Gold(III) Complexes in the Oncological Preclinical Arena: From Aminoderivatives to Peptidomimetics.

abstract：:The computational assessment of drug metabolism has gained considerable interest in pharmaceutical research. Amongst others, machine learning techniques have been employed to model relationships between the chemical structure of a compound and its metabolic fate. Examples for these techniques, which were originally de...

journal_title：Current topics in medicinal chemistry

authors： Fox T,Kriegl JM

更新日期：2006-01-01 00:00:00

abstract：:The pharmacophore modeling in modern drug research has been applied for both bioactivity profiling and early stage of risk assessment of potential side effects and toxicity due to interactions of drug candidates with antitargets namely P-glycoprotein, hERG, cytochrome P450 and pregnane X-receptor. In this article, an ...

journal_title：Current topics in medicinal chemistry

authors： Thai KM,Ngo TD,Tran TD,Le MT

更新日期：2013-01-01 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：:Autoimmune diseases are characterized by the production of autoantibodies directed against specific organs of own organism. Additional common traits of autoimmune diseases are chronic inflammation due to generation of inflammatory mediators, and disorders of redox processes. The pathogenesis of autoimmune diseases is ...

journal_title：Current topics in medicinal chemistry

authors： Tomczynska M,Bijak M,Saluk J

更新日期：2016-01-01 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：:Histone deacetylase (HDAC) inhibitors constitute a novel and growing class of anticancer agents that function by altering intracellular patterns of histone acetylation, the so-called epigenetic "histone code," thereby producing changes in cell cycle arrest, differentiation, and/or apoptosis in tumor cells. This overvi...

journal_title：Current topics in medicinal chemistry

authors： Moradei O,Vaisburg A,Martell RE

更新日期：2008-01-01 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：:In the last few years, there has been a great increase in our understanding of pain mechanisms. Given the complexity of the mechanisms involved in pain modulation, it is surprising that the pharmacological control of pain through the application of relatively simple analgesics can be effective. Nevertheless, the appli...

journal_title：Current topics in medicinal chemistry

authors： Mico JA,Berrocoso E,Ortega-Alvaro A,Gibert-Rahola J,Rojas-Corrales MO

更新日期：2006-01-01 00:00:00

abstract：:Malaria, caused by protozoa of the genus Plasmodium, remains one of the most dreadful infectious diseases worldwide killing more than 1 million people per year. The emergence of multidrug-resistant parasites highly demands a steadfast and continuous search not only for new targets but also for new anti-infectives addr...

journal_title：Current topics in medicinal chemistry

authors： Wegscheid-Gerlach C,Gerber HD,Diederich WE

更新日期：2010-01-01 00:00:00

abstract：:Natural quinoline alkaloid camptothecin (CPT) is used for the treatment of colon, lung, breast and ovarian cancers still facing challenges due to low solubility in aqueous and biological fluids. Its lactone form easily converts into a toxic carboxylic form at slightly basic pH, typical in blood and tissue fluid has ra...

journal_title：Current topics in medicinal chemistry

authors： Mishra D,Yadav V,Khare P,Jyotshna,Das MR,Meena A,Shanker K

更新日期：2016-01-01 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：:Parkinson's disease (PD) is one of the most prevalent and severe neurodegenerative disease affecting more than 6.1 million people globally. It is characterized by age-related progressive deterioration of neurological functions caused by neuronal damage or neuronal death. During PD, the dopamineproducing cells in the s...

journal_title：Current topics in medicinal chemistry

authors： Kumar B,Pandey M,Fayaz F,Izneid TA,Pottoo FH,Manchanda S,Sharma A,Sahoo PK

更新日期：2020-01-01 00:00:00

abstract：:PLA2 enzyme catalyses the hydrolysis of cellular phospholipids at the sn-2 position to liberate arachidonic acid and lysophospholipid to generate a family of pro-inflammatory eicosanoids and platelet activating factor. The generation of pro-inflammatory eicosanoids involves a series of free radical intermediates with ...

journal_title：Current topics in medicinal chemistry

authors： Nanda BL,Nataraju A,Rajesh R,Rangappa KS,Shekar MA,Vishwanath BS

更新日期：2007-01-01 00:00:00

abstract：:Aurora kinases are a group of serine/threonine kinases responsible for the regulation of mitosis. In recent years, with the increase in Aurora kinase-related research, the important role of Aurora kinases in tumorigenesis has been gradually recognized. Aurora kinases have been regarded as a new target for cancer thera...

journal_title：Current topics in medicinal chemistry

authors： Qi G,Liu J,Mi S,Tsunematsu T,Jin S,Shao W,Liu T,Ishimaru N,Tang B,Kudo Y

更新日期：2018-01-01 00:00:00

abstract：:Fragment-based drug discovery (FBDD) needs a biophysical assay to complement, or even replace, biochemical screening. NMR is the best choice for this because NMR delivers many different types of data that impacts medicinal chemistry decisions. There are a multitude of different NMR methods which can be employed to the...

