TGF-beta, and its type 1 (ALK5) receptor, are critical to the pathogenesis of fibrosis. In toxicologic studies of 4 or more days in 10-week-old Sprague-Dawley rats, using an ALK5 inhibitor (GW788388), expansion of hypertrophic and proliferation zones of femoral physes were noted. Sub...
参见例如holmgaard等人,“targeting the tgfβpathway with galunisertib,a tgfβri small moleculeinhibitor,promotes anti-tumor immunity leading to durable,complete responses,as monotherapy and in combination with checkpoint blockade[作为单一疗法以及与检查点阻断组合的情况下用tgfβri小分子抑制剂戈鲁尼色替靶向...
Inhibitor of Transforming Growth Factor‑βSuperfamily Type I Activin Receptor‑Like Kinase(ALK)Receptors ALK4,ALK5,and ALK7[SB‑431542是转化生长因 子‑β超家族I型激活素受体样激酶(ALK)受体ALK4、ALK5和ALK7的强效和特异性抑制剂]”, Molecular Pharmacology[分子药理学],2002,62,65。另外,开发...
参考文献 [1]. Moon JA, et al. IN-1130, a novel transforming growth factor-beta type I receptor kinase (ALK5) inhibitor, suppresses renal fibrosis in obstructive nephropathy. Kidney Int. 2006 Oct;70(7):1234-43. [2]. Park CY, et al. An novel inhibitor of TGF-β type I receptor, I...
inhibitor),而相应的经氧化的 软药(oxidized soft drug)表现出降低的ALK5抑制活性。例如,ALK5抑制剂和相应的经氧 化的ALK5抑制剂的抑制效力的差异可以为10至100倍。在一些实施方案中,例如通过吸入将 本文公开的软ALK5抑制剂施用至肺部,并抑制肺中的ALK5的活性。然而,当离开肺部时,软 ALK5抑制剂可以容易地在肝...
Identification of ALK5 inhibitor via structure-based virtual screening and ADMET predictionADMETALK5virtual screeningTGF-βTGF- plays a critical role in the initiation and progression of fibrosis in various organ systems such as kidney, heart, lung and liver. TGF- and its receptors (ALK5 and TR...
A Window of Opportunity Trial Evaluating the Oral TGF-beta Receptor I Inhibitor Vactosertib in Patients Undergoing Standard of Care Chemoradiotherapy for Locally Advanced Esophageal Adenocarcinoma This interventional clinical trial aims to find ways of improving treatments for individuals with esophageal canc...
ALK5 Inhibitor IV, A8301 T3031909910-43-6 A 83-01 (ALK5 Inhibitor IV) 是一种 TGF-βI 型受体 ALK5、ALK4 和 ALK7 的抑制剂 (IC50=12/45/7.5 nM)。A 83-01 可促进小鼠成纤维细胞重编程为 iPSCs。A 83-01 可用于类器官培养。
RESULTS: Inhibition of TGF-β1 signaling by SB-431542 reduced fibrosis, fat infiltration, and muscle weight loss. SB-431542 treatment reduced the number of FAPs in the injured muscle by promoting apoptosis of fibro/adipogenic progenitor cells (FAPs), which are an important cellular source of fibr...
[4] Lee AJ, et al. Sustained Delivery of SB-431542, a Type I Transforming Growth Factor Beta-1 Receptor Inhibitor, to Prevent Arthrofibrosis. Tissue Eng Part A. 2021 May 12. HB220916