|
|
|
题名
|
作者
|
年代
|
出处
|
被引量
|
| 1 | Identification of arylamine N-acetyltransferase inhibitors as an approach towards novel anti-tuberculars显示文摘New anti-tubercular drugs and drug targets are urgently needed to reduce the time for treatment and also to identify agents that will be effective against Mycobacterium tuberculosis persisting intracellularly.Mycobacteria have a unique cell wall.Deletion of the gene for arylamine N-acetyltransferase(NAT)decreases mycobacterial cell wall lipids,particularly the distinctive mycolates,and also increases antibiotic susceptibility and killing within macrophage of Mycobacterium bovis BCG.The nat gene and its associated gene cluster are almost identical in sequence in M.bovis BCG and M.tuberculosis.The gene cluster is essential for intracellular survival of mycobacteria.We have therefore used pure NAT protein for high-throughput screening to identify several classes of small molecules that inhibit NAT activity.Here,we characterize one class of such molecules—triazoles—in relation to its effects on the target enzyme and on both M.bovis BCG and M.tuberculosis.The most potent triazole mimics the effects of deletion of the nat gene on growth,lipid disruption and intracellular survival.We also present the structure-activity relationship between NAT inhibition and effects on mycobacterial growth,and use ligand-protein analysis to give further insight into the structure-activity relationships.We conclude that screening a chemical library with NAT protein yields compounds that have high potential as anti-tubercular agents and that the inhibitors will allow further exploration of the biochemical pathway in which NAT is involved. | Isaac M.Westwood Sanjib Bhakta Angela J.Russell Elizabeth Fullam Matthew C.Anderton Akane Kawamura Andrew W.Mulvaney Richard J.Vickers Veemal Bhowruth Gurdyal S.Besra Ajit Lalvani Stephen G.Davies Edith Sim | 2010 | Protein & Cell2010，1，1： | 3 |
| 2 | Predictive markers of endocrine response in breast cancer显示文摘Ongoing clinical and research efforts seek to optimise the use of endocrine therapy in the treatment of breast cancer. Accurate biomarkers are needed that predict response for individual patients. The presence of the estrogen receptor(ER) as the direct(for tamoxifen and fulvestrant) or indirect(for aromatase inhibitors) target molecule for endocrine therapy remains the foremost biomarker and determinant of response. However, ER expression only poorly predicts outcome and further indicators of response or resistance are required. The development and application of molecular signature assays such as Oncotype Dx, Prosigna, Mammaprint and Endopredict have provided valuable information on prognosis and these are being used to support clinical decision making on whether endocrine therapy alone alongside surgery is sufficient for ER-positive early stage breast cancers or whether combination of endocrine with chemotherapy are also warranted. Ki67, the proliferation marker, has been widely used in the neo-adjuvant(pre-operative) setting to help predict response and long term outcome. Gene expression studies within the same setting have allowed monitoring of changes of potential predictive markers. These have identified frequent changes in estrogenregulated and proliferation genes. Specific molecules such as mutant ER may also prove helpful biomarkers in predicting outcome and monitoring response to treatment. | Duniya Mosly Arran Turnbull Andrew Sims Carol Ward Simon Langdon | 2018 | World Journal of Experimental Medicine2018，8，1： | 2 |
| 3 | SJWD14072900000111显示文摘 | Jin Yao Teo Brian Kim Poh Goh Foong Koon Cheah John Carson Allen Richard Hoau Gong Lo David Chee Eng Ng Anthony Soon Whatt Goh Andrew Yu Keat Khor Hui Shan Sim Jia Jun Ng Pierce Kah‐Hoe Chow | 2014 | Journal of Digestive Diseases2014，，8： | 1 |
