FDA-approved small-molecule kinase inhibitors

P Wu, TE Nielsen, MH Clausen - Trends in pharmacological sciences, 2015 - cell.com
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 …

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 …

Structures of the HER2–HER3–NRG1β complex reveal a dynamic dimer interface

D Diwanji, R Trenker, TM Thaker, F Wang, DA Agard… - Nature, 2021 - nature.com
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 …

Genomic characterization of primary invasive lobular breast cancer

C Desmedt, G Zoppoli, G Gundem, G Pruneri… - Journal of clinical …, 2016 - ascopubs.org
Purpose Invasive lobular breast cancer (ILBC) is the second most common histologic
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

JS Ross, M Fakih, SM Ali, JA Elvin, AB Schrock, J Suh… - Cancer, 2018 - Wiley Online Library
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 …

Eph receptor signalling: from catalytic to non-catalytic functions

LY Liang, O Patel, PW Janes, JM Murphy, IS Lucet - Oncogene, 2019 - nature.com
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 …

Prospects for pharmacological targeting of pseudokinases

JE Kung, N Jura - Nature Reviews Drug Discovery, 2019 - nature.com
Pseudokinases are members of the protein kinase superfamily but signal primarily through
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

AB Hanker, BP Brown, J Meiler, A Marín, HS Jayanthan… - Cancer cell, 2021 - cell.com
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 …

Actionable activating oncogenic ERBB2/HER2 transmembrane and juxtamembrane domain mutations

KB Pahuja, TT Nguyen, BS Jaiswal, K Prabhash… - Cancer cell, 2018 - cell.com
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 …

Structural basis for the non-catalytic functions of protein kinases

JE Kung, N Jura - Structure, 2016 - cell.com
Protein kinases are known primarily for their ability to phosphorylate protein substrates,
which constitutes an essential biological process. Recently, compelling evidence has …