The structure and pharmacological functions of coumarins and their derivatives.

abstract：:Matrix metalloproteinases (MMPs) are essential for the degradation and turnover of components of the extracellular matrix (ECM) and, when pathologically elevated, mediate connective tissue loss (including bone destruction) in various inflammatory and other diseases. Tetracyclines (TCs) are known inhibitors of mammalia...

journal_title：Current medicinal chemistry

authors： Zhang Y,Gu Y,Lee HM,Hambardjieva E,Vranková K,Golub LM,Johnson F

更新日期：2012-01-01 00:00:00

abstract：:Glutamate carboxypeptidase II (GCPII) and its splice variants, paralogs and human homologs represent a family of proteins with diverse tissue distribution, cellular localization and largely unknown function which have been explored only recently. While GCPII itself has been thoroughly studied from different perspectiv...

journal_title：Current medicinal chemistry

authors： Hlouchová K,Navrátil V,Tykvart J,Sácha P,Konvalinka J

更新日期：2012-01-01 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：:Mitochondria are cytoplasmic double-membraned organelles that are involved in a myriad of key cellular regulatory processes. The loss of mitochondrial function is related to the pathogenesis of several human diseases. Over the last decades, an increasing number of studies have shown that dietary polyphenols can regula...

journal_title：Current medicinal chemistry

authors： Teixeira J,Chavarria D,Borges F,Wojtczak L,Wieckowski MR,Karkucinska-Wieckowska A,Oliveira PJ

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:Nonalcoholic fatty liver disease (NAFLD), the most common chronic liver disease, is the leading cause of cryptogenic cirrhosis and has consistently been implicated in related metabolic disorders, such as dyslipidemia and type 2 diabetes (T2D). However, the pathogenesis of NAFLD remains to be elucidated, and ...

journal_title：Current medicinal chemistry

authors： Xu G,Huang K,Zhou J

更新日期：2018-01-01 00:00:00

abstract：:The market, sales and regulatory approval of new human medicines, during the past few years, indicates increasing number and share of new biologics and emergence of new multibillion dollar molecules. The global sale of monoclonal antibodies in 2006 were $20.6 billion. Remicade had annual sales gain of $1 billion durin...

journal_title：Current medicinal chemistry

authors： Maggon K

更新日期：2007-01-01 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：:The existence of functional NT/dopamine interactions in the central nervous system has been extensively documented. Among others, a possible molecular mechanism underlying the NT-induced modulation of dopamine release is a direct antagonistic NTS(1)/D(2) receptor interaction. More recently, neurochemical experiments a...

journal_title：Current medicinal chemistry

authors： Tanganelli S,Antonelli T,Tomasini MC,Beggiato S,Fuxe K,Ferraro L

更新日期：2012-01-01 00:00:00

abstract：:The alphavbeta3 receptor, which are members of the group of the cellular adhesion molecules (CAM), are heterodimeric transmembrane glycoprotein receptors involved in processes such as cell-cell and cell-matrix adhesion, cell migration and signaling. Integrin alphavbeta3 receptor is expressed on almost all cells origin...

journal_title：Current medicinal chemistry

authors： Cacciari B,Spalluto G

更新日期：2005-01-01 00:00:00

abstract：:Bone pain arising from secondary skeletal malignancy constitutes one of the most common types of chronic pain among patients with cancer which can lead to rapid deterioration of the quality of life. Radionuclide therapy using bone-seeking radiopharmaceuticals based on the concept of localization of the agent at bone m...

journal_title：Current medicinal chemistry

authors： Dash A,Das T,Knapp FFR

更新日期：2020-01-01 00:00:00

abstract：:COX-2, a key enzyme that catalyzed the rate-limiting steps in the conversion of arachidonic acid to prostaglandins, played a pivotal role in inflammatory process. Different from other family members, COX-2 was barely detectable in normal physiological conditions and highly inducible during acute inflammatory response ...

journal_title：Current medicinal chemistry

authors： Cui J,Jia J

更新日期：2020-09-17 00:00:00

abstract：:Deregulation of kinase function has been implicated in several important diseases, including cancer, neurological and metabolic disorders. Because of their key role in causing disease, kinases have become one of the most intensively pursued classes of drug targets. To date, several monoclonal antibodies (mAbs) and sma...

journal_title：Current medicinal chemistry

authors： Cerchia L,de Franciscis V

更新日期：2011-01-01 00:00:00

abstract：:The new drug class of dipeptidyl peptidase-4 (DPP4) inhibitors has been widely accepted in the daily management of type 2 diabetes since its strategic advantages with regard to body weight, risk of hypoglycaemia, and beta cell survival. We have previously evaluated the theoretical implications of DPP4 inhibition given...

journal_title：Current medicinal chemistry

authors： Matteucci E,Giampietro O

更新日期：2011-01-01 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：:Functioning of G protein-coupled receptors (GPCRs) is tightly linked to the membrane environment, but a molecular level understanding of the modulation of GPCR by membrane lipids is not available. However, specific receptor-lipid interactions as well as unspecific effects mediated by the bulk properties of the membran...

journal_title：Current medicinal chemistry

authors： Sadiq SK,Guixa-Gonzalez R,Dainese E,Pastor M,De Fabritiis G,Selent J

更新日期：2013-01-01 00:00:00

abstract：:Low molecular weight oligonucleotides have been discovered to have potential use for gene therapy by selectively inhibiting the expression of certain genes. Chemical conjugation of functional peptides to oligonucleotides can introduce desired properties to the oligonucleotides, such as cell-specific delivery, cellular...

