Combination of KRASG12C (ON) and SHP2 inhibitors overcomes adaptive resistance and enhances anti-tumour immunity

P Anastasiou, J Boumelha, E Mugarza… - European Journal of …, 2022 - ejcancer.com
… higher potency for inhibition of cell viability than the KRAS G12C (OFF) inhibitor MRTX849 in
… in RAS pathway reactivation which was blocked upon coincubation with the SHP2 inhibitor

[HTML][HTML] SHP2 as a primordial epigenetic enzyme expunges histone H3 pTyr-54 to amend androgen receptor homeostasis

S Chouhan, D Sridaran, C Weimholt, J Luo, T Li… - Nature …, 2024 - nature.com
… mutants of SHP2 may activate other signaling pathway that is … AR reactivation could partly
compensate for the loss of SHP2 … upon treatment with ACK1 and SHP2 inhibitor appears to be …

SHP-2 expression negatively regulates NK cell function

AK Purdy, KS Campbell - The Journal of Immunology, 2009 - journals.aai.org
… After transfer, membranes were air-dried, reactivated with methanol, washed once with …
conclude that SHP-2 is playing an inhibitory role at the level of pathways controlling cytoskeleton …

[PDF][PDF] sHP2 Inhibitors

P Torres-Ayuso, J Brognard - 2018 - researchgate.net
… Multiple attempts to therapeutically target RAS directly or pathways … on SHP2, and
reactivation of downstream signals. Inhibition of both MEK and SHP2 abrogates MEK inhibitor–…

From pyrazolones to azaindoles: evolution of active-site SHP2 inhibitors based on scaffold hopping and bioisosteric replacement

Y Mostinski, GJJE Heynen… - Journal of medicinal …, 2020 - ACS Publications
… The tyrosine phosphatase SHP2 controls the activity of pivotal signaling pathways, including
MAPK… Inhibition of ERK feedback reactivation is sustained after 48 h compared to PLX4032 …

SHP2 inhibitors: Recent advancements and potential breakthroughs in cancer therapy

M Meem - 2022 - dspace.bracu.ac.bd
… recent advances made with SHP2 inhibitors as a targeted therapy … of cancer treatment based
on SHP2 inhibition. An additional … due to the reactivation of the MAPK pathway for negative …

Combination mTOR and SHP2 inhibitor treatment of lymphatic malformation endothelial cells

JK Wolter, I Valencia-Sama, AJ Osborn, EJ Propst… - Microvascular …, 2022 - Elsevier
inhibitors are being investigated for treatment of various … determine the impact of SHP2
inhibition in combination with rapamycin … re-activation of AKT, and that targeting the RAS pathway

[PDF][PDF] Sulforaphane-mediated inhibition of SHP2 as a potential pharmacotherapy for Noonan syndrome

J Smith, E Schroder, O Prysyazhna, H Cho, M Mayr… - 2019 - kclpure.kcl.ac.uk
… would inhibit SHP2SHP2 activity was also attenuated in the spleen of both WT and NS
mice, strongly suggesting this therapeutic action of SFX-01 was mediated by inhibition of SHP2

[HTML][HTML] Tyrosyl phosphorylation of KRAS stalls GTPase cycle via alteration of switch I and II conformation

Y Kano, T Gebregiworgis, CB Marshall… - Nature …, 2019 - nature.com
… Protein tyrosine phosphatase SHP2 promotes RAF-to-MAPK signaling pathway and is an …
reactivates downstream signaling 6 . We further showed that pharmacologic inhibition of SHP2

ERAS-007 (ERK inhibitor)+ ERAS-601 (SHP2 inhibitor) exhibit nonclinical combination activity across KRAS mutated NSCLC, CRC, and PDAC tumor models

L Martin, ED Lew, R Patel, J Oh, J Zhang, R Nevarez… - Cancer Research, 2022 - AACR
pathway nodes has the potential to more robustly prevent reactivation relative to inhibition
… We are currently exploring the combination of an inhibitor of an upstream node, SHP2, with …