abstract：:Modification of cysteine (Cys) residues in proteins, due to (i) the participation of the thiol moiety of this amino acid in oxido-reductions reactions; (ii) its ability to strongly coordinate transition metal ions; or (iii) its nucleophilic nature and facile reaction with electrophiles, may be of critical importance f...

journal_title：Current medicinal chemistry

authors： Scozzafava A,Casini A,Supuran CT

更新日期：2002-06-01 00:00:00

abstract：:Benzamide riboside (BR) after anabolism to an analogue of NAD, was shown to inhibit the activity of NAD-dependent enzymes such as inosine 5'-monophosphate dehydrogenase (IMPDH), the rate limiting enzyme in de novo guanylate biosynthesis, and malate dehydrogenase which is involved in the citric cycle and respiratory ch...

journal_title：Current medicinal chemistry

authors： Polgar D,Gfatter S,Uhl M,Kassie F,Leisser C,Krupitza G,Grusch M

更新日期：2002-04-01 00:00:00

abstract：:Non-small cell lung cancer (NSCLC) remains a fatal disease: the majority of patients are diagnosed as having metastases or advanced inoperable tumors. The activity of chemotherapy in NSCLC patients is low with objective response rarely complete and sustained. Cisplatin-based combinations are considered as the standard...

journal_title：Current medicinal chemistry

authors： Gridelli C,De Vivo R

更新日期：2002-04-01 00:00:00

abstract：:The discovery of anandamide as an endogenous ligand for the cannabinoid receptors has led to a resurgence of interest in the fatty acid amides. However, N-palmitoylethanolamine (PEA), a shorter and fully saturated analogue of anandamide, has been known since the fifties. This endogenous compound is a member of the N-a...

journal_title：Current medicinal chemistry

authors： Lambert DM,Vandevoorde S,Jonsson KO,Fowler CJ

更新日期：2002-03-01 00:00:00

abstract：:Serotonin (5-hydroxytryptamine, 5-HT) is one of the most attractive targets for medicinal chemists. Among 5-HTRs, the 5-HT(1A) subtype is the best studied and it is generally accepted that it is involved in psychiatric disorders such as anxiety and depression. Several structurally different compounds are known to bind...

journal_title：Current medicinal chemistry

authors： López-Rodríguez ML,Ayala D,Benhamú B,Morcillo MJ,Viso A

更新日期：2002-02-01 00:00:00

abstract：:Potent enzyme inhibitors have long been recognized as powerful tools for assessing the physiological roles of enzymes and have led to the therapeutic drugs able to modulate their activities in vivo. However, to be valuable tools such inhibitors should be selective so that they do not interfere with other members of th...

journal_title：Current medicinal chemistry

authors： Batra S,Srinivasan T,Rastogi SK,Kundu B

更新日期：2002-02-01 00:00:00

abstract：:In the human brain several cell types are capable of initiating and amplifying a brain specific inflammatory response involving the synthesis of cytokines, prostaglandins and oxygen free radicals. In Alzheimer's disease (AD), signs of an inflammatory activation of microglia and astroglia are present inside and outside...

journal_title：Current medicinal chemistry

authors： Hüll M,Lieb K,Fiebich BL

更新日期：2002-01-01 00:00:00

abstract：:Complete DNA sequence information has now been obtained for several prokaryotic genomes, defining the entire genetic complement of these organisms. The collection of genomic data has provided new insights into the molecular architecture of bacterial cells, revealing the basic genetic and metabolic structures that supp...

journal_title：Current medicinal chemistry

authors： Buysse JM

更新日期：2001-12-01 00:00:00

abstract：:Polycyclic aromatic hydrocarbons (PAH) are considered potentially carcinogenic. Substituted PAH derivatives, in contrast, may serve as anticancer agents, and as chemotherapeutics. This article presents a review of their use. Particular emphasis is placed on the synthesis of these new compounds, electrophilic substitut...

journal_title：Current medicinal chemistry

authors： Banik BK,Becker FF

更新日期：2001-10-01 00:00:00

abstract：:The oxime formation reaction of therapeutical progestogen (levonorgestrel, levonorgestrel acetate, norethisterone), androgen (methyltestosterone, testosterone phenylpropionate) and anabolic (nortestosterone phenylpropionate) Delta(4)-3-ketosteroids has been investigated. The ketosteroid-hydroxylamine reaction was moni...

journal_title：Current medicinal chemistry

authors： Szentesi A,Gergely A,Horváth P,Mahó S,Mátyus P,Szász G

更新日期：2001-09-01 00:00:00

abstract：:Perceiving a pharmacophore is the first essential step towards understanding the interaction between a receptor and a ligand. Once a pharmacophore is established, a beneficial use of it is 3D database searching to retrieve novel compounds that would match the pharmacophore, without necessarily duplicating the topologi...

