2012年8月11日星期六

Universal Detector Measures Major Biomolecule Classes

Neutralizer displacement assay works for small molecules as well as nucleic acids and proteins

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Dual vector for inhibition of human immunodeficiency virus

The present invention provides an expression vector for preventing or inhibiting HIV entry, fusion or replication in mammalian cells. In particular, the invention provides a recombinant retroviral vector that encodes an inhibitor of a HIV co-receptor, such as CCR5 or CXCR4, and a protein that inhibits HIV fusion to target cells...

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Bufexamac: a review of its pharmacological properties and therapeutic efficacy in inflammatory dermatoses.

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Bufexamac: a review of its pharmacological properties and therapeutic efficacy in inflammatory dermatoses.

Drugs. 1975;10(5-6):351-6

Authors: Brogden RN, Pinder RM, Sawyer PR, Speight TM, Avery GS

PMID: 1204506 [PubMed - indexed for MEDLINE]

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Pupil Dilation May Reveal Sexuality

Many experts believe that pupil dilation can reveal sexual orientation when a person looks at attractive people. Yet until now there has been no research supporting that theory. A new study by researchers at Cornell University, published in the journal PLoS ONE, measured pupillary changes of participants watching erotic videos by using a specialized infrared lens...

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Group Health Experience Shows How Practice And Research Can Inform Each Other

In the United States, clinicians are struggling to provide better and more affordable health care to more people - while keeping up with new scientific developments. The idea of a "learning health system" is one proposed solution for rapidly applying the best available scientific evidence in real-time clinical practice...

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2012年8月10日星期五

Bosutinib Buyer Beware

The wrong isomer has been sold under the name of the cancer-fighting compound

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[Cutaneous side-effects of nonsteroidal anti-inflammatory drugs (NSAID)].

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[Cutaneous side-effects of nonsteroidal anti-inflammatory drugs (NSAID)].

Z Rheumatol. 1995 Nov-Dec;54(6):405-12

Authors: Gebhardt M, Wollina U

Abstract
NSAID are able to induce cutaneous side-effects by both systematical and topical application. Nearly all kinds of exanthema are possible by any type of these drugs. However, particular substances are more likely to induce certain drug eruptions; aspirin and indometacine may induce urticarial reactions, whereas piroxicam can lead to phototoxic or photoallergic dermatitis. Contact dermatitis induced by topical NSAID is still rare but increasing. Ketoprofen and bufexamac were major contact allergens based on the number of reports, but local differences among different countries were observed. The diagnosis of drug reactions, especially in systemic drugs, remains a problem because reliable in vitro methods are not yet in use and skin test procedures do not work in most cases. Therefore, the case history is still the most useful tool in evaluating anamnestic allergic events. Prospective studies of drug compatibility as well as an improvement of side-effect reports are necessary to assess specific risks for several drugs.

PMID: 8578891 [PubMed - indexed for MEDLINE]

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Therapeutic inhibitor of vascular smooth muscle cells

Methods are provided for inhibiting stenosis following vascular trauma or disease in a mammalian host, comprising administering to the host a therapeutically effective dosage of a therapeutic conjugate containing a vascular smooth muscle binding protein that associates in a specific manner with a cell surface of the vascular smooth muscle cell,...

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[Bufexamac-induced pigmented purpuric eruption].

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[Bufexamac-induced pigmented purpuric eruption].

Hautarzt. 2009 May;60(5):424-7

Authors: Waltermann K, Marsch WCh, Kreft B

Abstract
We report on a case of a bufexamac-induced allergic contact dermatitis with hematogenous dissemination presenting with the clinical and histological picture of a pigmented purpuric eruption. To our knowledge this is the first report on a bufexamac-induced pigmented purpuric dermatosis. It represents a further example of the clinical variety of cutaneous side-effects caused by bufexamac.

PMID: 19093092 [PubMed - indexed for MEDLINE]

Bufexamac

2012年8月9日星期四

[Current contact allergens].

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[Current contact allergens].

Z Hautkr. 1987 Dec 1;62(23):1631-4, 1637-8

Authors: Frosch PJ

Abstract
We present the patch test results of 2,623 patients treated at the Department of Dermatology, University of Heidelberg, from July, 1984 to June, 1986. One test at least was positive in 680 patients (25.9%). 257 allergens produced a total of 1,450 positive reactions. (average: 2.1 per patient). 9.7% of the allergens caused 64.4% of the positive reactions. The 5 most frequent allergens were nickel sulfate, balsam of Peru, formaldehyde, neomycin sulfate, and cobalt sulfate. Mixed fragrances and Kathon CG were among the 20 most frequent allergens though only tested during half of the study period. Glyceril monothioglycolate was the leading allergen with hairdressers. Other allergens clinically relevant were rubber gloves, bufexamac, bronopol, and propolis.

