Pub. Date : 2015 Mar 24
PMID : 25801024
5 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | Structure guided design of potent and selective ponatinib-based hybrid inhibitors for RIPK1. | ponatinib | receptor interacting serine/threonine kinase 1 | Homo sapiens |
| 2 | In the current work, we report that the Bcr-Abl inhibitor and anti-leukemia agent ponatinib is also a first-in-class dual inhibitor of RIPK1 and RIPK3. | ponatinib | receptor interacting serine/threonine kinase 1 | Homo sapiens |
| 3 | Ponatinib potently inhibited multiple paradigms of RIPK1- and RIPK3-dependent cell death and inflammatory tumor necrosis factor alpha (TNF-alpha) gene transcription. | ponatinib | receptor interacting serine/threonine kinase 1 | Homo sapiens |
| 4 | We further describe design strategies that utilize the ponatinib scaffold to develop two classes of inhibitors (CS and PN series), each with greatly improved selectivity for RIPK1. | ponatinib | receptor interacting serine/threonine kinase 1 | Homo sapiens |
| 5 | In particular, we detail the development of PN10, a highly potent and selective "hybrid" RIPK1 inhibitor, capturing the best properties of two different allosteric RIPK1 inhibitors, ponatinib and necrostatin-1. | ponatinib | receptor interacting serine/threonine kinase 1 | Homo sapiens |