That is so cool! but the article needs to come with a translation into Standard (non research based) English for the rest of us :-) IT is nice to know what it is you are working on.
"This moiety is the result of a 10-year comprehensive scientific program at Tularik and Amgen resulting in what could be a significant clinical advancement in the treatment of Type 2 Diabetes. Insulin resistance is the key etiological feature to the onset and subsequent progression of the disease and as a true SPPARM, INT131 promises insulin sensitization benefits without the edema, fluid retention and weight gain exhibited by the TZDs."
*** PPARg is a natural sensor for fatty acids in the body and impacts the body's response to food including how insulin is released and responded to. It is also the target of drugs like Avandia and Actos, used by some diabetics to control blood sugar levels by improving their body's sensitivity to the insulin they already make. Those drugs (like Avandia) are called TZD's for a chemical structure common to both. One common side-effect of TZD's is that the person has an increase in body weight and fluid retention that can actually make their diabetes worse and is also a contributor to heart disease issues. The Tularik compound has a very different chemical structure and appears to selectively activate some features of the PPARg receptor and to block other features, depending on a variety of things like tissue distribution and others that are not yet understood. This selectivity is indicated in the SPPARM label for 'Selective PPARg Modulator'. Modulator meaning that some effects are blocked and others are activated. Recently the TZD's have been issued warnings about the heart disease issues and their sales have dropped off significantly, so perhaps there is market room for another oral diabetes drug that works at this receptor.
2 comments:
That is so cool! but the article needs to come with a translation into Standard (non research based) English for the rest of us :-) IT is nice to know what it is you are working on.
"This moiety is the result of a 10-year comprehensive scientific program at Tularik and Amgen resulting in what could be a significant clinical advancement in the treatment of Type 2 Diabetes. Insulin resistance is the key etiological feature to the onset and subsequent progression of the disease and as a true SPPARM, INT131 promises insulin sensitization benefits without the edema, fluid retention and weight gain exhibited by the TZDs."
***
PPARg is a natural sensor for fatty acids in the body and impacts the body's response to food including how insulin is released and responded to. It is also the target of drugs like Avandia and Actos, used by some diabetics to control blood sugar levels by improving their body's sensitivity to the insulin they already make. Those drugs (like Avandia) are called TZD's for a chemical structure common to both. One common side-effect of TZD's is that the person has an increase in body weight and fluid retention that can actually make their diabetes worse and is also a contributor to heart disease issues. The Tularik compound has a very different chemical structure and appears to selectively activate some features of the PPARg receptor and to block other features, depending on a variety of things like tissue distribution and others that are not yet understood. This selectivity is indicated in the SPPARM label for 'Selective PPARg Modulator'. Modulator meaning that some effects are blocked and others are activated. Recently the TZD's have been issued warnings about the heart disease issues and their sales have dropped off significantly, so perhaps there is market room for another oral diabetes drug that works at this receptor.
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