Recent advances of SHP2 inhibitors in cancer therapy: current development and clinical application
X Yuan, H Bu, J Zhou, CY Yang… - Journal of medicinal …, 2020 - ACS Publications
… SHP2 abnormality and human disease makes SHP2 an attractive target for developing
mechanism-based therapy. Identification of highly bioactive and selective SHP2 inhibitors will be …
mechanism-based therapy. Identification of highly bioactive and selective SHP2 inhibitors will be …
[HTML][HTML] Strategies to overcome drug resistance using SHP2 inhibitors
M Liu, S Gao, RM Elhassan, X Hou, H Fang - Acta Pharmaceutica Sinica B, 2021 - Elsevier
… of SHP2, and briefly review the development of SHP2 inhibitors. … tumor immunotherapy
using SHP2 inhibitors. We also discuss … inhibitor 2a as a selective SHP2 inhibitor (SHP2 IC 50 …
using SHP2 inhibitors. We also discuss … inhibitor 2a as a selective SHP2 inhibitor (SHP2 IC 50 …
Allosteric inhibition of SHP2: identification of a potent, selective, and orally efficacious phosphatase inhibitor
J Garcia Fortanet, CHT Chen, YNP Chen… - Journal of medicinal …, 2016 - ACS Publications
… a potential immunomodulator, controlling SHP2 activity is of significant … inhibitor of SHP2
was identified as an allosteric modulator that stabilizes the autoinhibited conformation of SHP2. …
was identified as an allosteric modulator that stabilizes the autoinhibited conformation of SHP2. …
Allosteric inhibition of SHP2 stimulates antitumor immunity by transforming the immunosuppressive environment
E Quintana, CJ Schulze, DR Myers, TJ Choy, K Mordec… - Cancer research, 2020 - AACR
… selective allosteric inhibitor of SHP2, RMC-4550 (1), to generate an in-depth understanding
of the integrated effects of SHP2 inhibition … unanticipated impact of SHP2 on tumor immunity …
of the integrated effects of SHP2 inhibition … unanticipated impact of SHP2 on tumor immunity …
Identification of TNO155, an allosteric SHP2 inhibitor for the treatment of cancer
MJ LaMarche, M Acker, A Argintaru… - Journal of medicinal …, 2020 - ACS Publications
… tunnel inhibitors, compound 1 was completely selective over … selectivity is a result of the
allosteric mechanism of inhibition which occurs via the ligands binding to the tunnel site of SHP2…
allosteric mechanism of inhibition which occurs via the ligands binding to the tunnel site of SHP2…
Emerging chemical scaffolds with potential SHP2 phosphatase inhibitory capabilities–A comprehensive review
RKP Tripathi, SR Ayyannan - Chemical Biology & Drug Design, 2021 - Wiley Online Library
… Even though substantial advancements have been attained in the design of selective SHP2
inhibitors in the past two decades, a veritable breakthrough in the field happened only with …
inhibitors in the past two decades, a veritable breakthrough in the field happened only with …
Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases
YNP Chen, MJ LaMarche, HM Chan, P Fekkes… - Nature, 2016 - nature.com
… a highly potent (IC 50 = 0.071 μM), selective and orally bioavailable small-molecule SHP2
… inhibition, we developed screening strategies aimed at identifying SHP2 allosteric inhibitors. …
… inhibition, we developed screening strategies aimed at identifying SHP2 allosteric inhibitors. …
SHP2 inhibition prevents adaptive resistance to MEK inhibitors in multiple cancer models
… the SHP2 inhibitor SHP099 with a … inhibitors show limited efficacy as single agents, in
part because of the rapid development of adaptive resistance. We find that SHP2/MEK inhibitor …
part because of the rapid development of adaptive resistance. We find that SHP2/MEK inhibitor …
Allosteric inhibitors of SHP2: an updated patent review (2015-2020)
J Wu, H Zhang, G Zhao, R Wang - Current Medicinal Chemistry, 2021 - ingentaconnect.com
… site of SHP2 with high selectivity and low toxicity are under development. This paper reviews
allosteric inhibitors of SHP2 … SHP2 has long been considered as an ‘undruggable’ protein. …
allosteric inhibitors of SHP2 … SHP2 has long been considered as an ‘undruggable’ protein. …
[HTML][HTML] Tyrosine phosphatase SHP2 inhibitors in tumor-targeted therapies
… Notably, various potent and selective SHP2 inhibitors have … SHP2 inhibitors and revisited
the SHP2-targeted anticancer strategies, and combination therapies with other PTK inhibitors …
the SHP2-targeted anticancer strategies, and combination therapies with other PTK inhibitors …
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