Big opportunities for small molecules in immuno-oncology

JL Adams, J Smothers, R Srinivasan… - Nature reviews Drug …, 2015 - nature.com
The regulatory approval of ipilimumab (Yervoy) in 2011 ushered in a new era of cancer
immunotherapies with durable clinical effects. Most of these breakthrough medicines are …

Research trends in pharmacological modulation of tumor‐associated macrophages

N Wang, S Wang, X Wang, Y Zheng… - Clinical and …, 2021 - Wiley Online Library
As one of the most abundant immune cell populations in the tumor microenvironment (TME),
tumor‐associated macrophages (TAMs) play important roles in multiple solid malignancies …

Safety and clinical activity of a new anti-PD-L1 antibody as monotherapy or combined with targeted therapy in advanced solid tumors: the PACT phase Ia/Ib trial

A Patnaik, TA Yap, HC Chung, MJ de Miguel… - Clinical Cancer …, 2021 - AACR
Abstract Purpose: This phase Ia/Ib PACT study evaluated the safety, pharmacokinetics,
pharmacodynamics, and antitumor activity of a new programmed cell death ligand 1 (PD-L1) …

Tailoring therapies to counter the divergent immune landscapes of breast cancer

S Attalla, T Taifour, W Muller - Frontiers in Cell and Developmental …, 2023 - frontiersin.org
Breast cancer remains a significant clinical concern affecting millions of women worldwide.
Immunotherapy is a rapidly growing drug class that has revolutionized cancer treatment but …

MST1R kinase accelerates pancreatic cancer progression via effects on both epithelial cells and macrophages

ML Babicky, MM Harper, J Chakedis, A Cazes… - Oncogene, 2019 - nature.com
Abstract The MST1R (RON) kinase is overexpressed in> 80% of human pancreatic cancers,
but its role in pancreatic carcinogenesis is unknown. In this study, we examined the …

Myeloid cells as targets for therapy in solid tumors

T Cotechini, TR Medler, LM Coussens - The Cancer Journal, 2015 - journals.lww.com
It is well established that cancer development ensues based on reciprocal interactions
between genomically altered neoplastic cells and diverse populations of recruited “host” …

[HTML][HTML] Small-molecule agents for cancer immunotherapy

F Wang, K Fu, Y Wang, C Pan, X Wang, Z Liu… - … Pharmaceutica Sinica B, 2023 - Elsevier
Cancer immunotherapy, exemplified by the remarkable clinical benefits of the immune
checkpoint blockade and chimeric antigen receptor T-cell therapy, is revolutionizing cancer …

Preclinical efficacy of Ron kinase inhibitors alone and in combination with PI3K inhibitors for treatment of sfRon-expressing breast cancer patient-derived xenografts

M Bieniasz, P Radhakrishnan, N Faham… - Clinical Cancer …, 2015 - AACR
Purpose: Recent studies have demonstrated that short-form Ron (sfRon) kinase drives
breast tumor progression and metastasis through robust activation of the PI3K pathway. We …

OPN promotes the aggressiveness of non-small-cell lung cancer cells through the activation of the RON tyrosine kinase

C Hao, Y Cui, S Chang, J Huang, E Birkin, M Hu… - Scientific Reports, 2019 - nature.com
Osteopontin (OPN) is identified as a diagnostic and prognostic biomarker of tumor
progression and metastasis. In non-small-cell lung cancer (NSCLC), the functions of OPN …

Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets

FM Franco, DE Jones, PKW Harris, Z Han… - Bioorganic & Medicinal …, 2015 - Elsevier
Hepatocyte growth factor activator (HGFA), matriptase and hepsin are all S1 trypsin-like
serine endopeptidases. HGFA is a plasma protease while hepsin and matriptase are type II …