journal_title：Current medicinal chemistry

authors： Kurogi Y,Güner OF

更新日期：2001-07-01 00:00:00

abstract：:Combination therapy in the treatment of viral infections in which, for example, three different drugs against three different targets on three independent proteins are administered, has been highly successful clinically. However, it is only a matter of time before a virus will arise resistant to all three drugs, becau...

journal_title：Current medicinal chemistry

authors： Mangel WF,McGrath WJ,Brown MT,Baniecki ML,Barnard DL,Pang YP

更新日期：2001-07-01 00:00:00

abstract：:In order to ascertain the role of dietary flavonoids as antioxidants in vivo it is necessary to understand the chemical nature of the absorbed forms in the circulation in vivo and how the multiplicity of research findings in vitro reflect the bioactivity of flavonoids in vivo. Only when we gain adequate information on...

journal_title：Current medicinal chemistry

authors： Rice-Evans C

更新日期：2001-06-01 00:00:00

abstract：:The polystyrene-based 2-chlorotrityl resin was originally used in the synthesis of peptides using an Fmoc-amino acid/carboxyl-linked protocol. While traditionally employed to prepare a number of biologically active peptides, the resin has received increasing attention as a support for the synthesis of pseudopeptide an...

journal_title：Current medicinal chemistry

authors： Hoekstra WJ

更新日期：2001-05-01 00:00:00

abstract：:Recent work on a number of different classes of anticancer agents that alkylate DNA in the minor groove is reviewed. There has been much work with nitrogen mustards, where attachment of the mustard unit to carrier molecules can change the normal patterns of both regio- and sequence-selectivity, from reaction primarily...

journal_title：Current medicinal chemistry

authors： Denny WA

更新日期：2001-04-01 00:00:00

abstract：:The reductive conversion of ribonucleotides to deoxyribonucleotides by ribonucleotide reductase (RR) is a crucial and rate-controlling step in the pathway leading to the biosynthesis of DNA, since deoxyribonucleotides are present in extremely low levels in mammalian cells. Mammalian ribonucleotide reductase (RR) is co...

journal_title：Current medicinal chemistry

authors： Li J,Zheng LM,King I,Doyle TW,Chen SH

更新日期：2001-02-01 00:00:00

abstract：:Tetracyclines (TCs) and their non-antimicrobial analogs (CMTs) have therapeutic potential to inhibit tissue destructive disease processes, such as cancer invasion and metastasis, by inhibiting certain matrix metalloproteinases. Enhanced matrix metalloproteinase-2 (MMP-2; gelatinase A) activity has been correlated to c...

journal_title：Current medicinal chemistry

authors： Lee HM,Golub LM,Cao J,Teronen O,Laitinen M,Salo T,Zucker S,Sorsa T

更新日期：2001-02-01 00:00:00

abstract：:Cellular resistance to anthracyclines is a major limitation of their clinical use in the treatment of human tumors. Resistance to doxorubicin is described as a multifactorial phenomenon involving the overexpression of defense factors and alterations in drug-target interactions. Such changes do not account for all mani...

journal_title：Current medicinal chemistry

authors： Perego P,Corna E,De Cesare M,Gatti L,Polizzi D,Pratesi G,Supino R,Zunino F

更新日期：2001-01-01 00:00:00

abstract：:Radical induced oxidative damage is extremely harmful to tissues and organs due to molecular modifications brought to polyunsaturated membrane lipids, proteins and nucleic acids. Oxidative stress is believed to be one of the pathophysiological mechanisms that operate in neurodegenerative disorders such as cerebral isc...

journal_title：Current medicinal chemistry

authors： Goldstein S,Lestage P

更新日期：2000-12-01 00:00:00

abstract：:The identification and characterisation of the isoenzyme cyclooxygenase 2 (COX-2) stimulated investigations to develop efficient non-steroidal anti-inflammatory drugs with reduced side effects compared to standard NSAIDs. This review will focus on the structural features needed to achieve COX-2 selectivity. Five struc...

journal_title：Current medicinal chemistry

authors： Dannhardt G,Laufer S

更新日期：2000-11-01 00:00:00

abstract：:Current strategies in pharmaceutical research comprise two methodologically different but complementary approaches for lead finding purposes, namely the random screening of compound libraries and the structure-based effort, commonly termed rational drug design. The structure-based approach is aimed to exploit 3D struc...

journal_title：Current medicinal chemistry

authors： Müller G

更新日期：2000-09-01 00:00:00

abstract：:Advances in combinatorial chemistry, high-throughput screening, and molecular modeling have revolutionized the process of drug discovery in the pharmaceutical industry. Drug discovery efforts for the primary protozoal parasitic diseases of the developing world, malaria, leishmaniasis, and trypanosomiasis, have also be...

