178445-86-8Relevant articles and documents
NEUROPROTECTIVE COMPOUNDS AND METHODS OF USE THEREOF
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, (2021/04/10)
The present disclosure provides neuroprotective compounds along with their use in treating disease such as Parkinson's disease (PD). The compounds can be used as inhibitors for Parthanatos Associated AIF (apoptosis-inducing factor) Nuclease (PAAN), also known as macrophage migration inhibitor factor (MIF).
PROTEIN-BINDING COMPOUNDS
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, (2020/05/19)
The technology relates in part to compounds that bind to proteins. In certain examples, the compounds can bind to proteins that bind to rapamycin. In some examples, the compounds can bind to cellular proteins, and/or variant forms of cellular proteins, th
Targeted Covalent Inhibition of Plasmodium FK506 Binding Protein 35
Atack, Thomas C.,Raymond, Donald D.,Blomquist, Christa A.,Pasaje, Charisse Flerida,McCarren, Patrick R.,Moroco, Jamie,Befekadu, Henock B.,Robinson, Foxy P.,Pal, Debjani,Esherick, Lisl Y.,Ianari, Alessandra,Niles, Jacquin C.,Sellers, William R.
, p. 2131 - 2138 (2020/12/17)
FK506-binding protein 35, FKBP35, has been implicated as an essential malarial enzyme. Rapamycin and FK506 exhibit antiplasmodium activity in cultured parasites. However, due to the highly conserved nature of the binding pockets of FKBPs and the immunosuppressive properties of these drugs, there is a need for compounds that selectively inhibit FKBP35 and lack the undesired side effects. In contrast to human FKBPs, FKBP35 contains a cysteine, C106, adjacent to the rapamycin binding pocket, providing an opportunity to develop targeted covalent inhibitors of Plasmodium FKBP35. Here, we synthesize inhibitors of FKBP35, show that they directly bind FKBP35 in a model cellular setting, selectively covalently modify C106, and exhibit antiplasmodium activity in blood-stage cultured parasites.