Update on Hsp90 inhibitors in clinical trial.

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 clinical trials in 1999. There are now 13 Hsp90 inhibitors in clinical trial, representing multiple drug classes, and hundreds of patients have been treated in adult oncology and pediatric oncology trials. This review will provide an overview of the clinical trial results thus far. In addition, pivotal issues in further development of Hsp90 inhibitors as anticancer drugs will be discussed.

journal_name

Curr Top Med Chem

authors

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

doi

10.2174/156802609789895728

subject

Has Abstract

pub_date

2009-01-01 00:00:00

pages

1479-92

issue

15

eissn

1568-0266

issn

1873-4294

pii

CTMC-Abs-031-9-15

journal_volume

9

pub_type

杂志文章,评审
  • Synthesis and evaluation of indole based molecules for treatment of oxidative stress related diseases.

    abstract::The chemical versatility of the indole nucleus still inspires the pharmaceutical research to develop innovative suitable indole based drugs. The present work is an overview of the use and application of indole molecule based derivatives, as possible treatment in the main Oxidative Stress related diseases, such as card...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026614666141203142926

    authors: Aiello F,Valacchi G

    更新日期:2014-01-01 00:00:00

  • Selective androgen receptor modulators in drug discovery: medicinal chemistry and therapeutic potential.

    abstract::Modulation of the androgen receptor has the potential to be an effective treatment for hypogonadism, andropause, and associated conditions such as sarcopenia, osteoporosis, benign prostatic hyperplasia, and sexual dysfunction. Side effects associated with classical anabolic steroid treatments have driven the quest for...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802606776173456

    authors: Cadilla R,Turnbull P

    更新日期:2006-01-01 00:00:00

  • Half a century of L-DOPA.

    abstract::L-DOPA is a di-hydroxy-phenyl, catecholamine precursor, amino acid, initially considered as an inert compound and now the key stone for the treatment of Parkinson's disease (PD) and some hereditary dystonias. L-DOPA, when administered to mammals, is rapidly metabolized to dopamine and 3-OM-DOPA, and its half-life in p...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:

    authors: Mena MA,Casarejos MJ,Solano RM,de Yébenes JG

    更新日期:2009-01-01 00:00:00

  • Protective effect of schizolobium parahyba flavonoids against snake venoms and isolated toxins.

    abstract::Four compounds (isoquercitrin, myricetin-3-O-glucoside, catechin and gallocatechin) were isolated from lyophilized aqueous extract of Schizolobium parahyba leaves by chromatography on Sephadex LH-20, followed by semipreparative HPLC using a C-18 column, and identified by 1H and 13C NMR. The compounds were then, tested...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/156802611797633438

    authors: F Vale LH,Mendes MM,Fernandes RS,Costa TR,S Hage-Melim LI,A Sousa M,Hamaguchi A,Homsi-Brandeburgo MI,Franca SC,Silva CH,Pereira PS,Soares AM,Rodrigues VM

    更新日期:2011-01-01 00:00:00

  • Metformin - The Drug for the Treatment of Autoimmune Diseases; A New Use of a Known Anti-Diabetic Drug.

    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

    pub_type: 杂志文章,评审

    doi:10.2174/1568026616666160216152324

    authors: Tomczynska M,Bijak M,Saluk J

    更新日期:2016-01-01 00:00:00

  • Biological Activities of Artemisinin Derivatives Beyond Malaria.

    abstract::Artemisinin is isolated from Artemisia annua L. with peroxide-containing sesquiterpene lactone structure. Because of its unique structural characteristics and promising anticancer, antivirus activities, it has recently received increasing attention. The aim of this review is to summarize recent discoveries of artemisi...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026619666190122144217

    authors: Liu X,Cao J,Huang G,Zhao Q,Shen J

    更新日期:2019-01-01 00:00:00

  • Template dependent human DNA polymerases.

    abstract::The genetic material in humans contains approximately 6 billion base pairs in the nuclear genome and 16,569 base pairs in the mitochondrial genome [1-3]. In some cases the difference between a healthy and a sick individual consists in only one nucleotide. Thus, it is evident that the pristine replication of the genome...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802608786141098

    authors: Brieba LG

    更新日期:2008-01-01 00:00:00

  • Biochemical and structural investigations on kynurenine aminotransferase II: an example of conformation-driven species-specific inhibition?

    abstract::Kynurenic acid (KYNA), one of the metabolites belonging to the kynurenine pathway, has been described as an important neuroprotective compound, its unbalancing being associated with several pathological conditions. In human brain, the majority of KYNA production is sustained by kynurenine aminotransferase II (KAT II)....

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/156802611794863599

    authors: Casazza V,Rossi F,Rizzi M

    更新日期:2011-01-01 00:00:00

  • Machine learning techniques for in silico modeling of drug metabolism.

