Synthesis and properties of 14-epi-1α,25-dihydroxy-19-nortachysterol and its 2-substituted derivatives.

abstract：:Pharmacokinetic limitations affect drug bioavailability determining the loss or the reduction of the pharmacological effects. The Gastro Intestinal tract (GI) and the Blood Brain Barrier (BBB) are the most important restrictive and selective physiological lines of defense of the organism. Although several parameters s...

journal_title：Current topics in medicinal chemistry

authors： Colabufo NA,Berardi F,Contino M,Niso M,Perrone R

更新日期：2009-01-01 00:00:00

abstract：:Monoacylglycerol lipase (MAGL) has been recently proposed as the main enzymatic activity responsible for the in vivo hydrolysis of the most abundant endocannabinoid in the brain, the 2-arachidonoylglycerol (2-AG). The endocannabinoids, mainly anandamide (AEA) and 2-AG, are a class of lipid messengers that modulate a b...

journal_title：Current topics in medicinal chemistry

authors： Viso A,Cisneros JA,Ortega-Gutiérrez S

更新日期：2008-01-01 00:00:00

abstract：:Bacterial infections constitute an always growing health problem worldwide. The resistance to antibiotics of an increasing number of bacterial pathogens necessitates a permanent search for new molecules with different mechanisms of action. Histidine biosynthesis is an ancient pathway found in bacteria, archaebacteria,...

journal_title：Current topics in medicinal chemistry

authors： Monti SM,De Simone G,D'Ambrosio K

更新日期：2016-01-01 00:00:00

abstract：:Cathepsin S has been of increasing interest as a target of medicinal chemistry efforts given its role in modulating antigen-presentation by major histocompatibility class II (MHC II) molecules as well as its involvement in extracellular proteolytic activities. Inhibition of the cathepsin S enzyme reduces degradation o...

journal_title：Current topics in medicinal chemistry

authors： Wiener JJ,Sun S,Thurmond RL

更新日期：2010-01-01 00:00:00

abstract：:The Rho family small GTPases of the Ras superfamily play key roles in regulating diverse signaling pathways that control a myriad of fundamental cellular processes such as cytoskeletal dynamics, cell cycle progression, gene expression, cell polarity, migration and cell transformation. The Rho GTPases cycle between an ...

journal_title：Current topics in medicinal chemistry

authors： Ding F,Yin Z,Wang HR

更新日期：2011-12-01 00:00:00

abstract：:Most drug discovery programs today originate by selection of 'hit' molecules resulting from assays against large compound screening libraries. The chemical space in which these hits reside has implications for its biological activity in vivo and likelihood of progression to a drug candidate. We have created a database...

journal_title：Current topics in medicinal chemistry

authors： Zuegg J,Cooper MA

更新日期：2012-01-01 00:00:00

abstract：:Dementia is an increasing health problem in older aged populations worldwide. Age-related changes in the brain can be observed decades before the first symptoms of cognitive decline appear. Cognitive impairment has chronic inflammatory components, which can be enhanced by systemic immune activation. There exist mutual...

journal_title：Current topics in medicinal chemistry

authors： Leblhuber F,Steiner K,Geisler S,Fuchs D,Gostner JM

更新日期：2020-01-01 00:00:00

abstract：:Although water molecules are small and only consist of two different atom types, they play various roles in cellular systems. This review discusses their influence on the binding process between biomacromolecular targets and small molecule ligands and how this influence can be modeled in computational drug design appr...

journal_title：Current topics in medicinal chemistry

authors： de Beer SB,Vermeulen NP,Oostenbrink C

更新日期：2010-01-01 00:00:00

abstract：:In last decades, diet and dietary components have been regarded as important strategies to prevent the development or mitigate numerous chronic diseases, including inflammation, cardiovascular pathologies, cancer, etc. One of the most common dietary components of Asian population is soy. A plethora of research shows t...

journal_title：Current topics in medicinal chemistry

authors： Nabavi SF,Daglia M,Tundis R,Loizzo MR,Sobarzo-Sanchez E,Orhan IE,Nabavi SM

更新日期：2015-01-01 00:00:00

abstract：:Rheumatoid Arthritis (RA) is a chronic autoimmune inflammatory disease that affects largely synovial joints. It has been postulated that activated autoreactive CD4 T cells play a key role in triggering and/or maintaining the chronic inflammatory process in RA. Dendritic cells (DCs) are antigen-presenting cells that ac...

