Subtype-selective dopamine receptor radioligands for PET imaging: current status and recent developments.

abstract：:5-Aminoisoquinolin-1-one (5-AIQ) is a water-soluble inhibitor of the poly(ADPribose) polymerases (PARPs), lacking isoform-selectivity. Although of only moderate potency in vitro against PARP-1, it is highly active in many assays in cells and in models in vivo, indicating excellent uptake. Optimisation of the several s...

journal_title：Current medicinal chemistry

authors： Threadgill MD

更新日期：2015-01-01 00:00:00

abstract：:Since its discovery in 1995 adiponectin has garnered considerable interest from the academic, clinical and biotech communities due to its proposed salutary anti-inflammatory, anti-diabetic, anti-atherogenic and cardioprotective properties. As a result our appreciation of adiponectin's structure and the importance of p...

journal_title：Current medicinal chemistry

authors： Hickman IJ,Whitehead JP

更新日期：2012-01-01 00:00:00

abstract：:Peptide-based nanoparticles (pep-NPs) are emerging as promising imaging and therapeutic agents against cancer due to their biocompatibility and tunability. Optimized design of the peptide sequence and moderate conjugation of the sequence with extraneous molecules are crucial to the performance of the inherent properti...

journal_title：Current medicinal chemistry

authors： An L,Shah Gilani MR,Liang G

更新日期：2014-01-01 00:00:00

abstract：:β-Aryl-β-amino acids constitute very useful scaffolds able to lead, via various intra-molecular cyclisation reactions, to a great diversity of cyclic derivatives with numerous biological and therapeutic properties. The present article aims at reporting an exhaustive overview of these ring-closure sequences and their a...

journal_title：Current medicinal chemistry

authors： Rochais C,Rault S,Dallemagne P

更新日期：2010-01-01 00:00:00

abstract：:The neuropeptide substance P (SP) shows a widespread distribution in both the central and peripheral nervous systems and it is known that after binding to the neurokinin-1 (NK-1) receptors, SP regulates many biological functions in the central nervous system such as emotional behaviour, stress, depression, anxiety, em...

journal_title：Current medicinal chemistry

authors： Muñoz M,Coveñas R

更新日期：2011-01-01 00:00:00

abstract：:Dendrotoxins are small proteins isolated from mamba (Dendroaspis) snakes. The original dendrotoxin was found in venom of the Eastern green mamba, Dendroaspis angusticeps, and related proteins were subsequently found in other mamba venoms. The dendrotoxins contain 57-60 amino acid residues cross-linked by three disulph...

journal_title：Current medicinal chemistry

authors： Harvey AL,Robertson B

更新日期：2004-12-01 00:00:00

abstract：:Protein Kinase Inhibitors (PKIs) and Histone Deacetylase Inhibitors (HDACIs) are two important classes of anticancer agents and have provided a variety of small molecule drugs for the treatment of various types of human cancers. However, malignant tumors are of a multifactorial nature that can hardly be "cured" by tar...

journal_title：Current medicinal chemistry

authors： Ling Y,Liu J,Qian J,Meng C,Guo J,Gao W,Xiong B,Ling C,Zhang Y

更新日期：2020-01-01 00:00:00

abstract：:Despite advances in cancer treatment, a large number of patients eventually develop metastatic disease that is generally incurable. Systemic chemotherapy remains the standard treatment for these patients. Several chemotherapeutic combinations have proven effective in the management of cancer. Paradoxically, although t...

journal_title：Current medicinal chemistry

authors： Prados J,Alvarez PJ,Melguizo C,Rodriguez-Serrano F,Carrillo E,Boulaiz H,Vélez C,Marchal JA,Caba O,Ortiz R,Rama A,Aranega A

更新日期：2012-01-01 00:00:00

abstract：:Snakes are fascinating creatures and have been residents of this planet well before ancient humans dwelled the earth. Venomous snakes have been a figure of fear, and cause notable mortality throughout the world. The venom constitutes families of proteins and peptides with various isoforms that make it a cocktail of di...

journal_title：Current medicinal chemistry

authors： Waheed H,Moin SF,Choudhary MI

更新日期：2017-01-01 00:00:00

abstract：:A growing body of evidence has shown that oxidative stress may be involved in the development of vascular complications associated with diabetes. However, the molecular mechanism for increased reactive oxygen species (ROS) production in diabetes remains uncertain. Among various possible mechanisms, attention have incr...

