Protein‐Reactive Natural Products

Drahl, Carmen; Cravatt, Benjamin F.; Sorensen, Erik J.

doi:10.1002/anie.200500900

Cited by 235 publications

(151 citation statements)

References 363 publications

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“…Since secondary metabolic from natural resources have been elaborated within living systems, they are often perceived as showing more "drug likeness and biological friendliness than totally synthetic molecules" making them good candidates for further drug development. Biomolecules of plant origin appear to be one of the alternatives for the control of these antibiotic resistant human pathogens (Koehn, and Carter 2005;Balunas, 2005;Drahl, 2005).…”

Section: Introductionmentioning

confidence: 99%

Phytochemical screening and antimicrobial activity of roots, stem-bark and leave extracts of Grewia mollis

Shagal¹,

Kubmarawa²,

Idi³

2012

Afr. J. Biotechnol.

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The roots, stem-bark and leaves of Grewia mollis which is used as herbal remedies for the cure of diarrhea and dysentery by natives in northern part of Nigeria were studied. The ethanol and water extracts of roots, stem-bark and leaves of the plant were subjected to phytochemical screening and antimicrobial activity against Salmonella typhii, Escherichia coli, Streptococcus sp. and Staphylococcus aureus. From the tests carried out, the result reveals the presence of saponins, flavonoids, glycosides, tannins, volatile oils, alkaloids and phenols in the leaves extract of the plant. The antimicrobial activity revealed that ethanol extracts of the plant parts were active against E. coli, S. aureus and Streptococcus sp. This supports the claims of efficacy reported in fork use of the plant in the treatment of disease caused by some pathogens and if further purified can be used as source of novel antibiotics.

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Section: Introductionmentioning

confidence: 99%

Phytochemical screening and antimicrobial activity of roots, stem-bark and leave extracts of Grewia mollis

Shagal¹,

Kubmarawa²,

Idi³

2012

Afr. J. Biotechnol.

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“…These data do not conflict with previous reports demonstrating that FAS inhibitors activate the intrinsic cell death pathway and that ceramide accumulation contributes to FAS inhibitor induced cell death (34,41). In fact, a previous study demonstrated that ceramide accumulation is also associated with thapsigargin induced ER stress and apoptosis (36). It is possible that FAS inhibitor induced ER stress may result in ceramide accumulation that is important in for cell death; however, the relationship between FAS inhibition, ER stress, and subsequent downstream events remains to be determined.…”

Section: Pharmacological Inhibition Of Fas Induces Phosphorylation Ofmentioning

confidence: 97%

“…(36). The stability of the intermediate appears to come from the extensive contacts of the lipophilic components of Orlistat to the enzyme surface ( Fig.…”

Section: Key Research Accomplishmentsmentioning

confidence: 98%

Inhibition of Fatty Acid Synthase in Prostate Cancer by Olristat, a Novel Therapeutic

Kridel¹

2006

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Public reporting burden for this collection of information is estimated to average 1 hour per response, including the time for reviewing instructions, searching existing data sources, gathering and maintaining the data needed, and completing and reviewing this collection of information. Send comments regarding this burden estimate or any other aspect of this collection of information, including suggestions for reducing this burden to Department of Defense, Washington Headquarters Services, Directorate for Information Operations and Reports (0704-0188), 1215 Jefferson Davis Highway, Suite 1204, Arlington, VA 22202-4302. Respondents should be aware that notwithstanding any other provision of law, no person shall be subject to any penalty for failing to comply with a collection of information if it does not display a currently valid OMB control number. PLEASE DO NOT RETURN YOUR FORM TO THE ABOVE ADDRESS. REPORT DATE PERFORMING ORGANIZATION NAME(S) AND ADDRESS(ES) 8. PERFORMING ORGANIZATION REPORT NUMBERWake Forest University Health Sciences Winston-Salem, NC 27157 SPONSORING / MONITORING AGENCY NAME(S) AND ADDRESS(ES) 10. SPONSOR/MONITOR'S ACRONYM(S) U.S. Army Medical Research and Materiel Command Fort Detrick, Maryland 21702-5012 SPONSOR/MONITOR'S REPORT NUMBER(S) DISTRIBUTION / AVAILABILITY STATEMENTApproved for Public Release; Distribution Unlimited SUPPLEMENTARY NOTESOriginal contains colored plates: ALL DTIC reproductions will be in black and white. ABSTRACTThe overall goal of this project s to understand the anti-tumor effects of FAS inhibitors. We have followed up on our previous findings by further evaluating the role of ER stress in tumor cells treated with FAS inhibitors. Our results suggest that ER stress may initiate the cell death program when FAS is inhibited in prostate tumor cell lines. Moreover, the data also suggest that the ER may sense fatty acid levels in tumor cells. A further connection to ER stress was discovered by showing that other ER stressing agents like Velcade induce fatty acid synthase activity and sensitize cells to the effects of FAS inhibitors. We have also made the novel observation that FAS expression is regulated by the src oncogene and that FAS inhibitors can block src driven matrigel invasion. Combined these data provide insight into how disruption of the FAS axis can be further exploited to inhibit prostate tumor growth and metastases. We have also extended our previous crystallography studies by solving the crystal structure of FAS bound to a cleaved orlistat. These data will provide valuable insight into future drug discovery and design within the FAS pathway. In total, we have made great strides toward understanding the anti-tumor effects of orlistat and other FAS inhibitors in prostate cancer through a multi-disciplinary approach combining cell biology, biochemistry and crystallography. SUBJECT TERMS A. IntroductionThis is the annual report for grant # W81XWH-05-1-0065 entitled "Inhibition of Fatty Acid Synthase by Orlistat: A Novel Therapeutic". The funding period fo...

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“…Majority of the plant metabolites in drug discovery has come from the diverse structures of the medicinal plants. These are often perceived as immense drug-likeness and more biological friendliness and making them good candidates in drug development [5][6][7][8][9] .…”

Section: Introductionmentioning

confidence: 99%

Bactericidal activity of Flavonoids isolated from Muntingia calabura

Gorripati¹,

Rajashekar²,

Dasu³

et al. 2018

IJLSSR

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The investigation was carried out for the isolation and characterization of the compounds from heart wood of root and root bark of Muntingia calabura. We have isolated six compounds, three from each extract and were identified as flavonoids. The bactericidal activity of these compounds found significant against tested bacterial strains. Among the tested compounds, 8-methoxy, 3ʹ,5ʹ7ʹ-trihydroxyflavone and 3,5,7-trihydroxyflavone (Galangin) showed paramount activity against MRSA. The results are compared with known standards gentamycin sulphate and cefixime.

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Protein‐Reactive Natural Products

Cited by 235 publications

References 363 publications

Phytochemical screening and antimicrobial activity of roots, stem-bark and leave extracts of Grewia mollis

Phytochemical screening and antimicrobial activity of roots, stem-bark and leave extracts of Grewia mollis

Inhibition of Fatty Acid Synthase in Prostate Cancer by Olristat, a Novel Therapeutic

Bactericidal activity of Flavonoids isolated from Muntingia calabura

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