Preclinical and clinical studies on bryostatins, a class of marine-derived protein kinase C modulators: A mini-review.

Preclinical and clinical studies on bryostatins, a class of marine-derived protein kinase C modulators: A mini-review. Curr Top Med Chem. 2020 Mar 25;: Authors: Raghuvanshi R, Bharate S Abstract Bryostatins are complex macrolactones isolated from marine organism Bryozoan Bugula neritina. They are potent modulators of protein kinase C isozymes (PKCα: ki = 1.3-188 nM), and are one of the most extensively investigated marine natural products in clinical trials. Although ~21 natural bryostatins have been isolated, however only bryostatin-1 (1) has received much interest among medicinal chemists and clinicians. The structure-activity relationship of bryostatins has been well established, with the identification of key pharmacopjoric features important for PKC modulation. The low natural abundance and long synthetic route has promoted medicinal chemists to come-up with simplified analogs. Bryostatin skeleton primarily comprises three pyran rings connected to each other to form a macrocyclic lactone. The simplest analog 27 contains only one pyran, which is also able to modulate the PKCα activity, however the cyclic framework appears to be essential for desired potency. Another simplified analog 17 ("picolog") exhibited potent in vitro and in-vivo efficacy against lymphoma. Bryostatin-1 (1) has shown acceptable IV pharmacokinetic profile in mice and displayed promising in-vivo efficacy in mice models of various cancers and Alzheimer's disea...
Source: Current Topics in Medicinal Chemistry - Category: Chemistry Authors: Tags: Curr Top Med Chem Source Type: research

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Publication date: Available online 3 June 2020Source: Journal of the American College of RadiologyAuthor(s): Ruth C. Carlos, Katy Lowry, Gelareh Sadigh
Source: Journal of the American College of Radiology - Category: Radiology Source Type: research
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Source: Spine - Category: Orthopaedics Tags: HEALTH SERVICES RESEARCH Source Type: research
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Source: Spine - Category: Orthopaedics Tags: LITERATURE REVIEW Source Type: research
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Source: Spine - Category: Orthopaedics Tags: SURGERY Source Type: research
Authors: Carkic J, Nikolic N, Nisevic J, Lazarevic M, Kuzmanovic-Pficer J, Jelovac D, Milasin J Abstract Oral carcinoma is the sixth most common malignancy worldwide, with survival rates of approximately 50%. The major type of oral cancer, present in 90% of the cases, is oral squamous cell carcinoma (OSCC). The genetic background predisposing an individual to OSCC is complex and largely unknown. Studies have suggested that endothelial nitric oxide synthase (eNOS) gene polymorphisms modulate the cancer risk, prompting us to assess the impact of three functional eNOS gene polymorphisms on OSCC risk. The present study...
Source: Journal of oral science - Category: Dentistry Tags: J Oral Sci Source Type: research
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Source: Current Opinion in Clinical Nutrition and Metabolic Care - Category: Nutrition Tags: GENES AND CELL METABOLISM: Edited by Anastasia Z. Kalea and Dorothy Klimis-Zacas Source Type: research
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Source: Current Opinion in Hematology - Category: Hematology Tags: HEMATOPOIESIS: Edited by Hal E. Broxmeyer and Maegan L. Capitano Source Type: research
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Source: Journal of Clinical Gastroenterology - Category: Gastroenterology Tags: ALIMENTARY TRACT: Original Articles Source Type: research
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Source: Diseases of the Colon and Rectum - Category: Gastroenterology Tags: Technical Note Source Type: research
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Source: Fight Aging! - Category: Research Authors: Tags: Newsletters Source Type: blogs
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