abstract：:Runx2/Cbfa/AML3 is a member of the runt homology domain family of transcription factors, essential for osteoblast differentiation and bone formation. Defining the molecular mechanisms by which Runx2 can function as a master regulatory gene for activating the program of osteoblastogenesis has provided novel insights fo...

journal_title：Current pharmaceutical design

authors： Lian JB,Stein GS

更新日期：2003-01-01 00:00:00

abstract：:The search for methods to control physiological levels of carbon monoxide (CO), a vasoactive molecule, and bilibrubin, an antioxidant, have improved our understanding of the protective role of heme oxygenase (HO) against oxidative injury. HO activity can assist other antioxidant systems in diminishing the overall prod...

journal_title：Current pharmaceutical design

authors： Abraham NG

更新日期：2003-01-01 00:00:00

abstract：:Ischaemic stroke of the brain accounts for about one third of all deaths in industrialized countries. Many of the patients who survive are severily impaired. Thus, there is an enormous need for pharmacotherapy for the treatment of ischaemic stroke. Why is such a treatment not available yet? Are the pathophysiological ...

journal_title：Current pharmaceutical design

authors： Weiser T

更新日期：2002-01-01 00:00:00

abstract：:Carcinogenesis results from the long-term accumulation of genetic and epigenetic aberrations at the molecular level, which are under constant selection pressure for growth advantage. Recognizing that cancer is the result of this long-term, multi-step process provides opportunities for molecularly targeted cancer preve...

journal_title：Current pharmaceutical design

authors： Anderson WF,Umar A,Viner JL,Hawk ET

更新日期：2002-01-01 00:00:00

abstract：:HIV infection remains incurable although several anti-HIV drugs have been identified and developed. Among these the nucleoside analogues were and remain in the forefront of anti-HIV chemotherapeutic regimens. Most of these nucleoside analogues are modified mainly in the sugar moiety. In general, they lack a free hydro...

journal_title：Current pharmaceutical design

authors： el Kouni MH

更新日期：2002-01-01 00:00:00

abstract：:Pro-rich antimicrobial peptides are a group of linear peptides of innate immunity isolated from mammals and invertebrates, and characterised by a high content of proline residues (up to 50%). Members of this group are predominantly active against Gram-negative bacterial species which they kill by a non-lytic mechanism...

journal_title：Current pharmaceutical design

authors： Gennaro R,Zanetti M,Benincasa M,Podda E,Miani M

更新日期：2002-01-01 00:00:00

abstract：:Estrogens are known as important modulators of development, growth and maintenance of primary sexual physiology. The medical field has also grown increasingly appreciative of the effects of estrogens on non-traditional target tissues such as bone, cardiovascular tissue and the CNS. Postmenopausal women have been the b...

journal_title：Current pharmaceutical design

authors： Miller CP

更新日期：2002-01-01 00:00:00

abstract：:Strontium ranelate is composed of an organic moiety (ranelic acid) and of two atoms of stable non-radioactive strontium. In vitro, strontium ranelate increases collagen and non-collagenic proteins synthesis by mature osteoblast enriched cells. The effects of strontium ranelate on bone formation were confirmed as stron...

journal_title：Current pharmaceutical design

authors： Reginster JY

更新日期：2002-01-01 00:00:00

abstract：:This review describes gene therapy strategies that take advantage of defective signal transduction pathways to selectively kill cancer cells without adversely affecting normal cells. The distinctive features of cancer cells currently exploited by gene therapy include mitosis, cell permissiveness to infection, specific...

journal_title：Current pharmaceutical design

authors： Westphal EM,Melchner Hv Hv

更新日期：2002-01-01 00:00:00

abstract：:Benzodiazepines (BZs) have been widely investigated in terms of clinical efficacy, factors underlying dependence, associated cognitive impairments, and interactions with psychotherapy for anxiety control. However, few studies have systematically considered manner of BZ administration in relation to these variables. St...

journal_title：Current pharmaceutical design

authors： Westra HA,Stewart SH

更新日期：2002-01-01 00:00:00

abstract：:Improvements in our understanding of the intrinsic aberrancies in cancer cells have enabled the design and development of novel therapeutics that specifically target these changes. Among the many complex cellular pathways and mechanisms which have been unveiled by new molecular techniques, RAS-mediated signal transduc...

