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 …

[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 …

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 …

[HTML][HTML] PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …

Mutations disrupting neuritogenesis genes confer risk for cerebral palsy

SC Jin, SA Lewis, S Bakhtiari, X Zeng, MC Sierant… - Nature …, 2020 - nature.com
In addition to commonly associated environmental factors, genomic factors may cause
cerebral palsy. We performed whole-exome sequencing of 250 parent–offspring trios, and …

[HTML][HTML] Identification of ALK in Thinness

M Orthofer, A Valsesia, R Mägi, QP Wang… - Cell, 2020 - cell.com
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 …

Treatment-driven tumour heterogeneity and drug resistance: Lessons from solid tumours

S Crucitta, F Cucchiara, R Mathijssen, J Mateo… - Cancer treatment …, 2022 - Elsevier
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 …

Neurofibromin and suppression of tumorigenesis: beyond the GAP

J Mo, SL Moye, RM McKay, LQ Le - Oncogene, 2022 - nature.com
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 …

[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 …

[HTML][HTML] Phase separation of EML4–ALK in firing downstream signaling and promoting lung tumorigenesis

Z Qin, H Sun, M Yue, X Pan, L Chen, X Feng, X Yan… - Cell discovery, 2021 - nature.com
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 …