CALCIUM SENSING RECEPTORS, LIGANDS, COMPOSITIONS, AND METHODS OF USE
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Abstract
Described herein are compounds that can bind CaSR and/or a CaSR extracellular domain and formulations thereof. Also described herein are methods of inhibiting CaSR and/or treating a disease or disorder associated with a mutation in CaSR by administering a compound or formulation thereof described herein. Also described herein are assays that can be used to identify compounds that can bind an extracellular domain of CaSR.
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Citations
69 Claims
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1-52. -52. (canceled)
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53. A method of treating a disease in a subject, the method comprising the step of:
administering an amount of L-1,2,3,4-tetrahydronorharman-3-carboxylic acid (TNCA) to the subject in need thereof, wherein the subject has a disease associated with a mutation of the extracellular calcium-binding domain (ECD) of a calcium-sensing receptor protein (CaSR) or a disease where the symptom is abnormal CaSR expression, abnormal CaSR activity, or a symptom thereof in a subject in need thereof. - View Dependent Claims (54, 55, 56, 57, 58, 59, 60)
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61. A method comprising:
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contacting an extracellular calcium-binding domain (ECD) of a calcium sensing receptor protein (CaSR) with L-1,2,3,4-tetrahydronorharman-3-carboxylic acid (TNCA) and a candidate compound suspected of modulating the activity of the CaSR; and measuring CaSR activity or TNCA binding to the ECD. - View Dependent Claims (62, 63, 64, 65, 66, 67, 68)
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69. A method of modulating activity of a calcium sensing receptor protein (CaSR), the method comprising:
contacting the CaSR with L-1,2,3,4-tetrahydronorharman-3-carboxylic acid (TNCA) in an amount effective to modulate CaSR activity.
Specification