Abstract:
:The emergence of multidrug-resistant Mycobacterium tuberculosis strains has made many of the currently available anti-tuberculosis (TB) drugs ineffective. Accordingly, there is a pressing need to identify new drug targets. Filamentous temperature-sensitive protein Z (FtsZ), a bacterial tubulin homologue, is an essential cell-division protein that polymerizes in a GTP-dependent manner, forming a highly dynamic cytokinetic ring, designated as the Z ring, at the septum site. Other cell-division proteins are recruited to the Z ring and, upon resolution of the septum, two daughter cells are produced. Since inactivation of FtsZ or alteration of FtsZ assembly results in the inhibition of Z-ring and septum formation, FtsZ is a very promising target for novel antimicrobial drug development. This review describes the function and dynamic behaviors of FtsZ and the recent development of FtsZ inhibitors as potential anti-TB agents.
journal_name
Future Med Chemjournal_title
Future medicinal chemistryauthors
Kumar K,Awasthi D,Berger WT,Tonge PJ,Slayden RA,Ojima Idoi
10.4155/fmc.10.220subject
Has Abstractpub_date
2010-08-01 00:00:00pages
1305-23issue
8eissn
1756-8919issn
1756-8927journal_volume
2pub_type
杂志文章,评审abstract::The pharmaceutical industry is facing numerous, well-documented challenges - from the effects of patent expirations to high attrition rates in the drug-development pipeline. Future Medicinal Chemistry has invited a group of leaders from academia and industry to express their views on where the industry is heading and ...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.11.145
更新日期:2011-11-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc.13.126
更新日期:2013-09-01 00:00:00
abstract::PA-824 is an experimental anti-tubercular agent that has a novel mechanism of action. It is effective against both active and persistent forms of the disease and has recently shown early bactericidal activity in a Phase II clinical trial. This review summarizes recent studies on the mode of action of PA-824 and outlin...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.10.207
更新日期:2010-08-01 00:00:00
abstract::During the current decade, data on the post-translational hydroxylation of specific amino acid residues of some ribosomal proteins and translation factors in both eukaryotes and eubacteria have accumulated. The reaction is catalyzed by dedicated oxygenases (so-called ribosomal oxygenases), whose action is impaired und...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2018-0317
更新日期:2019-02-25 00:00:00
abstract:BACKGROUND:Cucurbit[n]urils (CB[n]; n = 5, 6, 7, 8 or 10) are a family of macrocycles made from the acid-catalyzed condensation of glycoluril and formaldehyde. RESULTS:The synthesis of CB[n] using microwave radiation has been examined and the effect of acid type, reaction time and temperature on the distribution of pr...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.09.118
更新日期:2010-02-01 00:00:00
abstract::Graphical abstract [Formula: see text]. ...
journal_title:Future medicinal chemistry
pub_type: 社论
doi:10.4155/fmc-2019-0313
更新日期:2020-02-01 00:00:00
abstract:AIM:Triterpenes are natural compounds, whose wide biological activity predestines them for application as promising new chemotherapeutics. In this paper, we report the results of our investigations into the substitution of oleanolic acid with aromatic and nitroaromatic moieties acting as bioreducing agents. RESULTS:Th...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2017-0154
更新日期:2018-03-01 00:00:00
abstract::Aim: The explosion of data based technology has accelerated pattern mining. However, it is clear that quality and bias of data impacts all machine learning and modeling. Results & methodology: A technique is presented for using the distribution of first significant digits of medicinal chemistry features: logP, logS, a...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2019-0006
更新日期:2019-09-01 00:00:00
abstract::An α-carbonic anhydrases (CAs, EC 4.2.1.1) was recently discovered, cloned and characterized in the genome of the protozoan parasite Trypanosoma cruzi, the causative agent of Chagas disease, a neglected but widespread tropical disease. Inhibition of this α-CAs (TcCA) with anions, sulfonamides, sulfamates, thiols and h...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.15.185
更新日期:2016-01-01 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
pub_type: 杂志文章
doi:10.4155/fmc-2018-0254
更新日期:2019-02-25 00:00:00
abstract:BACKGROUND:The F508del mutation impairs the trafficking of CFTR from endoplasmic reticulum to plasma membrane and is responsible of a severe form of cystic fibrosis. Trafficking can be improved by small organic molecules called 'correctors'. MATERIALS & METHODS:By different synthetic ways, we prepared 4-chloroanisole ...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.14.118
更新日期:2014-01-01 00:00:00
abstract::Chi-Chao Chan, an American board certified ophthalmologist, is the Chief of Immunopathology Section, Laboratory of Immunology and the Head of Histology Core at the National Eye Institute at National Institutes of Health (USA). In 1967, Dr Chan graduated from Chungzhan Medical College in Guangzhou, China and then earne...
