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Pharmaceuticals, Volume 5, Issue 7 (July 2012), Pages 674-778

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Research

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Open AccessArticle Pertuzumab Increases 17-AAG-Induced Degradation of ErbB2, and This Effect Is Further Increased by Combining Pertuzumab with Trastuzumab
Pharmaceuticals 2012, 5(7), 674-689; doi:10.3390/ph5070674
Received: 20 April 2012 / Revised: 13 June 2012 / Accepted: 21 June 2012 / Published: 28 June 2012
Cited by 6 | PDF Full-text (620 KB) | HTML Full-text | XML Full-text
Abstract
ErbB2 is an important oncogenic protein involved in carcinogenesis of, among others, breast, gastric, and ovarian carcinoma. Over-expression of ErbB2 is found in almost 20% of breast cancers, and this results in proliferative and anti-apoptotic signalling. ErbB2 is therefore an important treatment [...] Read more.
ErbB2 is an important oncogenic protein involved in carcinogenesis of, among others, breast, gastric, and ovarian carcinoma. Over-expression of ErbB2 is found in almost 20% of breast cancers, and this results in proliferative and anti-apoptotic signalling. ErbB2 is therefore an important treatment target. Antibodies recognizing full-length ErbB2 are clinically established, and drugs targeting the ErbB2 stabilizing heat shock protein 90 (Hsp90) are under clinical evaluation. We have investigated effects of the ErbB2-binding antibodies trastuzumab and pertuzumab alone and in combination, as well as the effect of the antibodies in combination with the Hsp90 inhibitor 17-AAG. Our results confirm the notion that combination of different ErbB2-binding antibodies more efficiently down-regulates ErbB2 than does one antibody in isolation. Additionally, our data demonstrate that ErbB2 is most efficiently down-regulated upon incubation with anti-ErbB2 antibodies in combination with Hsp90 inhibitors. The combination of anti-ErbB2 antibodies, and especially the combination of antibodies with 17-AAG, did also increase the inhibition of Akt activation of either agent, which could suggest an anti-proliferative effect. In such case, combining these agents could be beneficial in treatment of tumors not responding to trastuzumab only. Full article
(This article belongs to the Special Issue Hsp90 Inhibitors)
Open AccessArticle Synthesis, Reactions and Evaluation of the Antimicrobial Activity of Some 4-(p-Halophenyl)-4H-naphthopyran, Pyranopyrimidine and Pyranotriazolopyrimidine Derivatives
Pharmaceuticals 2012, 5(7), 745-757; doi:10.3390/ph5070745
Received: 14 May 2012 / Revised: 15 June 2012 / Accepted: 21 June 2012 / Published: 12 July 2012
Cited by 5 | PDF Full-text (187 KB) | HTML Full-text | XML Full-text
Abstract
A series of naphthopyran derivatives 3a–f were prepared. Reaction of 2-amino-4-(p-chlorophenyl)-7-methoxy-4H-naphtho[2,1-b]pyran-3-carbonitrile (3b) with Ac2O afforded two products, 2-acetylamino-7-methoxy-4-(p-chlorophenyl)-4H-naphtho-[2,1-b]pyran-3-carbonitrile (4) and 10,11-dihydro-3-methoxy-9-methyl-12-(p-chloro-phenyl)-12 [...] Read more.
