Structural and functional regulation of lactate dehydrogenase-A in cancer.

abstract：:Camellia oleifera Abel is a member of Camellia, and its seeds are used to extract Camellia oil, which is generally used as cooking oil in the south of China. Camellia oil consists of unsaturated fatty acids, tea polyphenol, squalene, saponin, carrot element and vitamins, etc. The seed remains after oil extraction of C...

journal_title：Future medicinal chemistry

authors： Xiao X,He L,Chen Y,Wu L,Wang L,Liu Z

更新日期：2017-11-01 00:00:00

abstract：:Cancer is a major devastating disease, and is a leading cause of death worldwide. Despite the progress in cancer treatment, cancer mortality rate remains high. Therefore, the discovery and development of improved anticancer drugs to treat cancer are needed. 4H-chromenes have strong cytotoxicity against a panel of huma...

journal_title：Future medicinal chemistry

authors： Patil SA,Patil R,Pfeffer LM,Miller DD

更新日期：2013-09-01 00:00:00

abstract：:Antibiotic drug discovery has been an essential field of research since the early 1900s, but the threat from infectious bacteria has only increased over the decades because of the emergence of widespread multidrug resistance. In this review, we discuss the recent advances in natural product, computational and medicina...

journal_title：Future medicinal chemistry

authors： Murphy KE,Sloan GF,Lawhern GV,Volk GE,Shumate JT,Wolfe AL

更新日期：2020-11-01 00:00:00

abstract：AIM:The undeniable indomethacin potency has always suffered serious obstacles such as gastric damage. Continuous attempts to develop potent yet safe indomethacin analogs have never ceased. RESULTS:Herein are new indole derivatives 4a-h and 5a-c, which were synthesized via Fisher indole reaction, evaluated for both the...

journal_title：Future medicinal chemistry

authors： Amin NH,El-Saadi MT,Hefny AA,Abdelazeem AH,Elshemy HA,Abdellatif KR

更新日期：2018-12-06 00:00:00

abstract：:Carbonic anhydrases (CAs; EC 4.2.1.1) are well known zinc metalloproteins involved in the catalysis of a very simple but essential physiological reaction: carbon dioxide hydration to bicarbonate and proton. These enzymes are of clinical relevance in cancer therapy as among the 15 isoforms known in humans, two cell sur...

journal_title：Future medicinal chemistry

authors： Supuran CT,Winum JY

更新日期：2015-01-01 00:00:00

abstract：:PEGylation is the covalent conjugation of PEG to therapeutic molecules. Protein PEGylation is a clinically proven approach for extending the circulation half-life and reducing the immunogenicity of protein therapeutics. Most clinically used PEGylated proteins are heterogeneous mixtures of PEG positional isomers conjug...

journal_title：Future medicinal chemistry

authors： Ginn C,Khalili H,Lever R,Brocchini S

更新日期：2014-01-01 00:00:00

abstract：BACKGROUND:The objective of this study was to develop and evaluate a more effective mucoadhesive thiomer for buccal drug-delivery systems. METHODS:2-iminothiolane was covalently attached to a chitosan backbone. A preactivation step followed, mediated by 6,6´dithionicotinamide, thiol groups were modified by disulfide b...

journal_title：Future medicinal chemistry

authors： Laffleur F,Shahnaz G,Islambulchilar Z,Bernkop-Schnürch A

更新日期：2013-04-01 00:00:00

abstract：:FGF19 is a noncanonical FGF ligand that can control a broad spectrum of physiological responses, which include bile acid homeostasis, liver metabolism and glucose uptake. Many of these responses are mediated by FGF19 binding to its FGFR4/β-klotho receptor complex and controlling activation of an array of intracellular...

journal_title：Future medicinal chemistry

authors： Prieto-Dominguez N,Shull AY,Teng Y

更新日期：2018-10-01 00:00:00

abstract：:Alzheimer's disease is a multifactorial syndrome, for which effective cures are urgently needed. Seeking for enhanced therapeutic efficacy, multitarget drugs have been increasingly sought after over the last decades. They offer the attractive prospect of tackling intricate network effects, but with the benefits of a s...

journal_title：Future medicinal chemistry

authors： Rosini M,Simoni E,Caporaso R,Minarini A

更新日期：2016-04-01 00:00:00

abstract：AIM:This research paper is aimed at designing a novel insulin alternative for the treatment of diabetes. MATERIALS & METHODS:Six novel vanadyl(II) compounds, [(AMP-2)(VO+2)(AA n-1)]·NH4+1, were synthesized from an equimolar ratio of adenosine monophosphate, VOSO4 and amino acids (AA n ). RESULTS:The magnetic moments ...