journal_title：Current medicinal chemistry

authors： Werbovetz KA

更新日期：2000-08-01 00:00:00

abstract：:This review summarizes our knowledge of biochemical, biological and medical applications and properties of phosphinic acid compounds. Phosphinic acid compounds (phosphinates) are derivatives of phosphinic acid H2P(O)(OH). The major attention of this article is focused on applications of phosphinates of a pseudopeptide...

journal_title：Current medicinal chemistry

authors： Collinsová M,Jirácek J

更新日期：2000-06-01 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：:The development of new drugs with potential therapeutic applications is one of the most complex and difficult process in the pharmaceutical industry. Millions of dollars and man-hours are devoted to the discovery of new therapeutical agents. As, the activity of a drug is the result of a multitude of factors such as bi...

journal_title：Current medicinal chemistry

authors： Ooms F

更新日期：2000-02-01 00:00:00

abstract：:Glucagon-like peptide-1 (GLP-1) is an insulinotropic hormone secreted from endocrine cells in the gut mucosa in response to meal ingestion. It is an important incretin hormone; mice with a null mutation in the GLP-1 receptor gene develop glucose intolerance. In addition, it inhibits gastrointestinal secretion and moti...

journal_title：Current medicinal chemistry

authors： Holst JJ

更新日期：1999-11-01 00:00:00

abstract：:Palmitoylethanolamide (PEA) and oleamide are two fatty acid amides which 1) share some cannabimimetic actions with delta9-tetrahydrocannabinol, anandamide and 2-arachidonoylglycerol, and 2) may interact with proteins involved in the biosynthesis, action and inactivation of endocannabinoids. Due to its pharmacological ...

journal_title：Current medicinal chemistry

authors： Lambert DM,Di Marzo V

更新日期：1999-08-01 00:00:00

abstract：:Inosine monophosphate dehydrogenase (IMPDH) catalyzes the conversion of IMP to XMP with the concomitant reduction of NAD to NADH. This reaction is the rate-limiting step in guanine nucleotide biosynthesis. IMPDH is a proven target for immunosuppressive, anticancer and antiviral chemotherapy, and may also be a target f...

journal_title：Current medicinal chemistry

authors： Hedstrom L

更新日期：1999-07-01 00:00:00

abstract：:Agents modulating apoptosis are of extraordinary promise for the treatment of several states of disease including cancer, AIDS, neurodegenerative and ischemic diseases. In this review a brief summary of cellular pathways relevant to programmed cell death first is given and potential therapeutic targets therein are emp...

journal_title：Current medicinal chemistry

authors： Deigner HP,Kinscherf R

更新日期：1999-05-01 00:00:00

abstract：:More than five decades since the Discovery of Penicillin, the chemistry and biological activity of b-lactams continue to attract the wide spread attention of research workers. Owing to high efficacy and extremely safe toxicological profile, they are agents of choice in the current therapeutic index for the bacterial i...

journal_title：Current medicinal chemistry

authors： Kidwai M,Sapra P,Bhushan KR

更新日期：1999-03-01 00:00:00

abstract：:The synthesis and biological evaluation of carbohydrate mimetics has begun to more clearly define the diverse roles of carbohydrates in nature. Often the strategy invoves the design and synthesis of glycosyltransferase and glycosidase inhibitors both as tools to elucidate the mechanism of action of these enzymes and a...

journal_title：Current medicinal chemistry

authors： Elhalabi JM,Rice KG

更新日期：1999-02-01 00:00:00

abstract：:The biological relevance of sulfur containing carbohydrates is gaining substantial attention. Thus the new developments, especially in the synthetic and medicinal chemistry of thio-sugars are critically important for carbohydrate drug design. New studies of biological processes including biosynthetic reactions and enz...

journal_title：Current medicinal chemistry

authors： Witczak ZJ

更新日期：1999-02-01 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：:Fluoxetine is an antidepressant drug, a potent and specific inhibitor of serotonin reuptake (SSRI). Evidence suggests that being compared with tricyclic antidepressants, fluoxetine may cause significantly fewer anticholinergic, antihistaminergic and cardiotoxic side effects in the treatment of major depressive disorde...

journal_title：Current medicinal chemistry

authors： Pacher P,Ungvari Z,Kecskemeti V,Furst S

更新日期：1998-10-01 00:00:00

abstract：:Thalidomide (N-alpha-phthalimidoglutarimide) was used widely as a hypnotic/sedative agent in the late 1950s and the early 1960s, but had to be withdrawn from the market because of its severe teratogenicity. In spite of this, there has been a resurgence of interest in the drug in recent years due to its potential usefu...

journal_title：Current medicinal chemistry

authors： Hashimoto Y

更新日期：1998-06-01 00:00:00