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 DRUG RELEASE FROM SOLID SUPPORTS
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Page/Page column 31-32, (2011/11/30)
The invention relates to solid supports useful in medical applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the solid support through a linkage that releases the drug or a prodrug through controlled beta elimination.
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.
HIGHLY AFFINE COSMETIC AGENT
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Page 25; 26, (2008/06/13)
The invention relates to a cosmetic agent which is made essentially of a peptide linker and at least one cosmetic active ingredient which is covalently connected thereto.
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