Patented small molecule inhibitors of p53-MDM2 interaction.

abstract：:Introduction: Pharmacotherapy is limited by the inefficient drug targeting of non-healthy cells/tissues. In this pharmacological landscape, liposomes are contributing to the impulse given by Nanotechnology to optimize drug therapy. Areas covered: The analysis of the state-of-the-art in liposomal formulations for drug ...

journal_title：Expert opinion on therapeutic patents

authors： El-Hammadi MM,Arias JL

更新日期：2019-11-01 00:00:00

abstract：INTRODUCTION:Na/K-ATPase is a heterodimeric transmembrane protein that regulates neuronal signaling, ion homeostasis, muscle contraction and substrate transportation. Modulators of Na/K-ATPase inhibit Na(+)/K(+) exchange and increase cytosolic Ca(2+) to induce inotropic activity in heart failure patients. Besides produ...

journal_title：Expert opinion on therapeutic patents

authors： Wang HY,O'Doherty GA

更新日期：2012-06-01 00:00:00

abstract：INTRODUCTION:Focal adhesion kinase (FAK) is a non-receptor tyrosine kinase that localizes at sites of cell adhesion to the extracellular matrix (ECM) and mediates signalling events downstream of integrin engagement of the ECM. FAK is known to regulate cell survival, proliferation and migration. AREAS COVERED:FAK expre...

journal_title：Expert opinion on therapeutic patents

authors： Lv PC,Jiang AQ,Zhang WM,Zhu HL

更新日期：2018-02-01 00:00:00

abstract：INTRODUCTION:HIV/AIDS is one of the most devastating diseases in the world affecting > 40 million people worldwide. Morbidity and mortality from AIDS are significantly reduced due to the advent of highly active antiretroviral therapy (HAART). Long-term toxicity, emergence of drug resistant HIV strains and drug-drug int...

journal_title：Expert opinion on therapeutic patents

authors： Singh IP,Chauthe SK

更新日期：2011-02-01 00:00:00

abstract：INTRODUCTION:TANK-binding kinase 1 (TBK1) is a noncanonical IκB kinase family member that regulates the innate immune response. Misregulation of TBK1 activity can promote inflammatory disorders and oncogenesis; therefore, TBK1 inhibitors are considered a promising therapy for inflammation and cancer. AREAS COVERED:In ...

journal_title：Expert opinion on therapeutic patents

authors： Yu T,Yang Y,Yin DQ,Hong S,Son YJ,Kim JH,Cho JY

更新日期：2015-01-01 00:00:00

abstract：:The two patent applications describe two novel compounds in the benzimidazole class of GyrB/ParE antibacterial agents and multiple phosphate prodrugs derived from these compounds. The new benzimidazole compounds have excellent antibacterial activity on Gram-positive strains. But like previous benzimidazoles, they have...

journal_title：Expert opinion on therapeutic patents

authors： Finn J

更新日期：2013-09-01 00:00:00

abstract：INTRODUCTION:Antimicrobial peptides (AMPs) represent the large group of endogenous compounds widely distributed in nature. Due to their broad spectrum of antibiotic activity, as well as anti-inflammatory and immunomodulatory properties, AMPs became a model for the discovery of novel antimicrobial drugs that could answe...

journal_title：Expert opinion on therapeutic patents

authors： Kosikowska P,Lesner A

更新日期：2016-06-01 00:00:00

abstract：BACKGROUND:Inhibitors of the renin angiotensin aldosterone system (RAAS) represent some of the most widely prescribed, successful and well-tolerated therapeutics of recent times and are of proven worth in the management/prevention of cardiovascular disease and diabetic nephropathy. However, as knowledge has grown about...

journal_title：Expert opinion on therapeutic patents

authors： Laight DW

更新日期：2009-06-01 00:00:00

abstract：BACKGROUND:The application is in the field of neural stem cells (NSCs) and cellular therapy. OBJECTIVE:It aims at establishing conditions for the isolation and propagation of neural progenitor and stem cells from human fetal tissue, with high rate of growth and high yields of differentiation into the neuronal, astrogl...

journal_title：Expert opinion on therapeutic patents

authors： Taupin P

更新日期：2009-03-01 00:00:00

abstract：INTRODUCTION:Angiogenesis is an important component of certain normal physiological processes, but aberrant angiogenesis contributes to some pathological disorders and in particular to tumor growth. Activation of vascular endothelial growth factor receptor-2 (VEGFR-2) by vascular endothelial growth factor (VEGF) is a c...

