Trends in kinase drug discovery: targets, indications and inhibitor design
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 …
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 …
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 …
protein kinase, which belongs to phosphatidylinositol-3-kinase-related kinase (PIKK) protein …
Targeting mTOR and metabolism in cancer: lessons and innovations
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 …
order to gain access to nutrients. Despite the heterogeneity in genetic mutations that lead to …
Renal cell carcinoma therapy: current and new drug candidates
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 …
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 …
feedback inhibition of receptor expression. To address these limitations, we designed a …
Anti-angiogenesis target therapy for advanced osteosarcoma
Osteosarcomas (OS), especially those with metastatic or unresectable disease, have limited
treatment options. The greatest advancement in treatments occurred in the 1980s when …
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 …
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
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 …
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 …
endothelium growth factor (VEGF) plays a leading role in angiogenesis progression …