journal_title：Current topics in medicinal chemistry

authors： Rodríguez-Fernández JL

更新日期：2013-01-01 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：:Rexinoids are selective ligands for the nuclear receptors known as RXRs. They do not bind to the receptors for all-trans-retinoic acid (RARs). Many new rexinoids have been synthesized and then assayed for their ability to suppress proliferation of cancer cells, to inhibit activation of inflammatory cells of the tumor ...

journal_title：Current topics in medicinal chemistry

authors： Liby KT,Sporn MB

更新日期：2016-06-16 00:00:00

abstract：:Telomeres are structurally nucleoprotein complexes at termini of linear chromosomes and essential to chromosome stability/integrity. In normal human cells, telomere length erodes progressively with each round of cell divisions, which serves as an important barrier to uncontrolled proliferation and malignant transforma...

journal_title：Current topics in medicinal chemistry

authors： Yuan X,Dai M,Xu D

更新日期：2020-01-01 00:00:00

abstract：:Seizures are one of the most common neurological disorders in clinical medicine. Triggering mechanisms by which seizures form remain unclear, but are related to a rapid change in ionic composition, including an increase of intracellular potassium concentration and pH shifts within the brain. pH buffering of extra- and...

journal_title：Current topics in medicinal chemistry

authors： Thiry A,Dogné JM,Supuran CT,Masereel B

更新日期：2007-01-01 00:00:00

abstract：:Cancer is a multifactorial disease including interactions of complex genetic and environmental factors. Clinical efficacy of anticancer chemotherapies is hampered by various factors including multidrug resistance (MDR). There is a strong need to discover more potent novel cancer drugs to kill cancer cells selectively....

journal_title：Current topics in medicinal chemistry

authors： Kucuksayan E,Ozben T

更新日期：2017-01-01 00:00:00

abstract：:The gradual alignment with all of drug metabolism with all aspects of drug discovery and development has led to a complete realignment of the way the work is conducted. From a background of conducting bespoke in vivo studies much of the work is now in a high throughput screening mode. Large technological advances have...

journal_title：Current topics in medicinal chemistry

authors： Smith DA

更新日期：2011-01-01 00:00:00

abstract：BACKGROUND:Biofilm is a critical virulence factor associated with the strains of Candida spp. pathogens as it confers significant resistance to the pathogen against antifungal drugs. METHODS:A systematic review of the literature was undertaken by focusing on natural products, which have been reported to inhibit biofil...

journal_title：Current topics in medicinal chemistry

authors： Singla RK,Dubey AK

更新日期：2019-01-01 00:00:00

abstract：:The dynamics of gene expression are regulated by histone acetylases (HATs) and histone deacetylases (HDACs) that control the acetylation state of lysine side chains of the histone proteins of chromatin. The catalytic activity of these two enzymes remodels chromatin to control gene expression without altering gene sequ...

journal_title：Current topics in medicinal chemistry

authors： Wiech NL,Fisher JF,Helquist P,Wiest O

更新日期：2009-01-01 00:00:00

abstract：:Much attention has focused on the development of protein kinases as drug targets to treat a variety of human diseases including diabetes, cancer, hypertension and arthritis. To date, Gleevec is one example of a drug targeting protein that has successfully treated human cancer. Several other protein kinase inhibitors a...

journal_title：Current topics in medicinal chemistry

authors： Haystead TA

更新日期：2006-01-01 00:00:00

abstract：:For effective tumour imaging by magnetic resonance imaging (MRI) there is a clear need to develop organ, tissue and cell specific contrast agents that can selectively bind to tumour biomarkers. The versatility of a range of bioconjugation techniques and facile coupling chemistries has facilitated the synthesis of MRI ...

journal_title：Current topics in medicinal chemistry

authors： Kamaly N,Miller AD,Bell JD

更新日期：2010-01-01 00:00:00

abstract：:Coumarins are natural products characterized as 1,2 benzopyrones widely distributed in plants, as well as, in many species of fungi and bacteria. Nowadays, many synthetic procedures allow the discovery of coumarins with expanded chemical space. The ability to exert noncovalent interactions with many enzymes and recept...