journal_title：Current pharmaceutical design

authors： Nottage M,Siu LL

更新日期：2002-01-01 00:00:00

abstract：:Aberrant expression of chemokines and their receptors play causative roles in the pathophysiology of numerous autoimmune and inflammatory disease processes. Moreover, an integral step in HIV infection involves binding to chemokine receptors, and hence chemokines are intimately linked to HIV-related diseases. Therefore...

journal_title：Current pharmaceutical design

authors： Rajarathnam K

更新日期：2002-01-01 00:00:00

abstract：:There is an increasing need to rapidly determine the specificity of proteases that potentially play a role in human and animal disease. Substrates for novel proteases can be discovered by testing standard protease substrates such as oxidized insulin B-chain, by screening commercially available substrates for other pro...

journal_title：Current pharmaceutical design

authors： Richardson PL

更新日期：2002-01-01 00:00:00

abstract：:Pyrimidine nucleotides, including UTP, UDP and UDP-glucose, are important signaling molecules which activate G protein-coupled membrane receptors of the P2Y family. Four distinct pyrimidine nucleotide-sensitive P2Y receptor subtypes have been cloned, P2Y(2), P2Y(4), P2Y(6) and P2Y(14). Pharmacological experiments indi...

journal_title：Current pharmaceutical design

authors： Müller CE

更新日期：2002-01-01 00:00:00

abstract：:The antifungal agents for systemic mycoses are only a few in number. Among them amphotericin-B is still the most widely used drug, but substantial side effects including nephrotoxicity limits its clinical usefulness. Efforts to lower the toxicity are synthesis of AMPH-B analogues such as AMPH-B esters and encapsulatio...

journal_title：Current pharmaceutical design

authors： Maesaki S

更新日期：2002-01-01 00:00:00

abstract：:Since ancient times the operation of the brain has elicited more than usual interest. Data mining of the human genome is revealing that many CNS abnormalities have a genetic component. As yet this information can not be used directly to cure or ameliorate specific CNS disorders although this is regarded as having grea...

journal_title：Current pharmaceutical design

authors： Wong MG,Tehan BG,Lloyd EJ

更新日期：2002-01-01 00:00:00

abstract：:Quinone based bioreductive drugs have, potentially, a very versatile use in cancer chemotherapy. They can be activated by DT-diaphorase and hence can be used to target tumour types rich in this (O2)-independent reductase enzyme. Small molecular modifications can substantially reduce specificity for DT-diaphorase and u...

journal_title：Current pharmaceutical design

authors： McNally VA,Patterson AV,Williams KJ,Cowen RL,Stratford IJ,Jaffar M

更新日期：2002-01-01 00:00:00

abstract：:Macrophage migration inhibitory factor (MIF) is a pro-inflammatory cytokine released from T-cells and macrophages, and is a key molecule in inflammation. Although a detailed understanding of the biological functions of MIF has not yet been found, it is known that MIF catalyzes the tautomerization of phenylpyruvate and...

journal_title：Current pharmaceutical design

authors： Orita M,Yamamoto S,Katayama N,Fujita S

更新日期：2002-01-01 00:00:00

abstract：:Ras is a 21 kDa membrane-localized G protein that is coupled to receptor and non-receptor tyrosine kinase activation of downstream cytoplasmic and nuclear events. Mutated ras genes are common, and occur in a wide variety of human malignancies. These activating mutations result in constitutive signaling, thereby stimul...

journal_title：Current pharmaceutical design

authors： Adjei AA

更新日期：2001-11-01 00:00:00

abstract：:This review describes recent advances in the development of DNA-photocleavage agents. Major mechanisms of photosensitized DNA photocleavage are presented and the most popular categories of compounds are considered, which include metal complexes and many organic functional derivatives. DNA-targeted conjugates of photos...

journal_title：Current pharmaceutical design

authors： Da Ros T,Spalluto G,Boutorine AS,Bensasson RV,Prato M

更新日期：2001-11-01 00:00:00

abstract：:In the early 1980s, an "atypical" beta-adrenergic receptor was discovered and subsequently called the beta (3)-adrenoceptor (beta(3)-AR). Agonists of the beta(3)-AR were observed to simultaneously increase lipolysis, fat oxidation, energy expenditure and insulin action leading to the belief that this receptor might se...

