·经典文献推荐·

·经典文献推荐·

基于 Web of Science检索结果，利用Histcite软件选取 LCS（Local Citation Score，本地引用次数）TOP50文献作为节点进行分析，得到本领域推荐的经典文献如下。

Structure of a covalently trapped catalytic complex of HIV-I reverse transcriptase: Implications for drug resistance

Huang, HF; Chopra, R; Verdine, GL; et al.

Molecular mechanisms that confer antibacterial drug resistance

Walsh, C

Resistance to antibiotics: Are we in the post-antibiotic era?

Alanis, AJ

来源出版物：Archives of Medical Research, 2005, 36(6): 697-705

New antibiotics for bad bugs: Where are we?

Bassetti, Matteo; Merelli, Maria; Temperoni, Chiara; et al.

Abstract: Bacterial resistance to antibiotics is growing up day by day in both community and hospital setting, with a significant impact on the mortality and morbidity rates and the financial burden that is associated. In the last two decades multi drug resistant microorganisms (both hospital- and community-acquired) challenged the scientific groups into developing new antimicrobial compounds that can provide safety in use according to the new regulation, good efficacy patterns, and low resistance profile. In this review we made an evaluation of present data regarding the new classes and the new molecules from already existing classes of antibiotics and the ongoing trends in antimicrobial development. Infectious Diseases Society of America (IDSA) supported a proGram, called “the 10 × 20' initiative”, to develop ten new systemic antibacterial drugs within 2020. Themicroorganisms mainly involved in the resistance process, so called the ESKAPE pathogens (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumanii, Pseudomonas aeruginosa, and enterobacteriaceae) were the main targets. In the era of antimicrobial resistance the new antimicrobial agents like fifth generation cephalosporins, carbapenems, monobactams, beta-lactamases inhibitors, aminoglycosides, quinolones, oxazolidones, glycopeptides, and tetracyclines active against Gram-positive pathogens, like vancomycin-resistant S. aureus (VRSA) and MRSA, penicillin-resistant streptococci, and vancomycin resistant Enterococcus (VRE) but also against highly resistant Gram-negative organisms are more than welcome. Of these compounds some are already approved by official agencies, some are still in study, but the need of new antibiotics still does not cover the increasing prevalence of antibiotic-resistant bacterial infections. Therefore the management of antimicrobial resistance should also include fostering coordinated actions by all stakeholders, creating policy guidance, support for surveillance and technical assistance.

Keywords: new antibiotics; resistance; bacteria; FDA; EMA

来源出版物：Annals of Clinical Microbiology and Antimicrobials, 2013, 12: 22-36

Acquired drug resistance is a major problem in the treatment of cancer. Of the more than 500000 annual deaths from cancer in the United States, many follow the development of resistance to chemotherapy. The emergence of resistance depends in part on the genetic instability, heterogeneity and high mutational rate of tumour cells. In contrast, endothelial cells are genetically stable, homogenous and have a low mutational rate. Therefore, anti-angiogenic therapy directed against a tumour’s endothelial cells should, in principle, induce little or no drug resistance, Endostatin, a potent angiogenesis inhibitor, was administered to mice bearing Lewis lung carcinoma, T241 fibrosarcoma or B16F10 melanoma. Treatment was stopped when tumours had regressed. Tumours were then allowed to re-grow and endostatin therapy was resumed. After 6, 4 or 2 treatment cycles, respectively, no tumours recurred after discontinuation of therapy, These experiments show that drug resistance does not develop in three tumour types treated with a potent angiogenesis inhibitor, An unexpected finding is that repeated cycles of antiangiogenic therapy are followed by prolonged tumour dormancy without further therapy.