journal_title：Future medicinal chemistry

authors： Naglah AM,Al-Omar MA,Kalmouch A,Alsuhaibani AM,El-Didamony AM,Hassan N,Taleb SA,Refat MS,Almehizia AA,Bhat MA,Al-Shakliah NS,Al-Humaidi JY,Al-Wasidi AS

更新日期：2019-01-15 00:00:00

abstract：:Metal complexes have been the subject of numerous investigations in oncology but, despite the plethora of newly synthesized compounds, their precise mechanisms of action remain generally unknown or, for the best, incompletely determined. The continuous development of efficient and sensitive techniques in analytical ch...

journal_title：Future medicinal chemistry

authors： Marloye M,Berger G,Gelbcke M,Dufrasne F

更新日期：2016-12-01 00:00:00

abstract：AIM:Cancer is among the leading causes of death worldwide. Medical interest has focused on macrocyclic polyamines because of their properties as antitumor agents. Results/Methodology: We have designed and synthesized a series of 1,2-diaminocyclohexane derivatives with notable in vitro antiproliferative activities again...

journal_title：Future medicinal chemistry

authors： Morales F,Ramírez A,Morata-Tarifa C,Navarro SA,Marchal JA,Campos JM,Conejo-García A

更新日期：2017-03-01 00:00:00

abstract：:Due to the impermeable structure and barrier function of the blood-brain barrier (BBB), the delivery of therapeutic molecules into the CNS is extremely limited. Nanodelivery systems are regarded as the most effective and versatile carriers for the CNS, as they can transport cargo molecules across the BBB via various m...

journal_title：Future medicinal chemistry

authors： Kim KT,Lee HS,Lee JJ,Park EK,Lee BS,Lee JY,Bae JS

更新日期：2018-11-01 00:00:00

abstract：:Metabolic stability is an important property of drug candidates and pharmaceutical companies often have human liver microsomal (HLM) data for a large number of molecules, enabling development of global quantitative structure-activity relationship models. RESULTS:This study describes a strategy for building a global H...

journal_title：Future medicinal chemistry

authors： Stålring J,Sohlenius-Sternbeck AK,Terelius Y,Parkes K

更新日期：2018-07-01 00:00:00

abstract：BACKGROUND:4'-seleno-homonucleosides were synthesized as next-generation nucleosides, and their cellular phosphorylation was studied to confirm the hypothesis that bulky selenium atom can sterically hinder the approach of cellular nucleoside kinase to the 5'-OH for phosphorylation. RESULTS:4'-seleno-homonucleosides (n...

journal_title：Future medicinal chemistry

authors： Yu J,Sahu PK,Kim G,Qu S,Choi Y,Song J,Lee SK,Noh M,Park S,Jeong LS

更新日期：2015-01-01 00:00:00

abstract：:As has been widely reviewed elsewhere, the pharmaceutical industry is experiencing an 'innovation deficit' as evidenced by the decline in new chemical entity output. This decline, compounded by increased costs and regulatory requirements highlights the need to significantly revise strategic options across the drug-dis...

journal_title：Future medicinal chemistry

authors： Robertson GM,Mayr LM

更新日期：2011-12-01 00:00:00

abstract：:Nutrient-sensing receptors, including fatty acid receptors (FFA1-FFA4), Ca2+-sensing receptors and Zn2+-sensing receptors, are involved in several biological processes. These receptors are abundantly expressed in the GI tract, where they have been shown to play crucial roles in regulating GI function. This review prov...

journal_title：Future medicinal chemistry

authors： Pongkorpsakol P,Moonwiriyakit A,Muanprasat C

更新日期：2017-03-01 00:00:00

abstract：BACKGROUND:Histone lysine demethylases (KDMs) are well-recognized targets in oncology drug discovery. They function at the post-translation level controlling chromatin conformation and gene transcription. KDM1A is a flavin adenine dinucleotide-dependent amine oxidase, overexpressed in several tumor types, including acu...

journal_title：Future medicinal chemistry

authors： Trifirò P,Cappa A,Brambillasca S,Botrugno OA,Cera MR,Zuffo RD,Dessanti P,Meroni G,Thaler F,Villa M,Minucci S,Mercurio C,Varasi M,Vianello P

更新日期：2017-07-01 00:00:00

abstract：:Hepatitis B Virus (HBV) is one of the most prevalent viral infections of human worldwide. The therapies are limited in the clinical context because of negative side effects of interferons and the development of viral resistance to the nucleoside/nucleotide inhibitors. In this review, we summarize the recent advances i...