    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

    pub_type: 杂志文章,评审

    doi:10.2174/156802606778108915

    authors: Fox T,Kriegl JM

    更新日期:2006-01-01 00:00:00

  • Inhibition of the function of TRPV1-expressing nociceptive sensory neurons by somatostatin 4 receptor agonism: mechanism and therapeutical implications.

    abstract::Release of somatostatin into the circulation from the activated TRPV1-expressing nociceptors revealed by antidromic stimulation of dorsal roots in the rat pinpointed to a novel potential drug target on these nociceptors. The review summarizes the functional, biochemical and pharmacological evidence for a novel somatos...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802611796904852

    authors: Szolcsányi J,Pintér E,Helyes Z,Petho G

    更新日期:2011-01-01 00:00:00

  • Immunophilins and coupled gating of ryanodine receptors.

    abstract::The ryanodine receptor (RyR) is the major calcium (Ca(2+)) release channel in the sarcoplasmic reticulum (SR) of skeletal and cardiac muscle and is required for excitation-contraction (EC) coupling. The 565 kDa RyR protein forms a tetrameric channel that is part of a macromolecular signaling complex that also includes...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026033451907

    authors: Lehnart SE,Huang F,Marx SO,Marks AR

    更新日期:2003-01-01 00:00:00

  • New Drugs and Therapeutic/Diagnostic Targets for Fungal and Parasitic Diseases - Part I.

    abstract:: ...

    journal_title:Current topics in medicinal chemistry

    pub_type: 社论

    doi:10.2174/156802661815181101110430

    authors: Dea-Ayuela MA,Serrano DR

    更新日期:2018-01-01 00:00:00

  • Syringeable self-assembled cyclodextrin gels for drug delivery.

    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

    pub_type: 杂志文章,评审

    doi:10.2174/1568026613666131219124308

    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

  • Coagulation factor Xa inhibition: biological background and rationale.

    abstract::Ischemic heart disease and cerebrovascular disease are the leading causes of death in the world. Surprisingly, these diseases are treated by relatively antiquated drugs. However, due to our improved understanding of the underlying pathology of these diseases, and a number of technological advances in tools for drug di...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026013395380

    authors: Leadley RJ Jr

    更新日期:2001-06-01 00:00:00

  • Current Breakthroughs in Structure-based Design of Synthetic and Natural Sourced Inhibitors Against Zika Viral Targets.

    abstract:BACKGROUND:Zika is a worldwide pandemic dreadful viral transmission through Aedes mosquito vector. It significantly causes fever, joint pain or rash, and conjunctivitis. Pregnant mothers suffering from Zika viral infection may have fetal abnormalities due to severe neurological problems, characterized by microcephaly a...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1568026619666181120125525

    authors: Nandi S,Kaur R,Kumar M,Sharma A,Naaz A,Mandal SC

    更新日期:2018-01-01 00:00:00

  • A practical guide to sequencing genomes and transcriptomes.

    abstract::The emergence of new DNA sequencing technologies has allowed an exponential growth of genomic and transcriptomic data that ultimately yielded important results to several areas such as medicine and biology. This continuous technological progress presents several advantages and caveats that have to be considered for ea...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026613666131204142353

    authors: Sanchez-Flores A,Abreu-Goodger C

    更新日期:2014-01-01 00:00:00

  • Overview of the Genetic Basis and Epigenetic Mechanisms that Contribute to FASD Pathobiology.

    abstract::Prenatal alcohol (ethanol) exposure (PAE) is the underlying cause for a variety of birth defects and neurodevelopmental deficits referred to as "Fetal Alcohol Spectrum Disorders (FASD)". The more visible phenotypes caused by PAE include growth retardation, and characteristic craniofacial abnormalities associated with ...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026616666160414124816

    authors: Liyanage VR,Curtis K,Zachariah RM,Chudley AE,Rastegar M

    更新日期:2017-01-01 00:00:00

  • Linking Biosynthetic Gene Clusters to their Metabolites via Pathway- Targeted Molecular Networking.

    abstract::The connection of microbial biosynthetic gene clusters to the small molecule metabolites they encode is central to the discovery and characterization of new metabolic pathways with ecological and pharmacological potential. With increasing microbial genome sequence information being deposited into publicly available da...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026616666151012111046

    authors: Trautman EP,Crawford JM

    更新日期:2016-01-01 00:00:00

  • Aptamers overview: selection, features and applications.

    abstract::Apatamer technology has been around for a quarter of a century and the field had matured enough to start seeing real applications, especially in the medical field. Since their discovery, aptamers rapidly emerged as key players in many fields, such as diagnostics, drug discovery, food science, drug delivery and therape...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026615666150413153717

    authors: Hernandez LI,Machado I,Schafer T,Hernandez FJ

    更新日期:2015-01-01 00:00:00

  • New therapeutic frontiers for metabotropic glutamate receptors.

    abstract::Our understanding of glutamatergic transmission in the central nervous system has been greatly expanded with the discovery and investigation of the metabotropic glutamate receptor family. Complementing the ionotropic glutamate-gated ion channels, these G-protein coupled receptors play critical roles in neuronal and gl...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026054750254

    authors: Niswender CM,Jones CK,Conn PJ

    更新日期:2005-01-01 00:00:00

  • Antioxidant properties of melatonin and its potential action in diseases.