journal_title：Expert opinion on therapeutic patents

authors： Peng FW,Liu DK,Zhang QW,Xu YG,Shi L

更新日期：2017-09-01 00:00:00

abstract：INTRODUCTION:Autophagy is a lysosome-dependent degradation pathway that maintains cellular homeostasis in response to a variety of cellular stresses. Accumulating reports based on animal models have indicated the importance of this catabolic program in many human pathophysiological conditions, including diabetes, neuro...

journal_title：Expert opinion on therapeutic patents

authors： Ha J,Kim J

更新日期：2016-11-01 00:00:00

abstract：INTRODUCTION:Over the past three years numerous patents and patent applications have been published relating to scientific advances in the use of the green tea polyphenol epigallocatechin gallate (EGCG) (the most abundant, and bioactive compound in green tea) and its analogs as anticancer agents. EGCG affects multiple ...

journal_title：Expert opinion on therapeutic patents

authors： Landis-Piwowar K,Chen D,Foldes R,Chan TH,Dou QP

更新日期：2013-02-01 00:00:00

abstract：INTRODUCTION:Bitopic M ligands, that is, ligands that interact both with the ortho- and allosteric binding sites of the M receptor subtypes, hold great potential as novel selective for muscarinic acetylcholine (M) ligands for several therapeutic applications. Areas covered: The patent application describes a set of com...

journal_title：Expert opinion on therapeutic patents

authors： Holzgrabe U,Decker M

更新日期：2017-02-01 00:00:00

abstract：INTRODUCTION:Hypoxia-inducible factor (HIF)-1α regulates the expression of genes involved in angiogenesis, cellular energy metabolism, and cell survival during cancer development. The increased expression of HIF-1α in most solid tumors is associated with poor prognoses and therapeutic outcomes. Therefore, HIF has been ...

journal_title：Expert opinion on therapeutic patents

authors： Ban HS,Uto Y,Won M,Nakamura H

更新日期：2016-01-01 00:00:00

abstract：INTRODUCTION:The orexin system consists of two G-protein-coupled receptors, orexin 1 and orexin 2 and two endogenous ligands, orexin A and orexin B . It is evolutionarily highly conserved. It is involved in the promotion of wakefulness as well as in anxiety and addictive disorders. In addition, its activation via the O...

journal_title：Expert opinion on therapeutic patents

authors： Boss C,Roch C

更新日期：2017-10-01 00:00:00

abstract：BACKGROUND:The application (WO2010075475) is involved in the diagnosis of angiogenesis-dependent diseases related with the soluble FMS-like tyrosine kinase-1 (sFlt-1) biomarker. OBJECTIVE:It aims to identify, characterize and produce antibodies raised against sFlt-1 for the diagnosis of preeclampsia as well as other c...

journal_title：Expert opinion on therapeutic patents

authors： Boyaud F,Inguimbert N

更新日期：2011-06-01 00:00:00

abstract：:In addition to its central role in haemostasis and wound healing, thrombin activates platelets and smooth muscle cells by proteolytic activation of cell surface protease-activated receptor-1 (PAR-1), which is also known as the thrombin receptor. Thrombin is the most potent activator of human platelets and, as such, a ...

journal_title：Expert opinion on therapeutic patents

authors： Chackalamannil S,Xia Y

更新日期：2006-04-01 00:00:00

abstract：:Increasing pharmacological studies have demonstrated that organic cation transporter 3 (OCT3) plays an important role in controlling the extracellular concentrations of released monoamine neurotransmitter, suggesting that OCT3 might be a promising target in the treatment of depression. As a consequence, compounds show...

journal_title：Expert opinion on therapeutic patents

authors： Hu T,Wang L,Pan X,Qi H

更新日期：2016-08-01 00:00:00

abstract：INTRODUCTION:Melanogenesis is the process of producing the melanin pigment, in which a series of chemical and enzymatic pathways are involved. Modulation at any level of this process would become an important approach in the treatment of hyper- or hypopigmentation-related diseases. Since hyperpigmentation covers import...

journal_title：Expert opinion on therapeutic patents

authors： Pillaiyar T,Manickam M,Jung SH

更新日期：2015-07-01 00:00:00

abstract：INTRODUCTION:The Rho kinase/ROCK is critical in vital signal transduction pathways central to many essential cellular activities. Since ROCK possess multiple substrates, modulation of ROCK activity is useful for treatment of many diseases. AREAS COVERED:Significant progress has been made in the development of ROCK inh...