A series of naphthopyran derivatives 3a–f were prepared. Reaction of 2-amino-4-(p-chlorophenyl)-7-methoxy-4H-naphtho[2,1-b]pyran-3-carbonitrile (3b) with Ac2O afforded two products, 2-acetylamino-7-methoxy-4-(p-chlorophenyl)-4H-naphtho-[2,1-b]pyran-3-carbonitrile (4) and 10,11-dihydro-3-methoxy-9-methyl-12-(p-chloro-phenyl)-12H-naphtho[2,1-b]pyran[2,3-d]pyrimidine-11-one (5) and treatment of 3b with benzoyl chloride gave the pyranopyrimidin-11-one derivative 6. While treatment of 3b with formamide afforded 11-amino-3-methoxy-12-(p-chlorophenyl)-12H-naphtho[2,1-b]pyrano[2,3-d]pyrimidine (7). Reaction of 3b with triethyl orthoformate gave the corresponding 2-ethoxymethyleneamino-7-methoxy-4-(p-chlorophenyl)-4H-naphtho-[2,1-b]pyran-3-carbonitrile (8). Hydrazinolysis of 8 in EtOH at room temperature yielded 10-amino-10,11-dihydro-11-imino-3-methoxy-12-(p-chlorophenyl)-12H-naphtho[2,1-b]pyrano-[2,3-d]pyrimidine (9), while aminolysis of 8 with methylamine or dimethylamine gave the corresponding pyranopyrimidine and N,N-dimethylaminomethylene derivatives 10 and 11. Condensation of 9 with some carboxylic acid derivatives afforded triazolopyrimidine derivatives 12–16, while reaction of 9 with benzaldehyde gave 10-benzalamino-10,11-dihydro-11-imino-3-methoxy-12-(p-chlorophenyl)12H-naphtho[2,1-b]pyrano[2,3-d]pyrimidine (17). The structures of the newly synthesized compounds were confirmed by spectral data. The synthesized compounds were also screened for their antimicrobial activity. Full article

Review

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Open AccessReview Chemotherapeutic Interventions Against Tuberculosis
Pharmaceuticals 2012, 5(7), 690-718; doi:10.3390/ph5070690
Received: 15 May 2012 / Revised: 12 June 2012 / Accepted: 21 June 2012 / Published: 28 June 2012
Cited by 5 | PDF Full-text (227 KB) | HTML Full-text | XML Full-text
Abstract
Tuberculosis is the second leading cause of infectious deaths globally. Many effective conventional antimycobacterial drugs have been available, however, emergence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) has overshadowed the effectiveness of the current first and second line drugs. Further, [...] Read more.
Tuberculosis is the second leading cause of infectious deaths globally. Many effective conventional antimycobacterial drugs have been available, however, emergence of multidrug-resistant tuberculosis (MDR-TB) and extensively drug-resistant tuberculosis (XDR-TB) has overshadowed the effectiveness of the current first and second line drugs. Further, currently available agents are complicated by serious side effects, drug interactions and long-term administration. This has prompted urgent research efforts in the discovery and development of new anti-tuberculosis agent(s). Several families of compounds are currently being explored for the treatment of tuberculosis. This review article presents an account of the existing chemotherapeutics and highlights the therapeutic potential of emerging molecules that are at different stages of development for the management of tuberculosis disease. Full article
(This article belongs to the Special Issue Antituberculosis Drugs)
Open AccessReview Association of Marijuana Use and Cyclic Vomiting Syndrome
Pharmaceuticals 2012, 5(7), 719-726; doi:10.3390/ph5070719
Received: 11 May 2012 / Revised: 13 June 2012 / Accepted: 19 June 2012 / Published: 29 June 2012
Cited by 3 | PDF Full-text (48 KB) | HTML Full-text | XML Full-text
Abstract
Cannabis use has become one of the most commonly abused drugs in the world. It is estimated that each year 2.6 million individuals in the USA become new users and most are younger than 19 years of age. Reports describe marijuana use [...] Read more.