journal_title：Current pharmaceutical design

authors： de Souza CJ,Burkey BF

更新日期：2001-09-01 00:00:00

abstract：:The most important glycoproteins of trypanosomatids are anchored by glycoinositolphospholipids (GIPLs) to their plasma membrane. In addition, free GIPLs have been described, for instance the lipopeptidophosphoglycan (LPPG) which is a major component of the surface of T. cruzi epimastigotes. An inositolphosphoceramide ...

journal_title：Current pharmaceutical design

authors： Lederkremer RM,Bertello LE

更新日期：2001-08-01 00:00:00

abstract：:Over the last several years, it has become increasingly clear that dendritic cells (DC) are not only critical for the initiation of T cell immunity, but these cells also determine the course of the subsequent immune response (i.e. tolerance vs. immunity, Th1 vs. Th2). However, the mechanisms by which DC can influence ...

journal_title：Current pharmaceutical design

authors： Wan Y,Bramson J

更新日期：2001-07-01 00:00:00

abstract：:Retinoids (vitamin A and its analogs) exert profound effects on a wide variety of life processes, including morphogenesis and embryonic development. Several retinoids are also effective drugs for therapy of skin diseases and some types of cancer. However, the applicability of this class of compounds is limited by thei...

journal_title：Current pharmaceutical design

authors： Tzimas G,Nau H

更新日期：2001-06-01 00:00:00

abstract：:The pharmacophore concept is central to the rational drug design and discovery process. Traditionally, a pharmacophore is defined as a specific three-dimensional (3D) arrangement of chemical functional groups found in active molecules, which are characteristic of a certain pharmacological class of compounds. Herein, b...

journal_title：Current pharmaceutical design

authors： Tropsha A,Zheng W

更新日期：2001-05-01 00:00:00

abstract：:Osteoblasts pass through a sequence of events controlled by hormones and transcriptional factors ensuring proper development of phenotype and functional properties until the osteoblast enter the osteocyte phenotype and/or undergo apoptosis. During its life cycle, the osteoblasts proliferate, deposit matrix proteins an...

journal_title：Current pharmaceutical design

authors： Gordeladze JO,Reseland JE,Drevon CA

更新日期：2001-03-01 00:00:00

abstract：:Nitric oxide is a ubiquitous molecule involved in a variety of biological processes. The specific action of NO depends on its enzymatic sources namely neuronal nitric oxide synthase (nNOS), endothelial NOS (eNOS) and inducible NOS (iNOS) and all three isoforms have been localized in the gastrointestinal tract. Constit...

journal_title：Current pharmaceutical design

authors： Barrachina MD,Panés J,Esplugues JV

更新日期：2001-01-01 00:00:00

abstract：:The common mechanism of action of aspirin and the chemically unrelated non-steroidal anti-inflammatory drugs (NSAIDs) is the inhibition of prostaglandin (PG) production due to interference with the enzymatic activity of cyclooxygenase (COX). These agents have long been used as effective treatments for arthritis. The r...

journal_title：Current pharmaceutical design

authors： Crofford LJ

更新日期：2000-11-01 00:00:00

abstract：:Helicobacter pylori infection causes progressive damage to gastric mucosa and results in serious disease such as peptic ulcer disease, MALT lymphoma, or gastric adenocarcinoma in 20% to 30% of patients. The current approach is to make a firm diagnosis, give combination antibiotic and antisecretory therapy, and confirm...

journal_title：Current pharmaceutical design

authors： Graham DY,Qureshi WA

更新日期：2000-10-01 00:00:00

abstract：:After years of pre-clinical and clinical testing monoclonal antibodies (mAbs) finally offer new therapeutic choices for patients with haematological and solid malignancies both as unconjugated antibody and as vectors to target radionuclides in radioimmunotherapy (RIT). In recent years some of the most exciting clinica...