PMID: 2964130 [PubMed - indexed for MEDLINE]

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War On Weeds

New crop traits that allow use of older herbicides may help farmers manage resistant weeds

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Pharmaceutical composition, methods for treating and uses thereof

The invention relates to the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia using a SGLT-2 inhibitor. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions....

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[Role of chemotherapy in castration-resistant prostate cancer: are there new approaches?].

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[Role of chemotherapy in castration-resistant prostate cancer: are there new approaches?].

Urologe A. 2012 Jan;51(1):39-43

Authors: De Santis M, Bachner M

Abstract
Chemotherapy options for the treatment of metastatic castration-resistant prostate cancer (CRPC) have been very limited for many decades. Until 2004, only mitoxantrone was approved, providing palliation, but no survival benefit. With the introduction of docetaxel, the landscape of chemotherapy for CRPC changed substantially. Prednisone and three-weekly docetaxel showed an overall survival (OS) benefit compared to mitoxantrone plus prednisone, in addition to a significant improvement of quality of life and pain reduction. Further strategies to treat CRPC with chemotherapy include reinduction with docetaxel in responding patients and the use of cabazitaxel, a novel semi-synthetic microtubule inhibitor, in the docetaxel-refractory population. This review article is meant to guide physicians through the optimal use of chemotherapy in CRPC patients in daily clinical practice.

PMID: 22258375 [PubMed - indexed for MEDLINE]

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2012年8月8日星期三

The topical anti-inflammatory effects of piroxicam in rodents.

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The topical anti-inflammatory effects of piroxicam in rodents.

Agents Actions. 1980 Jun;10(3):246-51

Authors: Larson DL, Lombardino JG

Abstract
Piroxicam is a structurally novel, long-acting anti-inflammatory drug with potent activity following oral administration in animal models of inflammation and in human inflammatory diseases. The present studies, performed in rats, demostrate that topically applied piroxicam is a potent inhibitor of inflammation induced by either carrageenin or complete Freund's adjuvant. Comparable potencies (ED50 approximately 1--5 mg/kg) were obtained for topically and orally administered piroxicam in these models of inflammation. The potency of topical piroxicam exceeds that of topically applied bufexamac or phenylbutazone in the rat adjuvant arthritis model.

PMID: 7405751 [PubMed - indexed for MEDLINE]

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Building A Jellyfish

Biomimetics: Researchers use polymer sheet, protein, and heart cells to replicate the swim stroke of the marine animal

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Despite Law, Critically Ill Uninsured Americans Still At Risk Of Being Turned Away From Hospitals

Despite a twenty-five year old law that bans "patient dumping" the practice continues to put uninsured Americans at risk, according to a national team of researchers led by a professor at the George Washington School of Public Health and Health Services. Patient dumping is the practice of turning away or transferring uninsured patients with emergency medical conditions...

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Biomarkers Help Pinpoint Mechanisms, Predict Outcomes In Depression

Scientists have discovered a biological marker that may help to identify which depressed patients will respond to an experimental, rapid-acting antidepressant. The brain signal, detectable by noninvasive imaging, also holds clues to the agent's underlying mechanism, which are vital for drug development, say National Institutes of Health researchers...

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Kinase inhibitors

The present invention provides a new group of protein kinase inhibitors, pyrropyrimidine and pyrazolopyrimidine derivatives, and pharmaceutically acceptable salts and prodrugs thereof that are useful for treating cell proliferative disease and disorder such as cancer, autoimmune diseases, infection, cardiovascular disease and neurodegenerative disease and disorder. The present invention provides methods for...

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2012年8月7日星期二

[A common and insidious side-effect: allergic contact dermatitis caused by bufexamac used in the treatment of dermatitis. Results from the Information Network of Departments of Dermatology (IDVK)].

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[A common and insidious side-effect: allergic contact dermatitis caused by bufexamac used in the treatment of dermatitis. Results from the Information Network of Departments of Dermatology (IDVK)].