journal_title：Current topics in medicinal chemistry

authors： Zartler ER,Mo H

更新日期：2007-01-01 00:00:00

abstract：:Firefly shows bioluminescence by "luciferin-luciferase" (L-L) reaction using luciferin, luciferase, ATP and O2. The chemical photon generation by an enzymatic reaction is widely utilized for analytical methods including biological imaging in the life science fields. To expand photondetecting analyses with firefly biol...

journal_title：Current topics in medicinal chemistry

authors： Hirano T

更新日期：2016-01-01 00:00:00

abstract：:There exists a huge attrition rate of molecules in clinical trials. It was expected that high-throughput screening and combinatorial chemistry would make the task of producing drugs easier. However, the efforts of the past decade have not been an unvarnished success. As a result, a lot of experimental and computationa...

journal_title：Current topics in medicinal chemistry

authors： Ajay

更新日期：2002-12-01 00:00:00

abstract：:Histone deacetylases (HDACs) have recently emerged as key elements in epigenetic control of gene expression. Due to the implication of HDACs in a variety of diseases ranging from cancer to neurodegenerative disorder, HDAC inhibitors have received increased attention in recent years. Over the last few decades, a myriad...

journal_title：Current topics in medicinal chemistry

authors： Kim B,Hong J

更新日期：2015-01-01 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：:The first-ever World Chagas Disease Day, celebrated in April 14, 2020, is a key initiative to raise awareness of the impact of this neglected tropical disease (NTD). This landmark comes along with the first World NTD Day and the new WHO Road Map on NTDs for 2021-2030. ...

journal_title：Current topics in medicinal chemistry

authors： Ferreira LLG,Andricopulo AD

更新日期：2020-01-01 00:00:00

abstract：:Chemical genomics combines chemistry with molecular biology as a means of exploring the function of unknown proteins or identifying the proteins responsible for a particular phenotype induced by a small cell-permeable bioactive molecule. Chemical genomics therefore has the potential to identify and validate therapeuti...

journal_title：Current topics in medicinal chemistry

authors： Olsen LC,Færgeman NJ

更新日期：2012-01-01 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：:The design of syringeable cyclodextrin (CD) gels is a developing area in the drug delivery and tissue engineering fields, since they offer the possibility of being administered with minimally invasive maneuvers to form depots that can remain for prolonged time in the implantation site. Two different supramolecular sys...

journal_title：Current topics in medicinal chemistry

authors： Simões SM,Veiga F,Torres-Labandeira JJ,Ribeiro AC,Concheiro A,Alvarez-Lorenzo C

更新日期：2014-01-01 00:00:00

abstract：:(18)F-labeled amino acids are an important class of imaging agents for positron emission tomography (PET) that target the increased rates of amino acid transport by many tumor cells. This class of tracers is structurally diverse, and the biological and imaging properties of a given (18)F-labeled amino acid depends lar...

journal_title：Current topics in medicinal chemistry

authors： Huang C,McConathy J

更新日期：2013-01-01 00:00:00

abstract：:Twenty-five years ago the first small molecule inhibitors of Hsp90 were identified. In the intervening years there has been dramatic progress in basic scientific understanding of the Hsp90 chaperone machinery and in the role of Hsp90 in malignancy. The first-in-class Hsp90 inhibitor 17-AAG entered into Phase I clinica...

journal_title：Current topics in medicinal chemistry

authors： Kim YS,Alarcon SV,Lee S,Lee MJ,Giaccone G,Neckers L,Trepel JB

更新日期：2009-01-01 00:00:00

abstract：:The serotonin receptor subtype 5 HT(1A) was one of the first serotonin receptor subtypes pharmacologically characterized. Over the last twenty years the 5 HT(1A) receptor has been the object of intense research efforts as witnessed by the 5 HT(1A) acting drugs marketed as anxiolytics. In recent years, several new chem...

journal_title：Current topics in medicinal chemistry

authors： Lacivita E,Leopoldo M,Berardi F,Perrone R

更新日期：2008-01-01 00:00:00

abstract：:Cancer research has progressed leaps and bounds over the years. This review is a brief overview of the cancer research, milestone achievements and therapeutic studies on it over the one hundred ten years which would give us an insight into how far we have come to understand and combat this fatal disease leading to mil...

journal_title：Current topics in medicinal chemistry

authors： Shastri S,Chatterjee B,Thakur SS

更新日期：2019-01-01 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：BACKGROUND:The high sequence and structural homology among the hsp90 paralogs - Hsp90α, Hsp90β, Grp94, and Trap-1 - has made the development of paralog-specific inhibitors a challenging proposition. OBJECTIVE:This review surveys the state of developments in structural analysis, compound screening, and structure-based ...

journal_title：Current topics in medicinal chemistry

authors： Gewirth DT

更新日期：2016-01-01 00:00:00

abstract：:In medical oncology, targeted therapy has emerged over the last decade, as the most promising strategy to fight cancer. In addition, a more complete understanding of tumor heterogeneity and pharmacology of the more conventional anti-cancer agents has led to development of metronomic chemotherapy (MC) (i.e. a more freq...

journal_title：Current topics in medicinal chemistry

authors： André N,Pasquier E,Kamen B

更新日期：2012-01-01 00:00:00