BioLLM Wiki β€Ί Targeted Small Molecules

Kinase Inhibitors

These papers examine kinase inhibitors as treatments and experimental approaches across solid cancers, hematologic malignancies, necrobiosis lipoidica, and bone-resorption disease. They include randomized and open-label clinical studies, cellular and animal models, signaling and transcriptomic analyses, and computational drug-target affinity prediction to assess efficacy, treatment resistance, safety, pharmacokinetic properties, and new inhibitor candidates.

Papers
6,483
Jan 2024 – Aug 2026
2024 share
5.91%
of the month's papers, on average
2025 share
5.95%
of the month's papers, on average
2026 share
4.57%
of the month's papers, on average
Change
β–Ό -22.7%
2024 β†’ 2026, relative

Share of papers by month

Peak 6.86% in Oct 2025. Month-by-month values and sub-terms are on Keyword Trends.

Jan 2024Aug 2026

Resistance to Targeted Inhibitors

Several studies examined mechanisms of resistance or treatment response during kinase inhibition. In EGFR-mutant lung adenocarcinoma, SOS2 deletion reduced PI3K/AKT reactivation and sensitized cells to osimertinib, whereas HGF/MET-driven bypass contributed to resistance; patient-derived EML4-ALK models were used to evaluate sequential crizotinib, alectinib, lorlatinib, ceritinib, and brigatinib. Type II JAK2 inhibitor resistance in myeloproliferative neoplasms involved AXL and MAPK activation while JAK2-STAT3/5 remained suppressed, and ERK5 inhibition reduced viability in dabrafenib-resistant, but not vemurafenib-resistant, BRAF-mutant melanoma cells. In chronic myeloid leukemia, USP8 knockdown increased TKI sensitivity by suppressing EIF2S1 protein stabilization.

πŸ“„ Molecular oncology β†—πŸ“„ Acta pharmacologica Sinica β†—πŸ“„ Clinical cancer research : an official journal of the American Association for Cancer Research β†—πŸ“„ FEBS letters β†—πŸ“„ The FEBS journal β†—

Clinical Targeted Therapy

Clinical studies evaluated iruplinalkib versus crizotinib in ALK-positive, ALK TKI-naive, locally advanced or metastatic NSCLC; amivantamab-lazertinib versus osimertinib as first-line treatment in previously untreated EGFR-mutated advanced NSCLC; pirtobrutinib versus investigator’s choice of idelalisib/rituximab or bendamustine/rituximab in covalent BTK inhibitor-pretreated relapsed/refractory CLL/SLL; upadacitinib maintenance in Crohn’s disease; and ivarmacitinib with background conventional synthetic DMARDs in patients with active rheumatoid arthritis and an inadequate response to conventional synthetic DMARDs.

πŸ“„ Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer β†—πŸ“„ The New England journal of medicine β†—πŸ“„ Journal of clinical oncology : official journal of the American Society of Clinical Oncology β†—πŸ“„ Journal of Crohn's & colitis β†—πŸ“„ Annals of the rheumatic diseases β†—

Computational Inhibitor Discovery

A group of studies uses virtual screening and molecular simulation to nominate kinase inhibitors before experimental testing. Machine-learning QSAR, docking, and molecular dynamics screened DrugBank compounds against PI3KΞ± in gastric cancer; virtual screening, docking, pharmacokinetics, and MM/PBSA identified the natural compounds (-)-balanol, digallic acid, and scutellarin as NEK7 candidates; and ZINC-library screening selected natural-product CDK8 binders after Lipinski, ADME, and pan-assay interference filters. AI and structure-based screening were also applied to TGFΞ²R1, while a language-model and graph-neural-network framework identified CDK9 inhibitor C1 with a reported IC50 of 1.2 nM and in vivo anti-leukemia activity.

πŸ“„ Applied biochemistry and biotechnology β†—πŸ“„ Molecular diversity β†—πŸ“„ Omics : a journal of integrative biology β†—πŸ“„ Computational biology and chemistry β†—πŸ“„ Advanced science (Weinheim, Baden-Wurttemberg, Germany) β†—

Mechanism, Combination, And Safety

The papers also examine pathway mechanisms and clinically relevant drug effects, metabolism, and absorption. The p38Ξ± inhibitor BMS-582949 suppressed RANKL-induced osteoclastogenesis, F-actin ring formation, osteoclast-specific gene expression, MAPK/AKT signaling, and bone loss in ovariectomized mice, while dasatinib reduced bladder cancer proliferation and induced G1 arrest, apoptosis, and autophagy through PI3K/AKT/mTOR suppression. Dasatinib also reduced SAMHD1 phosphorylation, HIV-1 infection, and the inflammatory potential of macrophages; separate studies assessed osimertinib-associated QT prolongation and cardiac dysfunction, X-376 metabolism in human liver microsomes, and AI prediction of TKI malabsorption in settings such as proton-pump inhibitor use or bariatric surgery.

πŸ“„ Biochemical pharmacology β†—πŸ“„ Investigative and clinical urology β†—πŸ“„ Biochemical pharmacology β†—πŸ“„ Lung cancer (Amsterdam, Netherlands) β†—πŸ“„ Journal of pharmacological and toxicological methods β†—πŸ“„ British journal of clinical pharmacology β†—

Written by gpt-5.6-luna from 96 of this keyword's papers, a few from every whole month through Aug 2026; every paragraph was checked against the abstracts it cites. A paper counts for the keyword when its title, abstract, keywords or MeSH headings match the keyword's terms. Not medical advice; see the Disclaimer.