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 …
[HTML][HTML] Molecular targeted therapy for anticancer treatment
HY Min, HY Lee - Experimental & molecular medicine, 2022 - nature.com
Since the initial clinical approval in the late 1990s and remarkable anticancer effects for
certain types of cancer, molecular targeted therapy utilizing small molecule agents or …
certain types of cancer, molecular targeted therapy utilizing small molecule agents or …
Bioactive pyrrole-based compounds with target selectivity
GL Petri, V Spano, R Spatola, R Holl… - European journal of …, 2020 - Elsevier
The discovery of novel synthetic compounds with drug-like properties is an ongoing
challenge in medicinal chemistry. Natural products have inspired the synthesis of …
challenge in medicinal chemistry. Natural products have inspired the synthesis of …
[HTML][HTML] PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …
durability of their effectiveness can be limited. Resistance to these therapies is often related …
Mutations disrupting neuritogenesis genes confer risk for cerebral palsy
In addition to commonly associated environmental factors, genomic factors may cause
cerebral palsy. We performed whole-exome sequencing of 250 parent–offspring trios, and …
cerebral palsy. We performed whole-exome sequencing of 250 parent–offspring trios, and …
[HTML][HTML] Identification of ALK in Thinness
There is considerable inter-individual variability in susceptibility to weight gain despite an
equally obesogenic environment in large parts of the world. Whereas many studies have …
equally obesogenic environment in large parts of the world. Whereas many studies have …
Treatment-driven tumour heterogeneity and drug resistance: Lessons from solid tumours
Molecular heterogeneity characterizes tumours' evolution and adaptation and, because of its
dynamics and continuous changes under external pressure, it is one of the major causes of …
dynamics and continuous changes under external pressure, it is one of the major causes of …
Neurofibromin and suppression of tumorigenesis: beyond the GAP
Abstract Neurofibromatosis type 1 (NF1) is an autosomal dominant genetic disease and one
of the most common inherited tumor predisposition syndromes, affecting 1 in 3000 …
of the most common inherited tumor predisposition syndromes, affecting 1 in 3000 …
[HTML][HTML] Structural basis for RNA surveillance by the human nuclear exosome targeting (NEXT) complex
MR Puno, CD Lima - Cell, 2022 - cell.com
RNA quality control relies on co-factors and adaptors to identify and prepare substrates for
degradation by ribonucleases such as the 3′ to 5′ ribonucleolytic RNA exosome. Here …
degradation by ribonucleases such as the 3′ to 5′ ribonucleolytic RNA exosome. Here …
[HTML][HTML] Phase separation of EML4–ALK in firing downstream signaling and promoting lung tumorigenesis
EML4–ALK fusion, observed in about 3%–7% of human lung adenocarcinoma, is one of the
most important oncogenic drivers in initiating lung tumorigenesis. However, it still remains …
most important oncogenic drivers in initiating lung tumorigenesis. However, it still remains …