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FDA-approved small-molecule kinase inhibitors
Kinases have emerged as one of the most intensively pursued targets in current
pharmacological research, especially for cancer, due to their critical roles in cellular …
pharmacological research, especially for cancer, due to their critical roles in cellular …
Antibody-drug conjugates targeting the human epidermal growth factor receptor family in cancers
J Yu, T Fang, C Yun, X Liu, X Cai - Frontiers in Molecular Biosciences, 2022 - frontiersin.org
Members of the human epidermal growth factor receptor (HER) family, which includes HER1
(also known as EGFR), HER2, HER3 and HER4, have played a central role in regulating cell …
(also known as EGFR), HER2, HER3 and HER4, have played a central role in regulating cell …
Structures of the HER2–HER3–NRG1β complex reveal a dynamic dimer interface
Human epidermal growth factor receptor 2 (HER2) and HER3 form a potent pro-oncogenic
heterocomplex,–upon binding of growth factor neuregulin-1β (NRG1β). The mechanism by …
heterocomplex,–upon binding of growth factor neuregulin-1β (NRG1β). The mechanism by …
Genomic characterization of primary invasive lobular breast cancer
Purpose Invasive lobular breast cancer (ILBC) is the second most common histologic
subtype after invasive ductal breast cancer (IDBC). Despite clinical and pathologic …
subtype after invasive ductal breast cancer (IDBC). Despite clinical and pathologic …
Targeting HER2 in colorectal cancer: The landscape of amplification and short variant mutations in ERBB2 and ERBB3
BACKGROUND In contrast to lung cancer, few precision treatments are available for
colorectal cancer (CRC). One rapidly emerging treatment target in CRC is ERBB2 (human …
colorectal cancer (CRC). One rapidly emerging treatment target in CRC is ERBB2 (human …
Eph receptor signalling: from catalytic to non-catalytic functions
Eph receptors, the largest subfamily of receptor tyrosine kinases, are linked with proliferative
disease, such as cancer, as a result of their deregulated expression or mutation. Unlike …
disease, such as cancer, as a result of their deregulated expression or mutation. Unlike …
Prospects for pharmacological targeting of pseudokinases
Pseudokinases are members of the protein kinase superfamily but signal primarily through
noncatalytic mechanisms. Many pseudokinases contribute to the pathologies of human …
noncatalytic mechanisms. Many pseudokinases contribute to the pathologies of human …
Co-occurring gain-of-function mutations in HER2 and HER3 modulate HER2/HER3 activation, oncogenesis, and HER2 inhibitor sensitivity
Activating mutations in HER2 (ERBB2) drive the growth of a subset of breast and other
cancers and tend to co-occur with HER3 (ERBB3) missense mutations. The HER2 tyrosine …
cancers and tend to co-occur with HER3 (ERBB3) missense mutations. The HER2 tyrosine …
Actionable activating oncogenic ERBB2/HER2 transmembrane and juxtamembrane domain mutations
Deregulated HER2 is a target of many approved cancer drugs. We analyzed 111,176 patient
tumors and identified recurrent mutations in HER2 transmembrane domain (TMD) and …
tumors and identified recurrent mutations in HER2 transmembrane domain (TMD) and …
Structural basis for the non-catalytic functions of protein kinases
Protein kinases are known primarily for their ability to phosphorylate protein substrates,
which constitutes an essential biological process. Recently, compelling evidence has …
which constitutes an essential biological process. Recently, compelling evidence has …