Publications by authors named "Diana L Schmidt"
Article Synopsis
- Researchers discovered a new glucocorticoid receptor modulator (GRM) that uses a thioester payload, designed to be quickly processed by the liver to reduce overall exposure in the body.
- This new payload clears from the system 10 times faster than earlier versions, leading to much lower drug levels and less risk of systemic effects.
- The antibody-drug conjugate demonstrated significant effectiveness in reducing inflammation in various mouse models, indicating potential for effective subcutaneous administration and applications in treating inflammatory diseases.
Using a convergent synthetic route to enable multiple points of diversity, a series of glucocorticoid receptor modulators (GRM) were profiled for potency, selectivity, and drug-like properties . Despite covering a large range of diversity, profiling the nonconjugated small molecule was suboptimal and they were conjugated to a mouse antitumor necrosis factor (TNF) antibody using the MP-Ala-Ala linker. Screening of the resulting antibody drug conjugates (ADCs) provided a better assessment of efficacy and physical properties, reinforcing the need to conduct structure-activity relationship studies on the complete ADC.
View Article and Find Full Text PDFTransient receptor potential vanilloid 3 (TRPV3) is a Ca(2+)- and Na(+)-permeable channel with a unique expression pattern. TRPV3 is found in both neuronal and non-neuronal tissues, including dorsal root ganglia, spinal cord, and keratinocytes. Recent studies suggest that TRPV3 may play a role in inflammation, pain sensation, and skin disorders.
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