Progress towards the discovery of orally active thrombin inhibitors.

abstract：:Breast cancer arises in about 48% of patients older than 65 years and more than 30% occurs in those over 70 years being the leading cause of cancer-related death in women older than 65. Elderly patients tolerate chemotherapy poorly compared to their younger counterpart because of progressive reduction of organ functio...

journal_title：Current medicinal chemistry

authors： Rossi A,Colantuoni G,Maione P,Ferrara C,Airoma G,Barzelloni ML,Castaldo V,Gridelli C

更新日期：2005-01-01 00:00:00

abstract：:Bicarbonate (HCO₃⁻) membrane transport systems are crucial players in the physiology of several tissues. The molecular basis of HCO₃⁻ membrane transport is of major physiological relevance since this ion is involved in the establishment of intracellular and extracellular ionic composition, osmolariy and pH. The membra...

journal_title：Current medicinal chemistry

authors： Bernardino RL,Jesus TT,Martins AD,Sousa M,Barros A,Cavaco JE,Socorro S,Alves MG,Oliveira PF

更新日期：2013-01-01 00:00:00

abstract：:Chronic Obstructive Pulmonary Disease (COPD) is a progressive respiratory disorder characterized by irreversible chronic inflammation and airflow obstruction. It affects more than 64 million patients worldwide and it is predicted to become the third cause of death in the industrialized world by 2030. Currently availab...

journal_title：Current medicinal chemistry

authors： Pirozzi F,Ren K,Murabito A,Ghigo A

更新日期：2019-01-01 00:00:00

abstract：:In the hit to lead process, a drug candidate is selected from a set of potential leads by screening its binding with potential targets. This review focuses on the lead identification assays that employ a bio-chemical or bio-physical test to detect molecular recognition events between proteins and small molecules in a ...

journal_title：Current medicinal chemistry

authors： Bergese P,Cretich M,Oldani C,Oliviero G,Di Carlo G,Depero LE,Chiari M

更新日期：2008-01-01 00:00:00

abstract：:Fabry disease (FD) is an X-linked glycosphingolipid storage disorder caused by deficient activity of the lysosomal enzyme alpha-galactosidase A. This leads to a progressive accumulation of globotriaosylceramide (Gb3) in the lysosomes of different cells and tissues, causing principally ventricular hypertrophy, renal fa...

journal_title：Current medicinal chemistry

authors： Caballero L,Climent V,Hernández-Romero D,Quintanilla MA,de la Morena G,Marín F

更新日期：2010-01-01 00:00:00

abstract：:APN is an important zinc dependent metallo-exopeptidase; it has been considered as a suitable target for anti-cancer drug design. In this review we focus on the most effective and the most promising inhibitors of aminopeptidase N. Their binding modes to the enzyme, the attempt to explain the origin of the inhibitory a...

journal_title：Current medicinal chemistry

authors： Zhang X,Xu W

更新日期：2008-01-01 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：:Characterization of liver-specific autoantigens has given a fresh impetus to research in the pathogenesis of autoimmune liver diseases, viral-triggered and drug-induced autoimmunity affecting the liver. Intriguing is the fact that most of the liver-specific autoantigens are enzymes of key importance for cell's homeost...

journal_title：Current medicinal chemistry

authors： Bogdanos DP,Dalekos GN

更新日期：2008-01-01 00:00:00

abstract：:Polycystic ovary syndrome (PCOS) is the most common endocrine and metabolic disorder affecting women in reproductive age. Although the etiology of PCOS remains unclear, it is believed to result from genetic, environmental and behavioral interactions. Women with PCOS have higher lifetime risk for cardiovascular disease...

journal_title：Current medicinal chemistry

authors： Vélez LM,Motta AB

更新日期：2014-01-01 00:00:00

abstract：:It is well accepted that inflammatory bowel disease (IBD), including ulcerative colitis and Crohn's disease, is one of high risk factors for colorectal cancer (CRC). This supports the notion that inflammation plays a key role in cancer development. Epidemiologic studies have shown that vitamin D (Vit D) deficiency is ...