来源出版物：Nature, 1997, 390(6658): 404-407

Abstract: A combinatorial disulfide cross-linking strategy was used to prepare a stalled complex of human immunodeficiency virus-type 1 (HIV-1) reverse transcriptase with a DNA template: Primer and a deoxynucleoside triphosphate (dNTP), and the crystal structure of the complex was determined at a resolution of 3.2 angstroms. The presence of a dideoxynucleotide at the 3’-primer terminus allows capture of a state in which the substrates are poised for attack on the dNTP. Conformational changes that accompany formation of the catalytic complex produce distinct clusters of the residues that are altered in viruses resistant to nucleoside analog drugs. The positioning of these residues in the neighborhood of the dNTP helps to resolve some Long-standing puzzles about the molecular basis of resistance. The resistance mutations are Likely to influence binding or reactivity ofthe inhibitors, relative to normal dNTPs, and the clustering of the mutations correlates with the chemical structure of the drug.

来源出版物：Science, 1998, 282(5394): 1669-1675

Abstract: Antibiotics compounds that are literally‘against life’ - are typically antibacterial drugs, interfering with some structure or process that is essential to bacterial growth or survival without harm to the eukaryotic host harbouring the infecting bacteria. We live in an era when antibiotic resistance has spread at an alarming rate and when dire predictions concerning the lack of effective antibacterial drugs occur with increasing frequency. In this context it is apposite to ask a few simple questions about these life-saving molecules. What are antibiotics? Where do they come from? How do they work? Why do they stop being effective? How do we find new antibiotics? And can we slow down the development of antibiotic-resistant superbugs?

来源出版物：Nature, 2000, 406(6797): 775-781

Abstract:Serious infections caused by bacteria that have become resistant to commonly used antibiotics have become a major global healthcare problem in the 21st century. They not only are more severe and require longer and more complex treatments, but they are also significantly more expensive to diagnose and to treat. Antibiotic resistance, initially a problem of the hospital setting associated with an increased number of hospital-acquired infections usually in critically ill and immunosuppressed patients, has now extended into the community causing severe infections difficult to diagnose and treat. The molecular mechanisms by which bacteria have become resistant to antibiotics are diverse and complex. Bacteria have developed resistance to all different classes of antibiotics discovered to date. The most frequent type of resistance is acquired and transmitted horizontally via the conjugation of a plasmid. In recent times new mechanisms of resistance have resulted in the simultaneous development of resistance to several antibiotic classes creating very dangerous multidrugresistant (MDR) bacterial strains, some also known as“superbugs”. The indiscriminate and inappropriate use of antibiotics in outpatient clinics, hospitalized patients and in the food industry is the single largest factor leading to antibiotic resistance. In recent years, the number of new antibiotics licensed for human use in different parts of the world has been lower than in the recent past. In addition, there has been less innovation in the field of antimicrobial discovery research and development. The pharmaceutical industry, large academic institutions or the government are not investing the necessary resources to produce the next generation of newer safe and effective antimicrobial drugs. In many cases, large pharmaceutical companies have terminated their anti-infective research programs altogether due to economic reasons. The potential negative consequences of all these events are relevant because they put society at risk for the spread of potentially serious MDR bacterial infections.

antibiotic resistance; bacterial resistance; new antibiotics; antibiotic research

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文章题目第一作者来源出版物1 Antiangiogenic therapy of experimental cancer does not induce acquired drug resistance Boehm, T Nature, 1997, 390(6658): 404-407 2 3 4 5 Structure of a covalently trapped catalytic complex of HIV-I reverse transcriptase: Implications for drug resistance Molecular mechanisms that confer antibacterial drug resistance Resistance to antibiotics: Are we in the post-antibiotic era? New antibiotics for bad bugs: Where are we? Huang, HF Walsh, C Alanis, AJ Bassetti, Matteo Science, 1998, 282(5394): 1669-1675 Nature, 2000, 406(6797): 775-781 Archives of Medical Research, 2005, 36(6): 697-705 Annals of Clinical Microbiology and Antimicrobials, 2013, 12: 22-36

Antiangiogenic therapy of experimental cancer does not induce acquired drug resistance

Boehm, T; Folkman, J; Browder, T; et al.