Emma McCullagh

TL;DR: It is proposed that IPA binding biases the PERK kinase towards its active conformation, which trans-activates apo-PERK molecules, which carries major implications for design and therapeutic application of kinase inhibitors.

TL;DR: A series of novel compounds that have low nanomolar potency against both BTK and PI3Kδ as well as acceptable PK properties that could be useful in the development of treatments against B-cell related diseases are reported.

TL;DR: These compounds are imidazotetrazine analogs, expected to act through the same mechanism as temozolomide, and have the potential to improve efficacy and therapeutic index in the treatment of glioblastoma.

TL;DR: It is found that this orally bioavailable dual inhibitor reduced tumor growth in a B cell lymphoma xenograft model more effectively than either ibrutinib or idelalisib, suggesting that dual inhibition of these two key pathways by a single molecule could be a viable approach for treatment of NHL patients.