Novel bone-targeted parathyroid hormone-related peptide antagonists inhibit breast cancer bone metastases
T Ponnapakkam, M Anbalagan, RE Stratford Jr… - Anti-Cancer …, 2021 - journals.lww.com
Patients with advanced breast cancer often develop bone metastases. Treatment is limited
to palliative care. Parathyroid hormone (PTH)/parathyroid hormone-related peptide (PTHrP)
antagonists for bone metastases failed clinically due to short half-life and inadequate
concentration in bone. We synthesized two novel PTHrP antagonists fused to an inert
bacterial collagen binding domain (CBD) that directs drugs to bone. PTH (7-33)-CBD is an N-
terminal truncated PTHrP antagonist.[W2] PTH (1-33)-CBD is an PTHrP inverse-agonist. The …
to palliative care. Parathyroid hormone (PTH)/parathyroid hormone-related peptide (PTHrP)
antagonists for bone metastases failed clinically due to short half-life and inadequate
concentration in bone. We synthesized two novel PTHrP antagonists fused to an inert
bacterial collagen binding domain (CBD) that directs drugs to bone. PTH (7-33)-CBD is an N-
terminal truncated PTHrP antagonist.[W2] PTH (1-33)-CBD is an PTHrP inverse-agonist. The …