| 4 | Discovering Your Authentic Leadership显示文摘 | George Bill Sims Peter McLean Andrew N Mayer Diana | | 0，，02： | 1 |
| 5 | Investigation into the physical and chemical properties of sodium casienate-maltodextrin glyco-conjugates显示文摘 | Gordon A Morris Ian M Sims Andrew J Robertson | 2004 | Food Colloids2004，，18： | 1 |
| 6 | V∞-leveraging for interplanetary missions: multiple-revolution orbit techniques 显示文摘 | JON A SIMS JAMES M LONGUSKI ANDREW J STAUGLER | 1997 | Journal of Guidance Control and Dynamics1997，20，3： | 1 |
| 7 | 修炼你的真诚领导力显示文摘安进公司(Amgen)的CEO兼总裁凯文?沙拉尔(Kevin Sharer)曾说:“领导力可以有多种表现形式。你应该坚持真实的自我,而不是去模仿他人。”模仿他人只会使自己变得不真实,而在21世纪,我们需要的是真诚的领导者。真诚的领导者会热切追求自己的目标,坚持自己的价值观,在工作中既用脑也用心。他们懂得与人建立长期且有意义的联系,并严格要求自己,以达到目标。更重要的是,他们能让公司长时期保持优秀的业绩。 | Bill George Peter Sims Andrew N. McLean Diana Mayer | 2007 | 工程经济2007，，7： | 1 |
| 8 | Unstable Proximal Extraarticular Tibia Fractures: A Biomechanical Evaluation of Four Methods of Fixation显示文摘 | Richard D. Peindl Robert D. Zura Andrew Vincent Edward R. Coley Michael J. Bosse Stephen H. Sims | 2004 | Journal of Orthopaedic Trauma2004，，8： | 1 |
| 9 | The Embryonic Transcription Cofaetor LBH Is a Direct Target of the Wnt Signaling Pathway in Epithelial Development and in Aggressive Basal Subtype Breast Cancers显示文摘 | Megan E Rieger Andrew H Sims Ebony R | 2010 | Mol Cell Biol2010，30，17： | 1 |
| 10 | The Embryonic Transcription Cofactor LBH is a Direct Target of the Wnt signaling Pathway in Epithelial Development and in Aggressive Basal Subtype Breast Cancers显示文摘 | Megan E Riger Andrew H Sims Ebony R | 2010 | Mol cell Biochem2010，30，17： | 1 |
| 11 | Gene expression profiling of response to mTOR inhibitor everolimus in pre-operatively treated post-menopausal women with oestrogen receptor-positive breast cancer显示文摘 | Vicky S. Sabine Andrew H. Sims E. Jane Macaskill Lorna Renshaw Jeremy S. Thomas J. Michael Dixon John M. S. Bartlett | 2010 | Breast Cancer Research and Treatment2010，，2： | 1 |
| 12 | Successful Treatment of Invasive Cavernous Sinus Aspergillosis with Oral Itraconazole Monotherapy显示文摘 | Andrew C Browning Kuan T Sim Judith M Timms Stephen A Vernon Norman S McConachie Richard Allibone Nick S Jones | 2006 | Journal of Neuro-Ophthalmology2006，，2： | 1 |
| 13 | Human epidermal growth factor receptor targeted inhibitors for the treatment of ovarian cancer显示文摘Ovarian cancer is the second most lethal gynecological cancer worldwide and while most patients respond to initial therapy, they often relapse with resistant disease. Human epidermal growth factor receptors(especially HER1/EGFR and HER2/ERBB2) are involved in disease progression; hence, strategies to inhibit their action could prove advantageous in ovarian cancer patients,especially in patients resistant to first line therapy. Monoclonal antibodies and tyrosine kinase inhibitors are two classes of drugs that act on these receptors. They have demonstrated valuable antitumor activity in multiple cancers and their possible use in ovarian cancer continues to be studied. In this review, we discuss the human epidermal growth factor receptor family; review emerging clinical studies on monoclonal antibodies and tyrosine kinase inhibitors targeting these receptors in ovarian cancer patients; and propose future research possibilities in this area. | Maria Bonello ANDrew Harvey Sims Simon Peter Langdon | 2018 | Cancer Biology & Medicine2018，15，4： | 1 |
| 14 | 修炼你的真诚领导力显示文摘何谓卓越的领导者?在过去的50年里,为了确定卓越领导者的管理风格、特征和性格特点,研究人员做了1,000多项研究。然而,这些研究者都没有将一个理想的领导者形象清晰地描述出来。不过,也幸亏他们没有做到这点,否则管理者就会去争相模仿,给自己戴上假面具,不但失去自我,也很容易被别人一眼看穿。 | 比尔·乔治(Bill George) 彼得·西姆斯(Peter Sims) 安德鲁·麦克莱恩(Andrew N.McLean) 戴安娜·迈耶(Diana Mayer) | 2007 | 商业评论2007，，7： | 0 |
| 15 | 牛奶加工过程中的压力监测显示文摘雀巢公司位于瑞士柯诺芬根的研发中心开发奶制品。并设计制造工艺。而监测换热器的压力,对于这家研发中心来说具有特殊的挑战性。 | Andrew Sim Baumer | 2010 | 软件2010，31，4： | 0 |
您所在的机构暂未开通此部分的功能，请联系管理员