ArticleThe Journal of biological chemistry2019
High-throughput screens for agonists of bone morphogenetic protein (BMP) signaling identify potent benzoxazole compounds.
Article in The Journal of biological chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 41 citations in OpenAlex.
- Metabolic stress-activated endothelial STING rewires the sinusoidal immune niche to promote MASLD progression.The Journal of clinical investigation · 2026Article
- Aberrant expression of Gremlin1 induces trophoblast senescence in the placenta of advanced maternal age pregnancy.Journal of translational medicine · 2026Article
- Effects of Bone Morphogenetic Protein Agonist Small Molecule, SB4, on Osteogenic Differentiation of Adipose-Derived Mesenchymal Stem Cells.Journal of bone metabolism · 2026Article
- A paracrine-to-autocrine shunt of GREM1 fuels colorectal cancer metastasis via ACVR1C.Molecular cancer · 2026Article
- AMOTL2 inhibits lymph node metastasis in gastric cancer by suppressing TGF-β/Smad signaling and is destabilized by the E3 ubiquitin ligase SMURF1.International journal of biological sciences · 2026Article
- Cardiac preservation usingFrontiers in cardiovascular medicine · 2025Article
- Examination of the functions and mechanism ofFrontiers in oncology · 2025Article
- Identification of apelin/APJ signaling dysregulation in a human iPSC-derived granulosa cell model of Turner syndrome.Cell death discovery · 2024Article
- Bone Morphogenetic Protein Signaling Agonist SB4 (BMPSB4) Inhibits Corticotroph Pituitary Neuroendocrine Tumors by Activation of Autophagy via a BMP4/SMADs-Dependent Pathway.ACS pharmacology & translational science · 2024Article
- Small-Molecule Probes as Pharmacological Tools for the Bone Morphogenetic Protein Signaling Pathway.ACS pharmacology & translational science · 2023Review
- Discovery of a novel class of benzimidazoles as highly effective agonists of bone morphogenetic protein (BMP) receptor signaling.Scientific reports · 2022Article
- Ligand-receptor promiscuity enables cellular addressing.Cell systems · 2022Article
- Identification of Pax protein inhibitors that suppress target gene expression and cancer cell proliferation.Cell chemical biology · 2022Article
- Addition of Chk1 inhibitor and BMP4 cooperatively promotes retinal tissue formation in self-organizing human pluripotent stem cell differentiation culture.Regenerative therapy · 2022Article
- Kartogenin Improves Osteogenesis of Bone Marrow Mesenchymal Stem Cells via Autophagy.Stem cells international · 2022Article
- A Process for the Design and Development of Novel Bone Morphogenetic Protein-7 (BMP-7) Mimetics With an Example: THR-184.Frontiers in pharmacology · 2022Article
- Optogenetic Control of the BMP Signaling Pathway.ACS synthetic biology · 2020Article
- Oxysterols as promising small molecules for bone tissue engineering: Systematic review.World journal of orthopedics · 2020Article
- Mutational Analysis of the Putative Anti-Müllerian Hormone (AMH) Binding Interface on its Type II Receptor, AMHR2.Endocrinology · 2020Article
- The Interactivity between TGFβ and BMP Signaling in Organogenesis, Fibrosis, and Cancer.Cells · 2019Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 2 countries.
Funding
Abstract
Bone morphogenetic protein (BMP) signaling is critical in renal development and disease. In animal models of chronic kidney disease (CKD), re-activation of BMP signaling is reported to be protective by promoting renal repair and regeneration. Clinical use of recombinant BMPs, however, requires harmful doses to achieve efficacy and is costly because of BMPs' complex synthesis. Therefore, alternative strategies are needed to harness the beneficial effects of BMP signaling in CKD. Key aspects of the BMP signaling pathway can be regulated by both extracellular and intracellular molecules. In particular, secreted proteins like noggin and chordin inhibit BMP activity, whereas kielin/chordin-like proteins (KCP) enhance it and attenuate kidney fibrosis or CKD. Clinical development of KCP, however, is precluded by its size and complexity. Therefore, we propose an alternative strategy to enhance BMP signaling by using small molecules, which are simpler to synthesize and more cost-effective. To address our objective, here we developed a small-molecule high-throughput screen (HTS) with human renal cells having an integrated luciferase construct highly responsive to BMPs. We demonstrate the activity of a potent benzoxazole compound, sb4, that rapidly stimulated BMP signaling in these cells. Activation of BMP signaling by sb4 increased the phosphorylation of key second messengers (SMAD-1/5/9) and also increased expression of direct target genes (inhibitors of DNA binding,
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