journal_title：Current pharmaceutical design

authors： Illidge TM,Brock S

更新日期：2000-09-01 00:00:00

abstract：:In the mid seventies a drug design programme using the Amanita muscaria constituent muscimol (7) as a lead structure, led to the design of guvacine (23) and (R)-nipecotic acid (24) as specific GABA uptake inhibitors and the isomeric compounds isoguvacine (10) and isonipecotic acid (11) as specific GABAA receptor agoni...

journal_title：Current pharmaceutical design

authors： Krogsgaard-Larsen P,Frølund B,Frydenvang K

更新日期：2000-08-01 00:00:00

abstract：:The essential nature of rapid radiotracer synthesis very early in drug discovery programs has driven the need for better and more varied tritium incorporation methods. This review presents a summary of recent advances for tritium introduction via tritiated water, tritium gas, complex tritides, and a range of recently ...

journal_title：Current pharmaceutical design

authors： Saljoughian M,Williams PG

更新日期：2000-07-01 00:00:00

abstract：:In recent years several new drugs (oxcarbazepine, lamotrigine, topiramate, gabapentin, zonisamide, tiagabine, fosphenytoin, vigabatrin and felbamate) have been added to the therapeutic armamentarium against epilepsy. Some of these represent structural modifications of pre-existing compounds, others were developed with...

journal_title：Current pharmaceutical design

authors： Gatti G,Bonomi I,Jannuzzi G,Perucca E

更新日期：2000-05-01 00:00:00

abstract：:The understanding of cytokine networks and the exploitation of these networks for the treatment of immune and inflammatory diseases as well as cancer depend on in vivo delivery of cytokines. Due to instability of recombinant cytokine proteins, investigators have employed cytokine-encoding gene therapy vectors to induc...

journal_title：Current pharmaceutical design

authors： Hitt MM,Gauldie J

更新日期：2000-04-01 00:00:00

abstract：:Angiogenesis is the process by which new blood vessels are formed from preexisting microvasculature. To ensure an adequate blood supply, tumor cells release angiogenic factors that are capable of promoting nearby blood vessels to extend vascular branches to the tumor. In addition, larger tumors have been shown to rele...

journal_title：Current pharmaceutical design

authors： Gourley M,Williamson JS

更新日期：2000-03-01 00:00:00

abstract：:A large body of evidence has accumulated indicating involvement of oxidative stress (OS) in the mode of action of various bioactive substances, including those of the immune system. The data for anticancer drugs (main and miscellaneous) are summarized herein. Although diverse origins pertain, reactive oxygen species (...

journal_title：Current pharmaceutical design

authors： Kovacic P,Osuna JA Jr

更新日期：2000-02-01 00:00:00

abstract：:Cathepsin K, a cysteine protease of the papain family, was identified by sequencing complementary DNA libraries derived from osteoclasts. Cathepsin K can cleave bone proteins such as Type I collagen, osteopontin, and osteonectin. The localization and maturation of cathepsin K in activated osteoclasts have been charact...

journal_title：Current pharmaceutical design

authors： Yamashita DS,Dodds RA

更新日期：2000-01-01 00:00:00

abstract：:Adenosine is released in large amounts during myocardial ischemia and is capable of exerting potent cardioprotective effects in the heart. Although these observations on adenosine have been known for a long time, how adenosine acts to achieve its anti-ischemic effect remains incompletely understood. However, recent ad...

journal_title：Current pharmaceutical design

authors： Liang BT,Jacobson KA

更新日期：1999-12-01 00:00:00

abstract：:Somatostatin is a tetradeca peptide hormone produced by many different endocrine cells throughout the body. It is also present in both the central and peripheral nervous system. The peptide has many different moods of action including inhibition of hormone secretion and influence on gastrointestinal motility. Somatost...

journal_title：Current pharmaceutical design

authors： Janson ET,Oberg K

更新日期：1999-09-01 00:00:00

abstract：:The acidic amino acid L-glutamate acts as both a primary excitatory neurotransmitter and a potential neurotoxin within the mammalian central nervous system. Functionally juxtaposed between these neurophysiological and pathological actions are an assorted group of integral membrane transporter proteins that rapidly and...

journal_title：Current pharmaceutical design

authors： Bridges RJ,Kavanaugh MP,Chamberlin AR

更新日期：1999-05-01 00:00:00