journal_title：Current topics in medicinal chemistry

authors： Pereira TM,Franco DP,Vitorio F,Kummerle AE

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:The considerable increase in the incidence of Candida infection in recent times has prompted the use of numerous antifungal agents, which has resulted in the development of resistance towards various antifungal agents. With rising Candida infections, the need for design and development of novel antifungal ag...

journal_title：Current topics in medicinal chemistry

authors： Gowda DV,Afrasim M,Meenakshi SI,Manohar M,Hemalatha S,Siddaramaiah H,Sathishbabu P,Rizvi SMD,Hussain T,Kamal MA

更新日期：2019-01-01 00:00:00

abstract：:Imidazo[1,2-a]pyridine has been shown to be an important biologically active moiety. This review is a compilation of the scattered output of results of the anticancer activities of the imidazo[1,2-a]pyridine system since 2001, which have been classified as inhibition of CDK, VEGFR, PI3K, EGFR, RGGT etc. along with inh...

journal_title：Current topics in medicinal chemistry

authors： Goel R,Luxami V,Paul K

更新日期：2016-01-01 00:00:00

abstract：:Human multidrug resistance protein (MRP/ABCC) family contains 9 members (MRP1-9) which transport a structurally diverse array of anticancer and antimicrobial drugs and several important endogenous substances including prostaglandins (PGs) and leukotrienes (LTs) with different substrate specificity. MRP1-5 can collecti...

journal_title：Current topics in medicinal chemistry

authors： Yang AK,Zhou ZW,Wei MQ,Liu JP,Zhou SF

更新日期：2010-01-01 00:00:00

abstract：:Fatty acid amide hydrolase (FAAH) and monoglyceride lipase (MGL) are hydrolytic enzymes which degrade the endogenous cannabinoids (endocannabinoids) N-arachidonoylethanolamine (anandamide, AEA) and 2-arachidonoylglycerol (2-AG), respectively. Endocannabinoids are an important class of lipid messenger molecules that ar...

journal_title：Current topics in medicinal chemistry

authors： Minkkilä A,Saario S,Nevalainen T

更新日期：2010-01-01 00:00:00

abstract：:Hepatitis C virus (HCV) is a major cause of acute hepatitis and chronic liver disease, including cirrhosis and hepatocellular carcinoma (HCC). No vaccine is currently available to prevent hepatitis C, and the current standard of care (SOC) - pegylated interferon-α (PEG-IFN-α) in combination with ribavirin (RBV) - is o...

journal_title：Current topics in medicinal chemistry

authors： Avolio S,Summa V

更新日期：2010-01-01 00:00:00

abstract：:(2R,3R)-2,3-Butanediol has many industrial applications, such as it is used as an antifreeze agent and low freezing point fuel. In addition, it is particularly important to provide chiral groups in drugs. In recent years, this valuable bio-based chemical has attracted increasing attention, and significant progress has...

journal_title：Current topics in medicinal chemistry

authors： Xie NZ,Chen XR,Wang QY,Chen D,Du QS,Zhou GP,Huang RB

更新日期：2017-01-01 00:00:00

abstract：:The majority of functionally important biological processes are regulated by allosteric communication within individual proteins and across protein complexes. The proteins controlling these communication networks respond to changes in the cellular environment by switching between different conformational states. Targe...

journal_title：Current topics in medicinal chemistry

authors： Persico M,Di Dato A,Orteca N,Fattorusso C,Novellino E,Andreoli M,Ferlini C

更新日期：2015-01-01 00:00:00

abstract：:Neglected diseases comprise a number of infectious diseases historically endemic to low- and middle-income countries, though recently they have spread to high-income countries due to human migrations. In the past, pharmaceutical companies have shown hesitant to invest in these health conditions, due to the limited ret...

journal_title：Current topics in medicinal chemistry

authors： Bellera CL,Sbaraglini ML,Talevi A

更新日期：2018-01-01 00:00:00

abstract：:Following the cloning of the classical opioid receptors (mu, delta and kappa), the opioid receptor like-1 (ORL-1) was identified as a G-protein coupled receptor (GPCR) with 65% structure homology to the other members of the opioid family. Its endogenous ligand nociception/orphanin FQ (N/OFQ) was discovered shortly the...

journal_title：Current topics in medicinal chemistry

authors： Fioravanti B,Vanderah TW

更新日期：2008-01-01 00:00:00