ATP-sensitive K(+) channels (K(ATP)channels) regulate insulin secretion by coupling intracellular metabolic changes to excitability of the plasma membrane in pancreatic beta-cells. The channels are closed when extracellular glucose levels are elevated due to enhanced feature. By contrast, cardiac-type K(ATP) channels,...

journal_title：Current medicinal chemistry

authors： Kakei M

更新日期：2003-02-01 00:00:00

abstract：:Fourier-transform infrared (FT-IR) based mapping and imaging is a fast emerging technology which is being increasingly applied to investigate tissues in the high-throughput mode. The high resolution close to the cellular level, the possibility to determine the bio-distribution of molecules of interest (proteins, pepti...

journal_title：Current medicinal chemistry

authors： Petter CH,Heigl N,Rainer M,Bakry R,Pallua J,Bonn GK,Huck CW

更新日期：2009-01-01 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：:Hydroxypyridinones (HPs) are a family of N-heterocyclic metal chelators, which have been an attractive target in the development of a variety of new pharmaceutical drugs, due to their high metal chelating efficacy/specificity and easy derivatization to tune the desired biological properties. In fact, along the last de...

journal_title：Current medicinal chemistry

authors： Chaves S,Piemontese L,Hiremathad A,Santos MA

更新日期：2018-01-01 00:00:00

abstract：:The ionotropic P2X7 receptor (P2X7R) has become the focus of intense research interest for a number of reasons: i) it is a cation selective ion channel that is modulated by extracellular ATP. Upon stimulation by high concentrations of ATP it generates a non-selective membrane pore which is permeable to hydrophilic mol...

journal_title：Current medicinal chemistry

authors： Gunosewoyo H,Coster MJ,Kassiou M

更新日期：2007-01-01 00:00:00

abstract：:Nuclear magnetic resonance spectroscopy has been exploited to study the metabolic characteristics (phenotype) of genetic disorders by taking advantage of some unique characteristics of the technique. The first application, metabolic profiling for diagnosis and therapeutic monitoring in vitro, demonstrates the exceptio...

journal_title：Current medicinal chemistry

authors： Iles RA

更新日期：2008-01-01 00:00:00

abstract：:Sarcomas are tumours of mesenchymal origin, which can arise in bone or soft tissues. They are rare but frequently quite aggressive and with a poor outcome. New approaches are needed to characterise these tumours and their resistance mechanisms to current therapies, responsible for tumour recurrence and treatment failu...

journal_title：Current medicinal chemistry

authors： Heredia-Soto V,Redondo A,Kreilinger JJP,Martínez-Marín V,Berjón A,Mendiola M

更新日期：2020-01-01 00:00:00

abstract：:The nucleotide metabolism has been targeted for many years and in various clinical settings, including cancer. The increased knowledge of certain enzymes involved in this metabolism and in associated cellular processes accumulated over the last few years, gives important information to the druggability of certain prot...

journal_title：Current medicinal chemistry

authors： Forey P,Cros-Perrial E,Dumontet C,Jordheim LP

更新日期：2020-11-25 00:00:00

abstract：:Dimerization and oligomerization of G protein-coupled receptors (GPCRs), proposed almost 30 years ago, have crucial relevance for drug design. Indeed, formation of GPCR oligomers may affect the diversity and performance by which extracellular signals are transferred to G proteins in the process of receptor transductio...

journal_title：Current medicinal chemistry

authors： Kaczor AA,Selent J

更新日期：2011-01-01 00:00:00

abstract：:Limitations associated with the production cost, metabolic instability, side-effects, resistance and poor pharmacokinetics of organic protease inhibitors (PIs), which form an essential component of the front line HAART treatment for HIV, have fuelled efforts into finding novel, transition metal-based alternatives. Som...

journal_title：Current medicinal chemistry

authors： Kellett A,Prisecaru A,Slator C,Molphy Z,McCann M

更新日期：2013-01-01 00:00:00

abstract：:Matrix metalloproteinases (MMPs) are zinc-endopeptidases responsible for degradation of the extracellular matrix (ECM) components including basement membrane collagen, interstitial collagen, fibronectin, and various proteoglycans, during normal remodeling and repair processes. The turnover and remodeling of ECM must b...

journal_title：Current medicinal chemistry

authors： Oikonomidi S,Kostikas K,Tsilioni I,Tanou K,Gourgoulianis KI,Kiropoulos TS

更新日期：2009-01-01 00:00:00

abstract：:Polyphenolic molecules produced by higher plants in response to biotic and abiotic stresses exert numerous effects on tumorigenic cell transformation, and on tumor cells in vitro and in vivo, and may interact with conventional anti-tumor therapies. In the present review, we collected and critically discussed data on: ...

journal_title：Current medicinal chemistry

authors： Korkina LG,De Luca C,Kostyuk VA,Pastore S

更新日期：2009-01-01 00:00:00

abstract：BACKGROUND:COVID-19 has brought the world to its knees and there is an urgent need for new strategies to identify molecules capable of fighting the pandemic. During the last few decades NMR (Nuclear Magnetic Resonance) spectroscopy has emerged as an intriguing structural biology instrument in the antiviral drug discove...

journal_title：Current medicinal chemistry

authors： Vincenzi M,Leone M

更新日期：2020-12-28 00:00:00

abstract：:Correct QSAR analysis requires reliable measured or calculated logP values, being logP the most frequently utilized and most important physico-chemical parameter in such studies. Since the publication of theoretical fundamentals of logP prediction, many commercial software solutions are available. These programs are a...

journal_title：Current medicinal chemistry

authors： Eros D,Kövesdi I,Orfi L,Takács-Novák K,Acsády G,Kéri G

更新日期：2002-10-01 00:00:00

abstract：:The new drug class of dipeptidyl peptidase-4 (DPP4) inhibitors has been widely accepted in the daily management of type 2 diabetes since its strategic advantages with regard to body weight, risk of hypoglycaemia, and beta cell survival. We have previously evaluated the theoretical implications of DPP4 inhibition given...

journal_title：Current medicinal chemistry

authors： Matteucci E,Giampietro O

更新日期：2011-01-01 00:00:00

abstract：:Inflammation is an initial response of the body to a harmful stimuli and it is achieved by the increased movement of leukocytes (especially granulocytes) from blood into injured tissues. It is required for healing wounds and infections. Despite their indispensable role in microbial killing, the inflammation reactions ...

journal_title：Current medicinal chemistry

authors： Soubhye J,Aldib I,Delporte C,Prévost M,Dufrasne F,Antwerpen PV

更新日期：2016-01-01 00:00:00

abstract：:Gossypol, a disesquiterpene from cottonseed, exhibits multiple biological properties, including male antifertility activity and anticancer activity. Gossypol also inhibits the growth of numerous parasitic organisms and shows antiviral activity against a number of enveloped viruses, including the AIDS virus. Derivative...

journal_title：Current medicinal chemistry

authors： Vander Jagt DL,Deck LM,Royer RE

更新日期：2000-04-01 00:00:00

abstract：:Breast cancer arises in about 48% of patients older than 65 years and more than 30% occurs in those over 70 years being the leading cause of cancer-related death in women older than 65. Elderly patients tolerate chemotherapy poorly compared to their younger counterpart because of progressive reduction of organ functio...

journal_title：Current medicinal chemistry

authors： Rossi A,Colantuoni G,Maione P,Ferrara C,Airoma G,Barzelloni ML,Castaldo V,Gridelli C

更新日期：2005-01-01 00:00:00