[HTML][HTML] Targeting tumor-associated macrophages for cancer treatment

M Li, L He, J Zhu, P Zhang, S Liang - Cell & bioscience, 2022 - Springer
Tumor-associated macrophages (TAMs) are abundant, nearly accounting for 30–50% of
stromal cells in the tumor microenvironment. TAMs exhibit an immunosuppressive M2-like …

Small-molecule CSF1R kinase inhibitors; review of patents 2015-present

WA Denny, JU Flanagan - Expert opinion on therapeutic patents, 2021 - Taylor & Francis
Introduction Colony stimulating factor 1 receptor (CSF-1R, also known as c-FMS kinase) is in
the class III receptor tyrosine kinase family, along with c-Kit, Flt3 and PDGFRα. CSF-1/CSF …

[HTML][HTML] Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance

T Zhang, R Qu, S Chan, M Lai, L Tong, F Feng, H Chen… - Molecular cancer, 2020 - Springer
Background Non-small cell lung cancer (NSCLC) patients with activating EGFR mutations
initially respond to first-generation EGFR inhibitors; however, the efficacy of these drugs is …

[HTML][HTML] Pexidartinib synergize PD-1 antibody through inhibiting treg infiltration by reducing TAM-derived CCL22 in lung adenocarcinoma

W Zhang, X Jiang, Y Zou, L Yuan… - Frontiers in Pharmacology, 2023 - frontiersin.org
There is a crosstalk between Tumor-associated macrophages (TAM) and tumor-infiltrating T
cells in tumor environment. TAM could inhibit the activity of cytotoxic T cells; TAM could also …

Design and synthesis of 1H-pyrazolo [3, 4-d] pyrimidine derivatives as hematopoietic progenitor kinase 1 (HPK1) inhibitors

J Zhang, Y Li, H Tang, Q Zhou, L Tong, J Ding, H Xie… - Bioorganic …, 2023 - Elsevier
Despite immune checkpoint inhibitors' tremendous success in the treatment of tumors, the
moderate response rate limits their widespread use. Hematopoietic progenitor kinase 1 …

[HTML][HTML] Cancer immune exclusion: breaking the barricade for a successful immunotherapy

S Bruni, MF Mercogliano, FL Mauro… - Frontiers in …, 2023 - frontiersin.org
Immunotherapy has changed the course of cancer treatment. The initial steps were made
through tumor-specific antibodies that guided the setup of an antitumor immune response. A …

Design, synthesis and pharmacological evaluation of bicyclic and tetracyclic pyridopyrimidinone analogues as new KRASG12C inhibitors

X Xiao, M Lai, Z Song, M Geng, J Ding, H Xie… - European journal of …, 2021 - Elsevier
KRAS is the most commonly altered oncogene of the RAS family, especially the G12C
mutant (KRAS G12C), which has been a promising drug target for many cancers. On the …

Discovery of N-(3-bromo-1H-indol-5-yl)-quinazolin-4-amine as an effective molecular skeleton to develop reversible/irreversible pan-HER inhibitors

Q Tang, T Peng, J Hu, T Zhang, P Chen, D Chen… - European Journal of …, 2022 - Elsevier
Pan-HER inhibitors exhibit extensive biological activity and offer unique advantages and
usually bind to targets in an irreversible manner. Owing to the off-target toxicity of irreversible …

C11, a novel fibroblast growth factor receptor 1 (FGFR1) inhibitor, suppresses breast cancer metastasis and angiogenesis

Z Chen, L Tong, B Tang, H Liu, X Wang… - Acta Pharmacologica …, 2019 - nature.com
The fibroblast growth factor receptors (FGFRs) are increasingly considered attractive targets
for therapeutic cancer intervention due to their roles in tumor metastasis and angiogenesis …

[HTML][HTML] Discovery of HCD3514 as a potent EGFR inhibitor against C797S mutation in vitro and in vivo

M Lai, T Zhang, H Chen, P Song, L Tong, J Chen… - Journal of …, 2023 - ncbi.nlm.nih.gov
Abstract Osimertinib (AZD9291), a third-generation epidermal growth factor receptor (EGFR)
tyrosine kinase inhibitors (TKI), has significantly improved the survival of non-small cell lung …