journal_title：Future medicinal chemistry

authors： Jia H,Rai D,Zhan P,Chen X,Jiang X,Liu X

更新日期：2015-01-01 00:00:00

abstract：:Cancer, still in the limelight due to its dreadful nature, shows overexpression of multiple signaling macromolecules leading to failure of many chemotherapeutic agents and acquired resistance to chemotherapy. These factors highlight the significance of shifting toward targeted therapy in cancer research. Recently, ERK...

journal_title：Future medicinal chemistry

authors： Pathania S,Rawal RK

更新日期：2020-04-01 00:00:00

abstract：:Despite the wealth of information available for the reverse transcriptase (RT)-associated ribonuclease H (RNaseH) domain of lentiviruses, gammaretroviruses and long terminal repeat containing retrotransposons, exploiting this information in the form of an RNaseH inhibitor with high specificity and low cellular toxicit...

journal_title：Future medicinal chemistry

authors： Corona A,Masaoka T,Tocco G,Tramontano E,Le Grice SF

更新日期：2013-12-01 00:00:00

abstract：:Several hundred genes associated or linked to obesity have been described in the scientific literature. Whereas many of these genes are potential targets for the treatment of obesity and associated conditions, none of them have permitted the developement of an efficient drug therapy. As proposed by the 'thrifty genoty...

journal_title：Future medicinal chemistry

authors： Braud S,Ciufolini M,Harosh I

更新日期：2010-12-01 00:00:00

abstract：BACKGROUND:Since trifluoromethyl-containing compounds have found diverse applications in the fields of pharmaceuticals and agrochemicals, facile and selective synthetic methods for trifluoromethyl-substituted compounds are an essential tool for advanced medicinal chemistry. Now that diverse synthetic transformations of...

journal_title：Future medicinal chemistry

authors： Shimizu M,Higashi M,Takeda Y,Murai M,Jiang G,Asai Y,Nakao Y,Shirakawa E,Hiyama T

更新日期：2009-08-01 00:00:00

abstract：BACKGROUND:Traditional and current opioid pharmacology is fundamentally based on interactions between opioid receptors and compounds isolated from natural sources. Adverse effects associated with opioids have led to the search for compounds with diminished side effects. DISCUSSION:Recent discoveries of non-nitrogenous...

journal_title：Future medicinal chemistry

authors： Lovell KM,Simpson DS,Cunningham CW,Prisinzano TE

更新日期：2009-05-01 00:00:00

abstract：:In comparison with other virus infections, such as HIV, HBV, HCV, influenza and herpes virus, dengue virus infections have received relatively little attention from a (chemo)therapeutic viewpoint, despite their global incidence (2.5 billion people estimated to be at risk) and absence of an effective prophylactic measu...

journal_title：Future medicinal chemistry

authors： De Clercq E

更新日期：2010-04-01 00:00:00

abstract：:Dextran has become a hot research topic in drug vehicle material because of its biodegradable, nonspecific cell adhesion, resistance to protein adsorption, low price and ease of structural modification. The fate and changes of dextran in vivo are not fully understood. It is helpful to guide the design and modification...

journal_title：Future medicinal chemistry

authors： Huang S,Huang G

更新日期：2019-07-01 00:00:00

abstract：:The rise of antibiotic resistant bacteria requires unconventional strategies toward efficient chemotherapeutic agents, preferably with alternative mechanisms of action. The bacterial cell membrane has become an appealing target since its essential and highly conservative structure are key challenges to resistance mech...

journal_title：Future medicinal chemistry

authors： Dias C,Rauter AP

更新日期：2019-02-25 00:00:00

abstract：:Richard H Ebright talks to Rachel Coleby, Commissioning Editor: Ebright is at Rutgers University (New Brunswick, NJ, USA), where he performs research on the structure, mechanism, and regulation of bacterial transcription and on antibacterial drug discovery targeting bacterial transcription. He has received research aw...

journal_title：Future medicinal chemistry

authors： Ebright RH

更新日期：2017-10-01 00:00:00

abstract：:MRI has been recognized as one of the most applied medical imaging techniques in clinical practice. However, the presence of background signal coming from water protons in surrounding tissues makes sometimes the visualization of local contrast agents difficult. To remedy this, fluorine has been introduced as a reliabl...

journal_title：Future medicinal chemistry

authors： Hequet E,Henoumont C,Muller RN,Laurent S

更新日期：2019-05-01 00:00:00

abstract：:Schistosomes, like many eukaryotic pathogens, typically display morphologically distinct stages during their life cycles. Epigenetic mechanisms underlie the pathogens' morphological transformations, and the targeting of epigenetics-driven cellular programs therefore represents an Achilles' heel of parasites. To speed ...

journal_title：Future medicinal chemistry

authors： Marek M,Oliveira G,Pierce RJ,Jung M,Sippl W,Romier C

更新日期：2015-01-01 00:00:00