Combinations with allosteric SHP2 inhibitor TNO155 to block receptor tyrosine kinase signaling
C Liu, H Lu, H Wang, A Loo, X Zhang, G Yang… - Clinical Cancer …, 2021 - AACR
Purpose: SHP2 inhibitors offer an appealing and novel approach to inhibit receptor tyrosine
kinase (RTK) signaling, which is the oncogenic driver in many tumors or is frequently …
kinase (RTK) signaling, which is the oncogenic driver in many tumors or is frequently …
Initial results from a dose finding study of TNO155, a SHP2 inhibitor, in adults with advanced solid tumors.
I Brana, G Shapiro, ML Johnson, HA Yu, D Robbrecht… - 2021 - ascopubs.org
3005 Background: SHP2 transduces signals from activated receptor tyrosine kinases to
downstream pathways including MAPK. TNO155 is a selective, allosteric, oral inhibitor of …
downstream pathways including MAPK. TNO155 is a selective, allosteric, oral inhibitor of …
Identification of TNO155, an allosteric SHP2 inhibitor for the treatment of cancer
MJ LaMarche, M Acker, A Argintaru… - Journal of medicinal …, 2020 - ACS Publications
SHP2 is a nonreceptor protein tyrosine phosphatase encoded by the PTPN11 gene and is
involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also plays …
involved in cell growth and differentiation via the MAPK signaling pathway. SHP2 also plays …
SHP2 inhibition sensitizes diverse oncogene-addicted solid tumors to re-treatment with targeted therapy
A Drilon, MR Sharma, ML Johnson, TA Yap, S Gadgeel… - Cancer discovery, 2023 - AACR
Rationally targeted therapies have transformed cancer treatment, but many patients develop
resistance through bypass signaling pathway activation. PF-07284892 (ARRY-558) is an …
resistance through bypass signaling pathway activation. PF-07284892 (ARRY-558) is an …
A12 the SHP2 inhibitor RMC-4630 in patients with KRAS-mutant non-small cell lung cancer: preliminary evaluation of a first-in-man phase 1 clinical trial
SI Ou, M Koczywas, S Ulahannan, P Janne… - Journal of Thoracic …, 2020 - jto.org
Background: Mutations in KRAS are among the most common aberrations in cancer.
However, despite considerable research efforts, KRAS remains a challenging therapeutic …
However, despite considerable research efforts, KRAS remains a challenging therapeutic …
SHP2 inhibition overcomes RTK-mediated pathway reactivation in KRAS-mutant tumors treated with MEK inhibitors
H Lu, C Liu, R Velazquez, H Wang, LM Dunkl… - Molecular cancer …, 2019 - AACR
FGFR1 was recently shown to be activated as part of a compensatory response to prolonged
treatment with the MEK inhibitor trametinib in several KRAS-mutant lung and pancreatic …
treatment with the MEK inhibitor trametinib in several KRAS-mutant lung and pancreatic …
Allosteric SHP2 inhibitors in cancer: Targeting the intersection of RAS, resistance, and the immune microenvironment
The nonreceptor protein tyrosine phosphatase SHP2 (encoded by PTPN11) integrates
growth and differentiation signals from receptor tyrosine kinases (RTKs) into the …
growth and differentiation signals from receptor tyrosine kinases (RTKs) into the …
Allosteric SHP2 inhibitor, IACS-13909, overcomes EGFR-dependent and EGFR-independent resistance mechanisms toward osimertinib
Src homology 2 domain-containing phosphatase (SHP2) is a phosphatase that mediates
signaling downstream of multiple receptor tyrosine kinases (RTK) and is required for full …
signaling downstream of multiple receptor tyrosine kinases (RTK) and is required for full …
Combined inhibition of SHP2 and CXCR1/2 promotes antitumor T-cell response in NSCLC
Abstract SHP2 inhibitors (SHP2i) alone and in various combinations are being tested in
multiple tumors with overactivation of the RAS/ERK pathway. SHP2 plays critical roles in …
multiple tumors with overactivation of the RAS/ERK pathway. SHP2 plays critical roles in …
Identification of GDC-1971 (RLY-1971), a SHP2 inhibitor designed for the treatment of solid tumors
AM Taylor, BR Williams, F Giordanetto… - Journal of Medicinal …, 2023 - ACS Publications
Protein tyrosine phosphatase SHP2 mediates RAS-driven MAPK signaling and has
emerged in recent years as a target of interest in oncology, both for treating with a single …
emerged in recent years as a target of interest in oncology, both for treating with a single …
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