250612-31-8Relevant articles and documents
Obviation of hydrogen fluoride in Boc chemistry solid phase peptide synthesis of peptide-αthioesters
Gates, Zachary P.,Dhayalan, Balamurugan,Kent, Stephen B. H.
, p. 13979 - 13982 (2016)
Under suitable conditions, trifluoromethanesulfonic acid performs comparably to hydrogen fluoride for the on-resin global deprotection of peptides prepared by Boc chemistry solid phase peptide synthesis (SPPS). Obviation of hydrogen fluoride in Boc chemis
Dimeric argininamide-type neuropeptide y receptor antagonists: Chiral discrimination between Y1 and Y4 receptors
Keller, Max,Kaske, Melanie,Holzammer, Tobias,Bernhardt, Guenther,Buschauer, Armin
supporting information, p. 6303 - 6322 (2013/10/22)
The structurally related peptides neuropeptide Y (NPY), peptide YY (PYY) and pancreatic polypeptide (PP) are endogenous agonists of the NPY receptor (YR) family, which in humans comprises four functionally expressed subtypes, designated Y1R, Y2R, Y4R and Y5R. Nonpeptide antagonists with high affinity and selectivity have been described for the Y1R, Y2R and Y5R, but such compounds are still lacking for the Y4R. In this work, the structures of the high affinity selective (R)-argininamide-type Y1R antagonists BIBP3226 and BIBO3304 were linked via the guanidine or urea moieties to give homo-dimeric argininamides with linker lengths ranging from 31 to 41 atoms. Interestingly, the twin compounds proved to be by far less selective for the Y1R than the R-configured monovalent parent compounds. The decrease in selectivity ratio was most pronounced for Y1R versus Y 4R subtype, resulting in comparable affinities of bivalent ligands for Y1R and Y4R (e.g. UR-MK177 ((R,R)-49): Ki = 230 nM (Y1R) and 290 nM (Y4R)). With a Ki value of 130 nM and a Kb value of 20 nM, UR-MK188 ((R,R)-51) was superior to all Y4R antagonists known to date. The S,S-configured optical antipodes of UR-MK177 and UR-MK188 (UR-MEK381 ((S,S)-49) and UR-MEK388 ((S,S)-51)) were synthesized to investigate the stereochemical discrimination by the different receptor subtypes. Whereas preference for R,R-configured argininamides was characteristic of the Y1R, stereochemical discrimination by the Y4R was not observed. This may pave the way to selective Y4R antagonists.
A modular cross-linking approach for exploring protein interactions
Trester-Zedlitz, Michelle,Kamada, Katsuhiko,Burley, Stephen K.,Fenyoe, David,Chait, Brian T.,Muir, Tom W.
, p. 2416 - 2425 (2007/10/03)
A method is described for the elucidation of protein-protein interactions using novel cross-linking reagents and mass spectrometry. The method incorporates (1) a modular solid-phase synthetic strategy for generating the cross-linking reagents, (2) enrichm
Pharmaceuticals for the imaging of angiogenic disorders
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, (2008/06/13)
The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present
Simultaneous imaging of cardiac perfusion and a vitronectin receptor targeted imaging agent
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, (2008/06/13)
The present invention describes a method of concurrent imaging in a mammal comprising: a) administering to said mammal a vitronectin receptor targeted imaging agent and a perfusion imaging agent; and b) concurrently detecting the vitronectin target imagin