journal_title：Expert opinion on therapeutic patents

authors： Feng Y,LoGrasso PV

更新日期：2014-03-01 00:00:00

abstract：INTRODUCTION:Apoptosis is an important and extensively studied pathway of programmed cell death, which is central to different physiological processes. Varied pathological implications, not limited to cancer and neurodegenerative diseases, occur if a slight dysfunction happens in the intricate apoptotic pathway. Theref...

journal_title：Expert opinion on therapeutic patents

authors： Kamal A,Faazil S,Malik MS

更新日期：2014-03-01 00:00:00

abstract：INTRODUCTION:Today, over 20 million people suffer from Alzheimer's disease (AD) worldwide. AD has become a critical issue to human health, especially in aging societies, and therefore it is a research hotspot in the global scientific community. The technology flow method differs from traditional reviews generating an i...

journal_title：Expert opinion on therapeutic patents

authors： Liu K,Lin HH,Pi R,Mak S,Han Y,Hu Y

更新日期：2018-04-01 00:00:00

abstract：IMPORTANCE OF THE FIELD:Small molecule glucokinase activators (GKAs) continue to represent a potential strategy to treat type 2 diabetes (T2D). Glucokinase (GK) primarily exerts its effect through modulatory actions in pancreatic β-cells and hepatocytes. It couples insulin secretion in the pancreas with plasma glucose ...

journal_title：Expert opinion on therapeutic patents

authors： Sarabu R,Berthel SJ,Kester RF,Tilley JW

更新日期：2011-01-01 00:00:00

abstract：:Introduction: The most conventional drug delivery systems exist with limitations such as drug degradation, toxicity and low bioavailability. Also, hypodermic injections can cause pain, compromising patient compliance. Due to this, transdermal drug delivery systems can minimize several problems associated with conventi...

journal_title：Expert opinion on therapeutic patents

authors： Queiroz MLB,Shanmugam S,Santos LNS,Campos CA,Santos AM,Batista MS,Araújo AAS,Serafini MR

更新日期：2020-06-01 00:00:00

abstract：INTRODUCTION:The oxadiazoles represent a class of five-membered heterocyclic compounds which are of considerable interest in different areas of medicinal chemistry and drug discovery. Oxadiazoles can exist in different regioisomeric forms and employ in various agents with a broad range of biological activities. This re...

journal_title：Expert opinion on therapeutic patents

authors： Zarghi A,Hajimahdi Z

更新日期：2013-09-01 00:00:00

abstract：INTRODUCTION:The N-acylhydrazone (NAH) moiety has been characterized as a privileged structure, capable of providing ligands points for more than one type of bioreceptor. Modifications of the subunits bonded to its acyl and imine functions resulted in several derivatives, which modulate a great diversity of molecular t...

journal_title：Expert opinion on therapeutic patents

authors： Maia Rdo C,Tesch R,Fraga CA

更新日期：2014-11-01 00:00:00

abstract：INTRODUCTION:New classes of synthetic and semi-synthetic β-glucan inhibitors have recently emerged, providing analogs that, in some cases, have been proven to have a high degree of activity against fungi, offering the prospect of alternatives to the commercially available lipopeptide/echinocandin agents caspofungin, mi...

journal_title：Expert opinion on therapeutic patents

authors： Hector RF,Bierer DE

更新日期：2011-10-01 00:00:00

abstract：INTRODUCTION:Monoacylglycerol lipase (MAGL) belongs to the endocannabinoid system and is responsible for the inactivation of endocannabinoid 2-arachidonoylglycerol. Importantly, it was found that MAGL degradation of lipids in cancer cells enhances the availability of free fatty acids for new cellular membrane formation...

journal_title：Expert opinion on therapeutic patents

authors： Bononi G,Poli G,Rizzolio F,Tuccinardi T,Macchia M,Minutolo F,Granchi C

更新日期：2020-11-01 00:00:00

abstract：INTRODUCTION:Xanthine oxidase (XO) is a molybdoflavoprotein that catalyzes the oxidative hydroxylation of purines to produce uric acid and reactive oxygen species. These reaction products can cause severe disease conditions like hyperuricemia which makes XO enzyme, an important therapeutic target in diseases like gout....

journal_title：Expert opinion on therapeutic patents

authors： Singh JV,Bedi PMS,Singh H,Sharma S

更新日期：2020-10-01 00:00:00

abstract：BACKGROUND:Severe acute respiratory syndrome (SARS) coronavirus emerged fleetingly in the winter of 2002 and again in the winter of 2003, resulting in the infection of ~8,000 people and the death of ~800. The identification of the putative natural reservoir suggests that a re-emergence is possible. The functions of man...

journal_title：Expert opinion on therapeutic patents

authors： Tong TR

更新日期：2009-03-01 00:00:00