Cannabis use has become one of the most commonly abused drugs in the world. It is estimated that each year 2.6 million individuals in the USA become new users and most are younger than 19 years of age. Reports describe marijuana use as high as 40–50% in male Cyclic Vomiting Syndrome patients. It is this interest in cannabis in the World, coupled with recognition of a cyclic vomiting illness associated with its chronic use that beckons a review of the most current articles, as well as a contribution from our own experiences in this area. The similarities we have demonstrated for both cannibinoid hyperemesis syndrome and cyclic vomiting make the case that cannibinoid hyperemesis syndrome is a subset of patients who have the diagnoses of cyclic vomiting syndrome and the role of marijuana should always be considered in the diagnosis of CVS, particularly in males. Full article
(This article belongs to the Special Issue Medical Marijuana)
Open AccessReview Probiotics and Atopic Dermatitis in Children
Pharmaceuticals 2012, 5(7), 727-744; doi:10.3390/ph5070727
Received: 12 April 2012 / Revised: 26 June 2012 / Accepted: 29 June 2012 / Published: 6 July 2012
Cited by 6 | PDF Full-text (181 KB) | HTML Full-text | XML Full-text
Abstract
There is increasing interest in the potential beneficial role of probiotic supplementation in the prevention and treatment of atopic diseases in children. Probiotics are defined as ingested live microorganisms that, when administered in an adequate amount, confer a health benefit to the [...] Read more.
There is increasing interest in the potential beneficial role of probiotic supplementation in the prevention and treatment of atopic diseases in children. Probiotics are defined as ingested live microorganisms that, when administered in an adequate amount, confer a health benefit to the host. They are mainly represented by Lactobacilli and Bifidobacteria. Several epidemiological data demonstrate that intestinal microflora of atopic children is different from the one of healthy children. Many literature data show that probiotics may modulate the intestinal microflora composition and may have immunomodulatory effect. Based on this hypothesis, probiotics are supposed to confer benefits to allergic diseases. Administration of probiotics when a natural population of indigenous intestinal bacteria is still developing could theoretically influence immune development by favoring the balance between Th1 and Th2 inflammatory responses. For this reason, some studies have evaluated the potential impact of probiotics supplementation in the prevention of atopic dermatitis, with contrasting results. Clinical improvement in immunoglobulin (Ig)E-sensitized (atopic) eczema following probiotic supplementation has been reported in some published studies and the therapeutic effects of probiotics on atopic dermatitis seemed to be encouraging. However, as far as the usefulness of probiotics as a prevention strategy is concerned, results are still inconclusive. In fact, the clinical benefits of probiotic therapy depend upon numerous factors, such as the type of bacteria, dosing regimen, delivery method and other underlying host factors, such as age and diet. More studies are still needed to definitively prove the role of probiotics in the treatment of allergic eczema. Full article
(This article belongs to the Special Issue Probiotics and Prebiotics)
Open AccessReview The Influence of Estrogens on the Biological and Therapeutic Actions of Growth Hormone in the Liver
Pharmaceuticals 2012, 5(7), 758-778; doi:10.3390/ph5070758
Received: 4 June 2012 / Revised: 9 July 2012 / Accepted: 12 July 2012 / Published: 19 July 2012
PDF Full-text (763 KB) | HTML Full-text | XML Full-text
Abstract
GH is main regulator of body growth and composition, somatic development, intermediate metabolism and gender-dependent dimorphism in mammals. The liver is a direct target of estrogens because it expresses estrogen receptors which are connected with development, lipid metabolism and insulin sensitivity, hepatic [...] Read more.
GH is main regulator of body growth and composition, somatic development, intermediate metabolism and gender-dependent dimorphism in mammals. The liver is a direct target of estrogens because it expresses estrogen receptors which are connected with development, lipid metabolism and insulin sensitivity, hepatic carcinogenesis, protection from drug-induced toxicity and fertility. In addition, estrogens can modulate GH actions in liver by acting centrally, regulating pituitary GH secretion, and, peripherally, by modulating GHR-JAK2-STAT5 signalling pathway. Therefore, the interactions of estrogens with GH actions in liver are biologically and clinically relevant because disruption of GH signaling may cause alterations of its endocrine, metabolic, and gender differentiated functions and it could be linked to dramatic impact in liver physiology during development as well as in adulthood. Finally, the interplay of estrogens with GH is relevant because physiological roles these hormones have in human, and the widespread exposition of estrogen or estrogen-related compounds in human. This review highlights the importance of these hormones in liver physiology as well as how estrogens modulate GH actions in liver which will help to improve the clinical use of these hormones. Full article
(This article belongs to the Special Issue Hormone Therapy)
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