YAP-dependent proliferation by a small molecule targeting annexin A2 was written by Shalhout, Sophia Z.;Yang, Peng-Yu;Grzelak, Edyta M.;Nutsch, Kayla;Shao, Sida;Zambaldo, Claudio;Iaconelli, Jonathan;Ibrahim, Lara;Stanton, Caroline;Chadwick, Stormi R.;Chen, Emily;DeRan, Michael;Li, Sijia;Hull, Mitchell;Wu, Xu;Chatterjee, Arnab K.;Shen, Weijun;Camargo, Fernando D.;Schultz, Peter G.;Bollong, Michael J.. And the article was included in Nature Chemical Biology in 2021.Computed Properties of C12H25N3O2 This article mentions the following:
Abstract: The transcriptional coactivator Yes-associated protein 1 (YAP) orchestrates a pro-proliferative transcriptional program that controls the fate of somatic stem cells and the regenerative responses of certain tissues. As such, agents that activate YAP may hold therapeutic potential in disease states exacerbated by insufficient proliferative repair. Here we report the discovery of a small mol., termed PY-60, which robustly activates YAP transcriptional activity in vitro and promotes YAP-dependent expansion of epidermal keratinocytes in mouse following topical drug administration. Chem. proteomics revealed the relevant target of PY-60 to be annexin A2 (ANXA2), a protein that directly associates with YAP at the cell membrane in response to increased cell d. PY-60 treatment liberates ANXA2 from the membrane, ultimately promoting a phosphatase-bound, nonphosphorylated and transcriptionally active form of YAP. This work reveals ANXA2 as a previously undescribed, druggable component of the Hippo pathway and suggests a mechanistic rationale to promote regenerative repair in disease. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1Computed Properties of C12H25N3O2).
tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate (cas: 373608-48-1) belongs to piperazine derivatives. Simple N-substituted piperazines have been found in many drug molecules. Piperazines are very broad chemical group, covering a wide range of drugs from antidepressants to antihistamines. The connecting property of all these chemicals is the presence of a piperazine functional group.Computed Properties of C12H25N3O2
Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics