The new opportunities in medicinal chemistry of fourth-generation EGFR inhibitors to overcome C797S mutation
Epidermal growth factor receptor (EGFR) is a receptor for epithelial growth factor (EGF) cell
proliferation and signaling, which is related to the inhibition of tumor cell proliferation …
proliferation and signaling, which is related to the inhibition of tumor cell proliferation …
Imidazopyridine-based kinase inhibitors as potential anticancer agents: A review
F Peytam, Z Emamgholipour, A Mousavi, M Moradi… - Bioorganic …, 2023 - Elsevier
Considering the fundamental role of protein kinases in the mechanism of protein
phosphorylation in critical cellular processes, their dysregulation, especially in cancers, has …
phosphorylation in critical cellular processes, their dysregulation, especially in cancers, has …
Chemical probes for understudied kinases: challenges and opportunities
RAM Serafim, JM Elkins, WJ Zuercher… - Journal of Medicinal …, 2021 - ACS Publications
Over 20 years after the approval of the first-in-class protein kinase inhibitor imatinib, the
biological function of a significant fraction of the human kinome remains poorly understood …
biological function of a significant fraction of the human kinome remains poorly understood …
Synthesis and evaluation of chiral rhodanine derivatives bearing quinoxalinyl imidazole moiety as ALK5 inhibitors
LM Zhao, FY Guo, HM Wang, T Dou, J Da Qi… - Medicinal …, 2022 - ingentaconnect.com
Background: TGF-β signaling pathway inhibition is considered an effective way to prevent
the development of several diseases. In the design and synthesis of TGF-β inhibitors, a …
the development of several diseases. In the design and synthesis of TGF-β inhibitors, a …
A highly selective chemical probe for activin receptor-like kinases ALK4 and ALK5
The transforming growth factor beta-receptor I/activin receptor-like kinase 5 (TGFBR1/ALK5)
and its close homologue ALK4 are receptor protein kinases associated with the …
and its close homologue ALK4 are receptor protein kinases associated with the …
Design, synthesis and optimization of 7-substituted-pyrazolo [4, 3-b] pyridine ALK5 (activin receptor-like kinase 5) inhibitors
M Sabat, H Wang, N Scorah, JD Lawson… - Bioorganic & Medicinal …, 2017 - Elsevier
A series of potent ALK5 inhibitors were designed using a SBDD approach and subsequently
optimized to improve drug likeness. Starting with a 4-substituted quinoline screening hit …
optimized to improve drug likeness. Starting with a 4-substituted quinoline screening hit …
Discovery of selective transforming growth factor β type II receptor inhibitors as antifibrosis agents
S Miwa, M Yokota, Y Ueyama, K Maeda… - ACS Medicinal …, 2021 - ACS Publications
Historically, modulation of transforming growth factor β (TGF-β) signaling has been deemed
a rational strategy to treat many disorders, though few successful examples have been …
a rational strategy to treat many disorders, though few successful examples have been …
Copper-mediated synthesis of N-arylated cyclic urea from diaminecarbamate
H Liu, Y Wang, X Lu, B Sun, Q Gong, FL Zhang - Tetrahedron Letters, 2024 - Elsevier
A convenient base-promoted CuI-mediated intermolecular synthesis of N-arylated cyclic
ureas from diaminecarbamate and aryl iodides was developed. A series of N-arylated five …
ureas from diaminecarbamate and aryl iodides was developed. A series of N-arylated five …
[PDF][PDF] 抗線維化薬を志向した選択的TGF-B RII 阻害剤の開発
三輪祥平 - 2022 - kanazawa-u.repo.nii.ac.jp
強皮症とは皮膚が硬くなる変化を代表とする病気で, 内臓にも変化を伴う全身性強皮症 (Systemic
sclerosis; SSc) と, 皮膚およびその下部の筋肉のみを硬化させる限局性強皮症に分類される. 1) …
sclerosis; SSc) と, 皮膚およびその下部の筋肉のみを硬化させる限局性強皮症に分類される. 1) …