journal_title：Current medicinal chemistry

authors： Inoguchi T,Tsubouchi H,Etoh T,Kakimoto M,Sonta T,Utsumi H,Sumimoto H,Yu HY,Sonoda N,Inuo M,Sato N,Sekiguchi N,Kobayashi K,Nawata H

更新日期：2003-09-01 00:00:00

abstract：BACKGROUND:Fatty liver, or steatosis, is a condition of excess accumulation of lipids, mainly under form of triglycerides (TG), in the liver, and it is the hallmark of non-alcoholic fatty liver disease (NAFLD). NAFLD is the most common liver disorder world-wide and it has frequently been associated with obesity, hyperl...

journal_title：Current medicinal chemistry

authors： Vergani L

更新日期：2019-01-01 00:00:00

abstract：:Mycobacterium tuberculosis (Mtb), the main aetiological agent of tuberculosis (TB) in humans, is estimated to cause nearly two million deaths every year. Despite their huge therapeutic value, existing antitubercular drugs have several shortcomings, such as for instance the insurgence of drug resistance, which is mostl...

journal_title：Current medicinal chemistry

authors： Fanzani L,Porta F,Meneghetti F,Villa S,Gelain A,Lucarelli AP,Parisini E

更新日期：2015-01-01 00:00:00

abstract：:The hyaluronidases (HAases) are a group of less extensively studied glycosidases distributed throughout the animal kingdom and are popularly known as 'spreading factors'. In recent years, HAases received much attention due to their ability to abruptly alter the hyaluronic acid (HA) homeostasis. HAases preferentially d...

journal_title：Current medicinal chemistry

authors： Girish KS,Kemparaju K,Nagaraju S,Vishwanath BS

更新日期：2009-01-01 00:00:00

abstract：:The introduction of highly active antiretroviral therapy (HAART) in 1996 dramatically changed the course of HIV infection. This therapy involves the use of at least three agents from two distinct classes of antivirals: a protease inhibitor (PI) in combination with two nucleoside/nucleotide reverse transcriptase inhibi...

journal_title：Current medicinal chemistry

authors： Mastrolorenzo A,Rusconi S,Scozzafava A,Barbaro G,Supuran CT

更新日期：2007-01-01 00:00:00

abstract：:The concept of click chemistry represented by the formation of the 1,2,3-triazole core has found wide application in drug discovery, particularly in the early discovery phases and the lead optimization process. 1,2,3-Triazoles ha ve attracted considerable attention in recent years because of their wide range of biolog...

journal_title：Current medicinal chemistry

authors： Raic-Malic S,Mescic A

更新日期：2015-01-01 00:00:00

abstract：:ATP binding cassette (ABC) transporters are involved in drug absorption, distribution and elimination. They also mediate multidrug resistance in cancer cells. Isoflavones, such as genistein (GNT), belong to a class of naturally-occurring compounds found at high concentrations in commonly consumed soya based-foods and ...

journal_title：Current medicinal chemistry

authors： Rigalli JP,Ciriaci N,Mottino AD,Catania VA,Ruiz ML

更新日期：2016-01-01 00:00:00

abstract：:The human body is composed of 60 trillion cells, which have their origin in a fertilized egg. During development, the potential of a cell or tissue can be achieved by environmental manipulation. Then, what molecular determinants underlie or accompany the potential of the cells? To obtain a broader understanding of the...

journal_title：Current medicinal chemistry

authors： Toyoda M,Hamatani T,Okada H,Matsumoto K,Saito H,Umezawa A

更新日期：2010-01-01 00:00:00

abstract：:Neural differentiation of embryonic stem cells (ESC) is considered a promising model to perform in vitro testing for neuroactive and neurotoxic compounds. We studied the potential of a dual reporter murine ESC line to identify bioactive and/or toxic compounds. This line expressed firefly luciferase under the control o...

journal_title：Current medicinal chemistry

authors： Kern I,Xu R,Julien S,Suter DM,Preynat-Seauve O,Baquié M,Poncet A,Combescure C,Stoppini L,Thriel CV,Krause KH

更新日期：2013-01-01 00:00:00

abstract：BACKGROUND:Since Signal Transducer and Activator of Transcription 3 (STAT3) is a transcription factor which plays an important role in multiple aspects of cancer, including progression and migration, and it is constitutively activated in various human tumors, STAT3 inhibition has emerged as a validated strategy for the...

journal_title：Current medicinal chemistry

authors： Gelain A,Mori M,Meneghetti F,Villa S

更新日期：2019-01-01 00:00:00

abstract：:Reprogramming technologies have been developed to revert somatic differentiated cells into pluripotent stem cells that can be differentiated into different lineages potentially useful in stem cell therapy. Reprogramming methods have been progressively refined to increase their efficiency, to obtain a cell population s...