journal_title：Current medicinal chemistry

authors： Luan Z,Ma Y,Xin Y,Qian J,Wang H

更新日期：2017-01-01 00:00:00

abstract：:Chymase stored in mast cells activates matrix metalloproteinase (MMP)-9, which may relate to the progression of sinusoidal obstruction syndrome (SOS). We investigated the preventive effect of a chymase inhibitor, TY-51469, on monocrotaline-induced SOS in hamsters. Hamsters were orally administrated with a single dose ...

journal_title：Current medicinal chemistry

authors： Masubuchi S,Komeda K,Takai S,Jin D,Tashiro K,Li ZL,Otsuki Y,Okamura H,Hayashi M,Uchiyama K

更新日期：2013-01-01 00:00:00

abstract：:The discovery of cannabinoid receptors at the beginning of the 1990s, CB1 cloned in 1990 and CB2 cloned in 1993, and the availability of selective and potent cannabimimetics could only be justified by the existence of endogenous ligands that are capable of binding to them. Thus, the characterisation and cloning of the...

journal_title：Current medicinal chemistry

authors： Páez JA,Campillo NE

更新日期：2019-01-01 00:00:00

abstract：BACKGROUND:During lead identification and optimization, the advancement criteria may be driven based on scientific principles, prior experiences, and/or by examining the path paved by approved drugs. However, accessing the discovery data on physicochemical and ADME properties of the approved kinase inhibitors is a monu...

journal_title：Current medicinal chemistry

authors： O Brien Z,Moghaddam MF

更新日期：2017-01-01 00:00:00

abstract：:Thymosin Beta-4 (Tβ4) is known as a major pleiotropic actin-sequestering protein that is involved in tumorigenesis. Tβ4 is a water-soluble protein that has different promising clinical applications in the remodeling and ulcerated tissues repair following myocardial infarction, stroke, plasticity and neurovascular remo...

journal_title：Current medicinal chemistry

authors： Bjørklund G,Dadar M,Aaseth J,Chirumbolo S

更新日期：2020-01-01 00:00:00

abstract：:The immunophilin ligands cyclosporin A, FK506 and rapamycin are best known for their immunosuppressive properties and their clinical use in transplantation medicine. These compounds or their analogs are also clinically used or investigated in various types of cancer, coronary angioplasty, dermatology, hepatitis C infe...

journal_title：Current medicinal chemistry

authors： Gaali S,Gopalakrishnan R,Wang Y,Kozany C,Hausch F

更新日期：2011-01-01 00:00:00

abstract：:Histone deacetylase inhibitors have generated significant interest as anti-cancer agents due to their ability to cause growth arrest, terminal differentiation and/ or apoptosis in carcinoma cells. Abbott entered this area after the serendipitous discovery of the biaryl hydroxamate A-161906 in a TGF beta mimetic screen...

journal_title：Current medicinal chemistry

authors： Curtin M,Glaser K

更新日期：2003-11-01 00:00:00

abstract：:Protein kinase B/AKT plays a central role in cancer. The serine/threonine kinase is overexpressed or constitutively active in many cancers and has been validated as a therapeutic target for cancer treatment. However, targeting the kinase activity has revealed itself to be a challenge due to non-selectivity of the comp...

journal_title：Current medicinal chemistry

authors： Meuillet EJ

更新日期：2011-01-01 00:00:00

abstract：:Giving a glance to the report of Wound Care Market by Product updated in 2017, we can see that wound care market is expected to reach USD 22.01 billion by 2022 from USD 18.35 billion at a CAGR of 3.7%. Numerous factors are driving the growth of this market, including the increasing prevalence of chronic wounds and acu...

journal_title：Current medicinal chemistry

authors： Polerà N,Badolato M,Perri F,Carullo G,Aiello F

更新日期：2019-01-01 00:00:00

abstract：:Over the past few years, use of the genome-wide association study (GWAS) has made it possible to identify the primary genetic mechanisms of essential hypertension. GWAS results have helped identify many loci in or near genes that generally were not expected to be associated with blood pressure or essential hypertensio...

journal_title：Current medicinal chemistry

authors： Pan S,Naruse H,Nakayama T

更新日期：2015-01-01 00:00:00

abstract：:Cell products are live cells that are given to patients in order to replace or modify the function of missing or dysfunctional cells. Progress in technology and in the understanding of pathobiology may lead to the use of cell products in many areas. This review outlines the use of cell products in the treatment of aut...

