Assessment of the Free Binding Energy of 1,25-Dihydroxyvitamin D(3) and Its Analogs With the Human VDR Receptor Model.
Assessment of the free binding energy of 1,25-dihydroxyvitamin D(3) and its analogs with the human VDR receptor model.
Filed under: Drug and Alcohol Rehabilitation
Acta Biochim Pol. 2012 Oct 16;
Kamel K, Kolinski A
1,25-dihydroxyvitamin D(3) has quite significant anticancer properties, but its strong calcemic effect in principle excludes it as a potential anticancer drug. Currently, a lot of effort is being devoted to develop potent anticancer analogs of 1,25-dihydroxyvitamin D(3) that would not induce hypercalcemia during therapy. In this work, the free binding energy of the VDR receptor with 1,25-dihydroxyvitamin D(3) and its three potent analogs (EB 1089, KH 1060 and RO 25-9022) is calculated and compared with each other. With this approach, we could estimate the relative binding affinity of the most potent analog, RO 25-9022, and also revealed a quite distinct mechanism of its interaction with VDR.
HubMed – drug
Some heterocyclic thione derivatives exhibit anticoccidial activity by inhibiting glycosidases.
Filed under: Drug and Alcohol Rehabilitation
Acta Biochim Pol. 2012 Oct 16;
Balbaa M, Abd El-Hady N, Taha N, El Ashry ES
Coccidiosis is one of the most common parasitic diseases affecting many species of domestic animals. This disease has a major economic significance and the search for new compounds having anticoccidial activity is of great importance. In this article, different levels of protection from coccidian infection by Eimeria stiedae were developed in rabbits by treatment with compounds incorporating the skeleton of thiourea. These compounds include 4,5-diphenylimidazole-2-thione (1), 4,5-Diphenyl-1,2,4-triazole-3-thiol (2) and 5-(2-Hydroxyphenyl)-4-phenyl-1,2,4-triazole-3-thiol (3) compared to the anticoccidial drug toltrazuril as a reference compound. Compounds 1-3 inhibit coccidiosis-induced activity of ?-glucosidase. The protection from coccidial infection by compound 1 was higher than that shown for compounds 2 and 3. These data suggest that diazole and triazole thione derivatives have a mimetic effect for anticoccidial drugs through their inhibition of glycosidases.
HubMed – drug
A risperidone-induced prolactinoma resolved when a woman with schizoaffective disorder switched to ziprasidone: a case report.
Filed under: Drug and Alcohol Rehabilitation
Innov Clin Neurosci. 2012 Sep; 9(9): 21-4
Arcari GT, Mendes AK, Sothern RB
Antipsychotic drug therapy, e.g., risperidone, can be associated with endocrine abnormalities, including an increase in serum prolactin level (sPrl) due to a drug-induced benign pituitary tumor (prolactinoma). A few case reports have noted a resolution of hyperprolactinemia and prolactinoma after cessation of risperidone treatment. We report a similar finding for a woman with schizoaffective disorder, manic type.Due to a neurological disorder involving the tongue (tardive dyskinesia), a woman with schizoaffective disorder switched from 50mg thioridazine after 21 years to 2mg of risperidone at bedtime for 10 years. Elevated sPrl was noted in June and August 2005 (83.8 and 100.1µg/L; normal: 3.4-24.1µg/L) and a cranial magnetic resonance imaging scan showed evidence of a small area of decreased signal in the pituitary gland consistent with a microadenoma. The subject transitioned slowly to ziprasidone and off risperidone in October and November of 2005. The prolactinoma completely resolved with the switch to ziprasidone. It is recommended that sPrl be measured annually in patients taking antipsychotic drugs to test for any indication of pituitary prolactinoma that could suggest the need to switch the primary treatment to another drug.
HubMed – drug
Bahareh Amidi at TEDxAbuDhabi – American-Iranian spiritual poet of light — Bahareh Amidi. TEDxAbuDhabi May 26, 2012 Having grown up in the USA, Bahareh has travelled across the world and currently lives in the Middle East (Abu Dhabi, UAE). Her Eastern roots, Western upbringing and years spent living in the Middle East have given her unique perspective on the challenges and triumphs of life, death, and relationships, and a universal appeal to her writing. She studied Philosophy in Menlo College, California; majored in Counseling Psychology from College of Notre Dame — Belmont, California; and, holds a Doctorate in Educational Psychology from Catholic University — Washington DC. Her area of study was “The Self-Image and Acculturation of Iranian-American Adolescents growing up in the US”. Bahareh has firsthand experience and a deep engagement with the human condition at various stages of life starting from her volunteering work with the elderly at Sharon Heights Convalescent Hospital — Menlo Park, California through her teenage years; her counseling and training in suicide prevention at the Crisis Center — Burlingame, California; working with children at the Stanford Children’s Health Center, California; researching drug and alcohol rehabilitation at Sequoia Hospital — Redwood City, California; teaching human development at Catholic University — Washington DC; and, counseling victims of gender abuse at the Women’s Safe House in Abu Dhabi, UAE.
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