journal_title:Future medicinal chemistry
pub_type: 历史文章,面试
doi:10.4155/fmc.12.171
更新日期:2012-11-01 00:00:00
abstract::Anthraquinones exhibit a unique anticancer activity. Since their discovery, medicinal chemists have made several structural modifications, resulting in the design and synthesis of a large number of novel anthraquinone compounds with different biological activities. In general, anthraquinone compounds have been conside...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2019-0322
更新日期:2020-04-01 00:00:00
abstract::Epothilone is a newly developed antitumor drug; its antitumor principle is to stop the cell cycle by binding to tubulin in tumor cells, promoting tubulin polymerization, inhibiting depolymerization of microtubules, and ultimately inducing apoptosis. There are many analogs of epothilone, such as epothilone B, epothilon...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2017-0320
更新日期:2018-06-01 00:00:00
abstract::Many natural products that consist of quinoline core are found to be bioactive and the versatility of quinoline and its derivatives have attracted great attention in the field of drug development. As a result, in recent years, many green and sustainable synthetic approaches for the synthesis of structurally diverse qu...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.15.34
更新日期:2015-01-01 00:00:00
abstract::Alzheimer's disease (AD) is the most common cause of dementia with no cure at present. Cholesterol metabolism is closely associated with AD at several stages. ACAT1 converts free cholesterol to cholesteryl esters, and plays important roles in cellular cholesterol homeostasis. Recent studies show that in a mouse model,...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.15.161
更新日期:2015-01-01 00:00:00
abstract::Due to the unusual structure and chemical composition of the mycobacterial cell wall, effective tuberculosis (TB) treatment is difficult, making many antibiotics ineffective and hindering the entry of drugs. With approximately 33% of infection, TB is still the second most deadly infectious disease worldwide. The reaso...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.10.227
更新日期:2010-09-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc-2016-0153
更新日期:2016-12-01 00:00:00
abstract::Radiation-induced lung injury (RILI) is a common complication in cancer patients receiving local thoracic radiation and bone marrow transplantation conditioning. It is divided into early-stage radiation pneumonitis and advanced radiation fibrosis of the lung. This severely hampers the quality of life and survival of c...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2019-0162
更新日期:2020-12-01 00:00:00
abstract::The last 10 years have seen advances in automation and high-throughput biochemistry in the drug-discovery arena. However, these advances have not led to improvements in drug-discovery success. Drug programs must find new ways to identify superior compounds. Advances in label-free assay technologies may provide advanta...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.10.246
更新日期:2010-11-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc-2018-0208
更新日期:2018-11-01 00:00:00
abstract:AIM:Due to the complex nature of Alzheimer's disease, there is a renewed search for pleiotropic agents. RESULTS:Purine+coumarin hybrids have been synthesized and tested for the potential treatment of Alzheimer's disease. Hybrids 6, 4a-b, 14c and 14e inhibit significantly soybean lipoxygenase, whereas derivatives 14b, ...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc.14.158
更新日期:2015-01-01 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
pub_type: 面试
doi:10.4155/fmc-2017-0188
更新日期:2017-10-01 00:00:00
abstract::The DNA repair protein, O6-methylguanine DNA methyltransferase (MGMT), can confer resistance to guanine O6-alkylating agents. Therefore, inhibition of resistant MGMT protein is a practical approach to increase the anticancer effects of such alkylating agents. Numerous small molecule inhibitors were synthesized and exh...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc-2018-0069
更新日期:2018-08-01 00:00:00
abstract::More research effort needs to be invested in antimicrobial drug development to address the increasing threat of multidrug-resistant organisms. The enzyme DHPS has been a validated drug target for over 70 years as the target for the highly successful sulfa drugs. The use of sulfa drugs has been compromised by the wides...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.13.97
更新日期:2013-07-01 00:00:00
abstract::The cystic fibrosis transmembrane conductance regulator (CFTR) is a cAMP-regulated chloride channel localized primarily at the apical surfaces of epithelial cells lining airway, gut and exocrine glands, where it is responsible for transepithelial salt and water transport. Several human diseases are associated with an ...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.12.1
更新日期:2012-03-01 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
pub_type: 杂志文章,评审
doi:10.4155/fmc.15.25
更新日期:2015-01-01 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
pub_type: 杂志文章
doi:10.4155/fmc-2018-0224
更新日期:2018-12-06 00:00:00
abstract::The pharmacokinetic treatment strategy targets the drug molecule itself, aiming to reduce drug concentration at the site of action, thereby minimizing any pharmacodynamic effect. This approach might be useful in the treatment of acute drug toxicity/overdose and in the long-term treatment of addiction. Phase IIa contro...
journal_title:Future medicinal chemistry
pub_type: 杂志文章,评审
doi:10.4155/fmc.11.190
更新日期:2012-02-01 00:00:00
abstract:AIM:The use of 3D information has shown impact in numerous applications in drug design. However, it is often under-utilized and traditionally limited to specialists. We want to change that, and present an approach making 3D information and molecular modeling accessible and easy-to-use 'for the people'. METHODOLOGY/RES...
journal_title:Future medicinal chemistry
pub_type: 杂志文章
doi:10.4155/fmc-2016-0081
更新日期:2016-09-01 00:00:00