Trends in kinase drug discovery: targets, indications and inhibitor design

MM Attwood, D Fabbro, AV Sokolov, S Knapp… - Nature Reviews Drug …, 2021 - nature.com
The FDA approval of imatinib in 2001 was a breakthrough in molecularly targeted cancer
therapy and heralded the emergence of kinase inhibitors as a key drug class in the oncology …

Properties of FDA-approved small molecule protein kinase inhibitors

R Roskoski Jr - Pharmacological research, 2019 - Elsevier
Because mutations, overexpression, and dysregulation of protein kinases play essential
roles in the pathogenesis of many illnesses, this enzyme family has become one of the most …

Research progress of mTOR inhibitors

Y Chen, X Zhou - European journal of medicinal chemistry, 2020 - Elsevier
Mammalian target of rapamycin (mTOR) is a highly conserved Serine/Threonine (Ser/Thr)
protein kinase, which belongs to phosphatidylinositol-3-kinase-related kinase (PIKK) protein …

Targeting mTOR and metabolism in cancer: lessons and innovations

C Magaway, E Kim, E Jacinto - Cells, 2019 - mdpi.com
Cancer cells support their growth and proliferation by reprogramming their metabolism in
order to gain access to nutrients. Despite the heterogeneity in genetic mutations that lead to …

Renal cell carcinoma therapy: current and new drug candidates

O Pontes, S Oliveira-Pinto, F Baltazar, M Costa - Drug Discovery Today, 2022 - Elsevier
Renal cell carcinoma (RCC) is the most common and lethal tumor of the urological system.
Curative treatment of localized RCC includes nephrectomy, radio-ablation, and active …

Selective inhibitors of mTORC1 activate 4EBP1 and suppress tumor growth

BJ Lee, JA Boyer, GL Burnett, AP Thottumkara… - Nature chemical …, 2021 - nature.com
The clinical benefits of pan-mTOR active-site inhibitors are limited by toxicity and relief of
feedback inhibition of receptor expression. To address these limitations, we designed a …

Anti-angiogenesis target therapy for advanced osteosarcoma

L Xie, T Ji, W Guo - Oncology reports, 2017 - spandidos-publications.com
Osteosarcomas (OS), especially those with metastatic or unresectable disease, have limited
treatment options. The greatest advancement in treatments occurred in the 1980s when …

Papillary renal cell carcinoma: current and controversial issues

S Angori, J Lobo, H Moch - Current opinion in urology, 2022 - journals.lww.com
Papillary renal cell carcinoma: current and controversial is... : Current Opinion in Urology
Papillary renal cell carcinoma: current and controversial issues : Current Opinion in Urology …

The PI3K/Akt/mTOR pathway in polycystic kidney disease: A complex interaction with polycystins and primary cilium

JP Margaria, CC Campa, MC De Santis, E Hirsch… - Cellular signalling, 2020 - Elsevier
Over-activation of the PI3K/Akt/mTOR network is a well-known pathogenic event that leads
to hyper-proliferation. Pharmacological targeting of this pathway has been developed for the …

Nanomaterials for antiangiogenic therapies for cancer: a promising tool for personalized medicine

HO Alsaab, AS Al-Hibs, R Alzhrani… - International journal of …, 2021 - mdpi.com
Angiogenesis is one of the hallmarks of cancer. Several studies have shown that vascular
endothelium growth factor (VEGF) plays a leading role in angiogenesis progression …