1094-76-4Relevant articles and documents
A peptide-based fluorescent probe images ERAAP activity in cells and in high throughput assays
Zhang, Jingtuo,Yang, Soo Jung,Gonzalez, Federico,Yang, Jiaying,Zhang, Yumiao,He, Maomao,Shastri, Nilabh,Murthy, Niren
, p. 7215 - 7218 (2018)
ERAAP is an intracellular amino-peptidase that plays a central role in determining the repertoire of peptides displayed by cells by MHC class I molecules, and dysfunctions in ERAAP are linked to a variety of diseases. There is therefore great interest in developing probes that can image ERAAP in cells. In this report we present a fluorescent probe, termed Ep, that can image ERAAP activity in live cells. Ep is composed of a 10 amino acid ERAAP substrate that has a donor quencher pair conjugated to it, composed of BODIPY and dinitro-toluene. Ep undergoes a 20-fold increase in fluorescence after ERAAP cleavage, and was able to image ERAAP activity in cell culture via fluorescence microscopy. In addition, we used Ep to develop a high throughput screen for ERAAP inhibitors, and screened an electrophile library containing 1460 compounds. From this Ep based screen we identified aromatic alkyne-ketone as a lead fragment that can irreversibly inhibit ERAAP activity. We anticipate numerous applications of Ep given its unique ability to image ERAAP within cells.
CONTROLLED RELEASE FROM MACROMOLECULAR CONJUGATES
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Page/Page column 24-25, (2011/11/30)
The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.
Synthesis and application of unprotected cyclic peptides as building blocks for peptide dendrimers
Zhang, Lianshan,Tam, James P.
, p. 2363 - 2370 (2007/10/03)
We describe an efficient regiospecific method for cyclization of unprotected peptide segments based on intramolecular transthioesterification of unprotected cysteinyl peptide thioesters under the control of ring-chain tautomeric equilibrium in aqueous buf