[HTML][HTML] Design and optimization of oestrogen receptor PROTACs based on 4-hydroxytamoxifen
G Loren, I Espuny, A Llorente, C Donoghue… - European Journal of …, 2022 - Elsevier
In the last four decades, treatment of oestrogen receptor positive (ER+) breast cancer (BCa),
has focused on targeting the estrogenic receptor signaling pathway. This signaling function
is pivotal to sustain cell proliferation. Tamoxifen, a competitive inhibitor of oestrogen, has
played a major role in therapeutics. However, primary and acquired resistance to hormone
blockade occurs in a large subset of these cancers, and new approaches are urgently
needed. Aromatase inhibitors and receptor degraders were approved and alternatively …
has focused on targeting the estrogenic receptor signaling pathway. This signaling function
is pivotal to sustain cell proliferation. Tamoxifen, a competitive inhibitor of oestrogen, has
played a major role in therapeutics. However, primary and acquired resistance to hormone
blockade occurs in a large subset of these cancers, and new approaches are urgently
needed. Aromatase inhibitors and receptor degraders were approved and alternatively …
Design and Optimization of Oestrogen Receptor PROTACs Based on 4-Hydroxytamoxifen
A Riera, G Loren, I Espuny, A Llorente… - Available at SSRN … - papers.ssrn.com
In the last four decades, treatment of oestrogen receptor positive (ER+) breast cancer (BCa),
has focused on targeting the estrogenic receptor signaling pathway. This signaling function
is pivotal to sustain cell proliferation. Tamoxifen, a competitor inhibitor of oestrogen, has
played a major role in therapeutics. However, primary and acquired resistance to hormone
blockade occurred in a large subset of these cancers, and new approaches were urgently
needed. Aromatase inhibitors and receptor degraders were approved and alternatively …
has focused on targeting the estrogenic receptor signaling pathway. This signaling function
is pivotal to sustain cell proliferation. Tamoxifen, a competitor inhibitor of oestrogen, has
played a major role in therapeutics. However, primary and acquired resistance to hormone
blockade occurred in a large subset of these cancers, and new approaches were urgently
needed. Aromatase inhibitors and receptor degraders were approved and alternatively …
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