journal_title：Current medicinal chemistry

authors： Tafani M,Perrone GA,Pucci B,Russo A,Bizzarri M,Mechanick JI,Carpi A,Russo MA

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:The sterile alpha motif (Sam) domain is a small helical protein module, able to undergo homo- and hetero-oligomerization, as well as polymerization, thus forming different types of protein architectures. A few Sam domains are involved in pathological processes and consequently, they represent valuable target...

journal_title：Current medicinal chemistry

authors： Vincenzi M,Mercurio FA,Leone M

更新日期：2020-01-01 00:00:00

abstract：:Honey has successfully been used in the treatment of a broad spectrum of injuries including burns and non-healing wounds. It acts as an antibacterial and anti-biofilm agent with anti/pro-inflammatory properties. However, besides these traditional properties, recent evidence suggests that honey is also an immunomodulat...

journal_title：Current medicinal chemistry

authors： Martinotti S,Bucekova M,Majtan J,Ranzato E

更新日期：2019-01-01 00:00:00

abstract：:Glucocorticoids (GC) play a fundamental role in controlling physiologic homeostasis and, when present in excess, can have a detrimental impact on glucose control, blood pressure and lipid levels. The oxidoreductase 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) mainly catalyzes the intracellular regeneration...

journal_title：Current medicinal chemistry

authors： Ge R,Huang Y,Liang G,Li X

更新日期：2010-01-01 00:00:00

abstract：:Breast cancer is an example of a solid tumour which is well treated in the early stages of disease by surgical excision, but once metastatic spread has occurred, medical therapies (chemotherapy and radiotherapy) are highly toxic, expensive and palliative. It is known that certain tumours exhibit specific patterns of m...

journal_title：Current medicinal chemistry

authors： Dowsland MH,Harvey JR,Lennard TW,Kirby JA,Ali S

更新日期：2003-04-01 00:00:00

abstract：:Complement plays a vital role in our innate immune defense against invasive microorganisms. Excessive complement activation or insufficient control of activation on host cells, however, is associated with several chronic disorders. Essential to the activation and amplification of the Alternative Pathway (AP) of comple...

journal_title：Current medicinal chemistry

authors： Wiles JA,Galvan MD,Podos SD,Geffner M,Huang M

更新日期：2020-01-01 00:00:00

abstract：:About 2.3% of the world's population is infected with hepatitis C virus (HCV) and patients have a high risk of developing liver cirrhosis and its complications. Current therapeutic strategies are based on a combination of pegylatedinterferon, ribavirin and (only for patients with genotype 1 infection) a protease inhib...

journal_title：Current medicinal chemistry

authors： Gentile I,Borgia F,Buonomo AR,Zappulo E,Castaldo G,Borgia G

更新日期：2014-01-01 00:00:00

abstract：:Analytical chemists have increasingly turned their attention to drug discovery and drug analysis and to solve fundamental questions of biological significance in physiology and genetics. New technologies have been developed, and a variety of instruments have been redesigned for biomedical applications. The development...

journal_title：Current medicinal chemistry

authors： Hanai T

更新日期：2005-01-01 00:00:00

abstract：:Two-component signal transduction systems and their expanded variants known as phosphorelays are integral elements of the virulence and antimicrobial resistance responses of a wide range of pathogenic bacteria and fungi and also regulate essential functions. As a consequence, two-component systems and phosphorelays ar...

journal_title：Current medicinal chemistry

authors： Stephenson K,Hoch JA

更新日期：2004-03-01 00:00:00

abstract：:Substituted 2-arylbenzothiazoles have emerged in recent years as an important pharmacophore in a number of diagnostic and therapeutic settings. Attractive features of drug candidates based on this benzothiazole scaffold include their synthetic accessibility, and synthetic approaches to 2-arylbenzothiazole-based compou...

journal_title：Current medicinal chemistry

authors： Weekes AA,Westwell AD

更新日期：2009-01-01 00:00:00

abstract：:To this point, efforts to develop therapeutic peptides for intracellular applications were guided by the perception that unmodified linear peptides are highly unstable and therefore structural modifications are required to reduce proteolytic breakdown. Largely, this concept is a consequence of the fact that most resea...

journal_title：Current medicinal chemistry

authors： Zuconelli CR,Brock R,Adjobo-Hermans MJW

更新日期：2017-01-01 00:00:00