Dtsch Med Wochenschr. 2005 Dec 16;130(50):2881-6

Authors: Schnuch A, Gefeller O, Uter W

Abstract
BACKGROUND AND OBJECTIVE: Bufexamac is a non-steroidal, anti-inflammatory drug used in the topical treatment of atopic dermatitis, stasis dermatitis and perianal eczema. The substance is known to cause severe allergic contact dermatitis (ACD) as an adverse effect (AE), which may be indistinguishable from the eczema which is to be treated. Hence the diagnosis of this AE is often considerably delayed. In order to estimate the quantitative importance of ACD to bufexamac, data of the Information Network of (German) Departments of Dermatology (IVDK) from July 1999 to December 2004 were analysed.
PATIENTS AND METHODS: During the study period, 39,392 unselected patients from 40 German departments of the IVDK were patch tested with bufexamac (5 % pet). The results of the reading after 72 hours were analysed. The dichotomized patch test result was further assessed for possible risk factors from the patients' history and clinical diagnosis by Poisson regression analysis.
RESULTS: In 560 of 39,392 patients contact allergy to bufexamac was diagnosed, i. e. 1.4 % (95 % confidence interval: 1.3 - 1.5), standardized for sex and age. The Poisson regression analysis revealed a significantly increased risk associated with the following factors: multiple sensitization, perianal eczema, underlying atopic dermatitis, leg dermatitis, female gender and residence in areas of Germany other than Eastern Germany. The latter observation can be explained by low prescription rates in Eastern Germany.
CONCLUSION: Bufexamac is an important allergen. Extrapolating the frequency of 1.4 % in our data to the whole German population by the CE-DUR approach yields an estimate of about 6000 cases per year. In view of the high frequency of sensitization, the pitfalls in diagnosis, the severity of the course of disease and the lack of efficacy of this drug, the risk to benefit ratio is obviously critical.

PMID: 16342011 [PubMed - indexed for MEDLINE]

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Single Amino Acid Forms Fibrils

Amyloid Disease: Phenylalanine aggregates may have a role in phenylketonuria

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Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors

or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.




The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of...

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Lactam compounds useful as protein kinase inhibitors

The present invention provides novel compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases....

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Thiazolopyrimidinone derivatives as pi3 kinase inhibitors

and derivatives thereof useful for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K}, PI3K?, and/or PI3K?.




This invention relates to novel compounds of formula (I):...

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2012年8月6日星期一

Medical Staff Often Miss Alcohol Problems If Patients Are Not Intoxicated

Medical staff struggle to spot problem drinking in their patients unless they are already intoxicated, according to research by the University of Leicester...

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Oligonucleotides inhibiting cellular migration

Oligonucleotides inhibiting cellular migration, and the use of at least one inhibitor of protein expression, which inhibits the expression of TSP1 protein, or a protein, which controls the expression of TSP1 or mediates the activity of TSP1, or one inhibitor of protein activity, this inhibitor inhibiting the activity of the TSP1...

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Imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine derivatives and their use as protein kinase inhibitors

or a stereoisomer, prodrug or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. Compositions and methods for using the same in the treatment of cancer and other Pim kinase-associated conditions are also disclosed.




The present invention provides protein kinase inhibitors comprising imidazo[1,2-b]pyridazine and pyrazolo[1,5-a]pyrimidine compounds of...

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Cocaine-Like Action Of Bath Salts

Over the last 5 years, synthetic stimulants known as "bath salts" have become more popular amongst recreational drug users because of their easy unrestricted availability over the Internet and at convenience stores. There are virtually no regulations in place to restrict the sale of these stimulants...

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Biocatalysis

As pharmaceutical manufacturers increasingly use enzymatic reactions in their processes, a robust business model still eludes biocatalysis companies

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2012年8月5日星期日

Biomarkers for iap inhibitor compounds

A method to predict which patients will respond to a IAP inhibiting compound comprising administering an IAP inhibitor compound to a patient/and measuring IL1B, Lymphotoxin alpha (LTa), TWEAK, LIGHT, Fas, TNF alpha or TRAIL levels....

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Triazole compounds useful as protein kinase inhibitors

wherein Z1 is nitrogen or CR9 and Z2 is nitrogen or CH, provided that at least one of Z1 and Z2 is nitrogen; G is Ring C or Ring D; Ring C is selected from a phenyl, pyridinyl, pyrimidinyl, pyridazinyl, pyrazinyl, or 1,2,4-triazinyl ring, wherein said Ring C has one or...

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Shrub-Mouse Duo Sows Seeds

Wasabi-like mustard sting thwarts animals? seed eating, making them spit out seeds instead

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Childhood Abuse And Age At Menarche Linked

Researchers from Boston University School of Medicine (BUSM) have found an association between childhood physical and sexual abuse and age at menarche. The findings are published online in the Journal of Adolescent Health...

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Responsiveness to angiogenesis inhibitors

The present invention relates to methods for improving the overall survival of a patient suffering from a malignant disease or a disease involving physiological and pathological angiogenesis by treatment with an angiogenesis inhibitor, such as bevacizumab, by determining the presence of one or more variant alleles of the vascular endothelial growth...

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