    abstract::In recent years, relationship between free radicals and oxidative stress with aging, cancer, atherosclerosis, neurodegenerative disorders, diabetes, and inflammatory diseases became increasingly clear. Confirming the role of oxidants in numerous pathological conditions such as cancer, the antioxidants developed as the...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026615666150220120946

    authors: Karaaslan C,Suzen S

    更新日期:2015-01-01 00:00:00

  • Glutamate receptor agonists: stereochemical aspects.

    abstract::The neurotransmitter (S)-glutamate [(S)-Glu] is responsible for most of the excitatory neurotransmission in the central nervous system. The effect of (S)-Glu is mediated by both ionotropic and metabotropic receptors. Glutamate receptor agonists are generally α-amino acids with one or more stereogenic centers due to st...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802611795164990

    authors: Vogensen SB,Greenwood JR,Bunch L,Clausen RP

    更新日期:2011-01-01 00:00:00

  • Fluorine-18 labeled amino acids for oncologic imaging with positron emission tomography.

    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

    pub_type: 杂志文章,评审

    doi:10.2174/1568026611313080002

    authors: Huang C,McConathy J

    更新日期:2013-01-01 00:00:00

  • Terpyridines and their complexes with first row transition metal ions: cytotoxicity, nuclease activity and self-assembly of biomacromolecules.

    abstract::Transition metal complexes with terpyridine ligands have attracted a widespread interest with respect to biomedical applications: [(tpy)PtCl]Cl and [(tpy)RuCl(3)] are potent anti-tumor agents with activities comparable to those of cisplatin and carboplatin. The Ru(II) complexes feature a high potential as reactive pro...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802612799078919

    authors: Winter A,Gottschaldt M,Newkome GR,Schubert US

    更新日期:2012-01-01 00:00:00

  • Tuberculosis: An Update on Pathophysiology, Molecular Mechanisms of Drug Resistance, Newer Anti-TB Drugs, Treatment Regimens and Host-Di-rected Therapies.

    abstract::The human tuberculosis (TB) is primarily caused by Mycobacterium tuberculosis (Mtb) that inhabits inside and amidst immune cells of the host with adapted physiology to regulate interdependent cellular functions with intact pathogenic potential. The complexity of this disease is attributed to various factors such as th...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1568026621999201211200447

    authors: Borah P,Deb PK,Venugopala KN,Al-Shar'i NA,Singh V,Deka S,Srivastava A,Tiwari V,Mailavaram RP

    更新日期:2020-12-11 00:00:00

  • Rational design of potent and selective VLA-4 inhibitors and their utility in the treatment of asthma.

    abstract::Asthma, a chronic inflammatory disease of the airways, is a significant burden on our healthcare system. There is high unmet need for treatments directed towards the underlying causes of the disease. The cell surface integrin VLA-4 (very late antigen-4; alpha4beta1; CD49d/CD29) plays an important role in the trafficki...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/1568026043387520

    authors: Singh J,Adams S,Carter MB,Cuervo H,Lee WC,Lobb RR,Pepinsky RB,Petter R,Scott D

    更新日期:2004-01-01 00:00:00

  • Practical aspects of NMR-based fragment discovery.

    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

    pub_type: 杂志文章

    doi:10.2174/156802607782341055

    authors: Zartler ER,Mo H

    更新日期:2007-01-01 00:00:00

  • Multi-target-directed ligands as innovative tools to combat trypanosomatid diseases.

    abstract::Of the tropical diseases, trypanosomiases and leishmaniases should most concern the pharmaceutical community because of their high prevalence in developing countries and the lack of effective drug treatments. Despite this, they have not historically received much attention in terms of investment and research effort, n...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章,评审

    doi:10.2174/156802611798184391

    authors: Bolognesi ML

    更新日期:2011-11-01 00:00:00

  • Synthesis of Coumarin Derivatives as Versatile Scaffolds for GSK-3β Enzyme Inhibition.

    abstract:BACKGROUND:Glycogen synthase kinase-3 (GSK-3) is involved in the phosphorylation and inactivation of glycogen synthase. GSK-3 inhibitors have been associated with a variety of diseases, including Alzheimer´s disease (AD), diabetes type II, neurologic disorders, and cancer. The inhibition of GSK-3β isoforms is likely to...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1568026619666191019105349

    authors: Francisco CS,Javarini CL,de S Barcelos I,Morais PAB,de Paula H,de S Borges W,Neto ÁC,Lacerda V

    更新日期:2020-01-01 00:00:00

  • Synthesis, Biological Evaluation and Molecular Docking Studies of Novel Di-hydropyridine Analogs as Potent Antioxidants.

    abstract:AIM:The aim of this study is to synthesize, characterize and biological evaluation of 3-ethyl 5- methyl2-(2-aminoethoxy)-4-(2-chlorophenyl)-1,4-dihydropyridine-3,5-dicarboxylate derivatives. BACKGROUND:An efficient synthesis of two series of novel carbamate and sulfonamide derivatives of amlodipine, 3-ethyl 5-methyl 2...

    journal_title:Current topics in medicinal chemistry

    pub_type: 杂志文章

    doi:10.2174/1568026619666191105100959

    authors: Sudhana SM,Adi PJ

    更新日期:2019-01-01 00:00:00