journal_title：Current medicinal chemistry

authors： Wang CF,Auriola S,Hirvonen J,Santos HA

更新日期：2014-04-01 00:00:00

abstract：:To date, many scientific attempts have been directed towards the development of experimental models for the identification of neuronal mechanisms evoking cardiovascular and hemodynamic dysfunctions. The spontaneously hypertensive rat (SHR), a genetic model of essential hypertension, has become a valuable rodent for th...

journal_title：Current medicinal chemistry

authors： Giusi G,Alò R,Avolio E,Zizza M,Facciolo RM,Talani G,Biggio G,Sanna E,Canonaco M

更新日期：2012-01-01 00:00:00

abstract：:Over the last decade there has been significant progress in understanding the molecular basis of disease processes. At the same time the technological advances in the area of genomics and the efforts in proteomics research have increased the possibility of discovering many proteins with defined therapeutic functions. ...

journal_title：Current medicinal chemistry

authors： Platis D,Labrou NE

更新日期：2008-01-01 00:00:00

abstract：:Active pharmaceutical ingredients (APIs), frequently delivered to the patient in the solid-state as part of an approved dosage form, can exist in such diverse solid forms as polymorphs, pseudopolymorphs, salts, co-crystals and amorphous solids. Various solid forms often display different mechanical, thermal, physical ...

journal_title：Current medicinal chemistry

authors： Lu J,Rohani S

更新日期：2009-01-01 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：:Correct QSAR analysis requires reliable measured or calculated logP values, being logP the most frequently utilized and most important physico-chemical parameter in such studies. Since the publication of theoretical fundamentals of logP prediction, many commercial software solutions are available. These programs are a...

journal_title：Current medicinal chemistry

authors： Eros D,Kövesdi I,Orfi L,Takács-Novák K,Acsády G,Kéri G

更新日期：2002-10-01 00:00:00

abstract：:Reversible phosphorylation is a key mechanism for regulating the biological activity of many human proteins that affect a diverse array of cellular processes, including protein-protein interactions, gene transcription, cell-cycle progression and apoptosis. Once viewed as simple house keeping enzymes, recent studies ha...

journal_title：Current medicinal chemistry

authors： Honkanen RE,Golden T

更新日期：2002-11-01 00:00:00

abstract：:Since photodynamic therapy emerged as a promising cancer treatment, the development of photosensitizers has gained great interest. In this context, the photosynthetic pigments, chlorophylls and bacteriochlorophylls, as excellent natural photosensitizers, attracted much attention. In effect, several (bacterio) chloroph...

journal_title：Current medicinal chemistry

authors： Staron J,Boron B,Karcz D,Szczygieł M,Fiedor L

更新日期：2015-01-01 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：:The bi-aryl urea multi-kinase inhibitor Sorafenib (BAY 43-9006, Nexavar) was initially approved for the treatment of unresectable hepatocellular carcinoma and advanced renal cell carcinoma. Eleven years after its first description in PubMed, the therapeutic potential of Sorafenib has been evaluated in an increasing nu...

journal_title：Current medicinal chemistry

authors： Zauli G,Voltan R,Tisato V,Secchiero P

更新日期：2012-01-01 00:00:00

abstract：:Paediatric Acquired ImmunoDeficiency Syndrome (AIDS) is a life-threatening and infectious disease in which the Human Immunodeficiency Virus (HIV) is mainly transmitted through Mother-To- Child Transmission (MTCT) during pregnancy, labour and delivery, or breastfeeding. This review provides an overview of the distinct ...

journal_title：Current medicinal chemistry

authors： Melo R,Lemos A,Preto AJ,Bueschbell B,Matos-Filipe P,Barreto C,Almeida JG,Silva RDM,Correia JDG,Moreira IS

更新日期：2020-01-01 00:00:00

abstract：:Osteoporosis is a pathological loss of bone mass due to an imbalance in bone remodeling where osteoclast-mediated bone resorption exceeds osteoblast-mediated bone formation resulting in skeletal fragility and fractures. Anti-resorptive agents such as bisphosphonates and SERMs, and anabolic drugs that stimulate bone fo...

journal_title：Current medicinal chemistry

authors： Li H,Xiao Z,Quarles LD,Li W

更新日期：2020-03-30 00:00:00

abstract：:alpha-Galactosylceramide (alpha-GalCer), is a glycolipid which has been identified as a ligand recognized by a special group of immune T cells, known as invariant NKT cells. alpha-GalCer can powerfully activate invariant NKT cells to produce immunoregulatory cytokines, including interferon-gamma and IL-4, and thereby ...

journal_title：Current medicinal chemistry

authors： Hayakawa Y,Godfrey DI,Smyth MJ

更新日期：2004-01-01 00:00:00

abstract：:Although the renin-angiotensin system (RAS) is already an old acquaintance, there are often exciting discoveries that improve our knowledge of it and open new therapeutic possibilities. Moreover, well-established drugs, such as angiotensin-converting enzyme inhibitors (ACEI), angiotensin receptor blockers (ARB), or be...

journal_title：Current medicinal chemistry

authors： Ramírez-Sánchez M,Prieto I,Wangensteen R,Banegas I,Segarra AB,Villarejo AB,Vives F,Cobo J,de Gasparo M

更新日期：2013-01-01 00:00:00

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