journal_title：Current medicinal chemistry

authors： Ernerudh J,Berlin G,Ekerfelt C

更新日期：2002-08-01 00:00:00

abstract：:The main challenge of cancer treatment is multidrug resistance during chemotherapy. Cancer cell can evade cell death during every round of orthodox chemotherapy drugs, consequently being resistant after several rounds of standard drug treatment. One of the regimens to address this multidrug resistance problem is by dr...

journal_title：Current medicinal chemistry

authors： Lou JS,Yao P,Tsim KWK

更新日期：2018-01-01 00:00:00

abstract：BACKGROUND:The therapeutic properties of cannabinoids are well-known since ancient years. Growing evidence exist on endocannabinoid system (ECS) modulation related with human tumorigenesis. OBJECTIVE:Taking into account the substantial role of ECS on immune cell regulation, the present review is aimed to summarize the...

journal_title：Current medicinal chemistry

authors： Giaginis C,Lakiotaki E,Korkolopoulou P,Konstantopoulos K,Patsouris E,Theocharis S

更新日期：2016-01-01 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：:Patients with peripheral arterial disease (PAD) suffer from increased cardiovascular morbidity and mortality. The ankle brachial index has been widely used as an easy tool to identify and stratify patients with PAD, however its predictive value remains limited. Higher levels of inflammatory and prothrombotic biomarker...

journal_title：Current medicinal chemistry

authors： Charakida M,Masi S,Tousoulis D

更新日期：2012-01-01 00:00:00

abstract：:Adenosine is an important autocoid, exerting its physiological effects on the human body by activation of four different G-protein-coupled-receptors (GPCRs) classified as A(1), A(2A), A(2B), and A(3). These receptors are coupled to secondary messenger systems including adenylate cyclase, inositol phosphate metabolism,...

journal_title：Current medicinal chemistry

authors： Romagnoli R,Baraldi PG,Tabrizi MA,Gessi S,Borea PA,Merighi S

更新日期：2010-01-01 00:00:00

abstract：:Although resin-based chemistry offers many practical advantages over conventional solution phase for the synthesis of combinatorial libraries, effective monitoring of reactions conducted on the support remains a challenge. A number of techniques have been developed to enable the analysis of solid phase organic synthes...

journal_title：Current medicinal chemistry

authors： Scicinski JJ,Congreveb MS,Kay C,Ley SV

更新日期：2002-12-01 00:00:00

abstract：:It is well-recognized that the majority of cancer-related deaths is attributed to metastasis, which can arise from virtually any type of tumor. Metastasis is a complex multistep process wherein cancer cells must break away from the primary tumor, intravasate into the circulatory or lymphatic systems, extravasate, prol...

journal_title：Current medicinal chemistry

authors： Wong KM,Song J,Saini V,Wong YH

更新日期：2019-01-01 00:00:00

abstract：:There is a need for novel drugs for the treatment of infectious diseases, autoimmunity and cancer. Cyclic peptides constitute a class of compounds that have made crucial contributions to the treatment of certain diseases. Penicillin, Vancomycin, Cyclosporin, the Echinocandins and Bleomycin are well-known cyclic peptid...

journal_title：Current medicinal chemistry

authors： Katsara M,Tselios T,Deraos S,Deraos G,Matsoukas MT,Lazoura E,Matsoukas J,Apostolopoulos V

更新日期：2006-01-01 00:00:00

abstract：:Alzheimer's disease (AD) is a widespread form of dementia that is estimated to affect 44.4 million people worldwide. AD pathology is closely related to the accumulation of amyloid beta (Aβ) peptides in fibrils and plagues, the small oligomeric intermediate species formed during the Aβ peptides aggregation presenting t...

journal_title：Current medicinal chemistry

authors： Chiorcea-Paquim AM,Enache TA,Oliveira-Brett AM

更新日期：2018-01-01 00:00:00

abstract：:The story of antimalarials as antinflammatory drugs dates back several centuries. Chinin, the extract of the Cinchona bark, has been exploited since the 18th century for its antimalarial and antifebrile properties. Later, during the Second World War, the broad use of antimalarials allowed arguing their antirheumatic e...

journal_title：Current medicinal chemistry

authors： Piscianz E,Cuzzoni E,Sharma R,Tesser A,Sapra P,Tommasini A

更新日期：2018-01-01 00:00:00