83610-64-4

Upstream product

• 70533-96-9 N-tert-butoxycarbonyl-(L)-leucinamide 
• 41324-66-7 H-Pro-OBzl 
• 16652-71-4 benzyl (2S)-2-pyrrolidinecarboxylate hydrochloride 
• 13139-15-6 N-tert-butoxycarbonyl-L-leucine 
• 83610-44-0 benzyl (2S)-1-[(2S)-2-{[(tert-butoxy)carbonyl]amino}-4-methylpentanoyl]pyrrolidine-2-carboxylate 

Downstream Products

• 89545-44-8 Boc-Orn(Z)-Leu-Pro-OBzl 
• 1222507-88-1 C₂₈H₃₈N₄O₃ 
• 97475-42-8 Boc-D-Phe-Val-Orn(Z)-Leu-Pro-OSu 
• 97475-31-5 Boc-D-Phe-Val-Orn(Z)-Leu-Pro-OH 
• 78834-10-3 H-Val-Orn(Z)-Leu-Pro-OH hydrochloride 
• 97475-43-9 H-D-Phe-Val-Orn(Z)-Leu-Pro-OH 
• 78834-09-0 Boc-Val-Orn(Z)-Leu-Pro-OH 
• 95716-13-5 (S)-1-[(S)-2-((S)-5-Benzyloxycarbonylamino-2-{(S)-2-[(R)-2-((R)-2-tert-butoxycarbonylamino-3-phenyl-propionylamino)-3-phenyl-propionylamino]-3-methyl-butyrylamino}-pentanoylamino)-4-methyl-pentanoyl]-pyrrolidine-2-carboxylic acid benzyl ester 

Relevant academic research and scientific papers

Peptidomimetics for Targeting Protein-Protein Interactions between DOT1L and MLL Oncofusion Proteins AF9 and ENL

MLL-fusion proteins, AF9 and ENL, play an essential role in the recruitment of DOT1L and the H3K79 hypermethylation of MLL target genes, which is pivotal for leukemogenesis. Blocking these interactions may represent a novel therapeutic approach for MLL-rearranged leukemia. Based on the 7 mer DOT1L peptide, a class of peptidomimetics was designed. Compound 21 with modified middle residues, achieved significantly improved binding affinities to AF9 and ENL, with KD values of 15 nM and 57 nM, respectively. Importantly, 21 recognizes and binds to the cellular AF9 protein and effectively inhibits the AF9-DOT1L interactions in cells. Modifications of the N- and C-termini of 21 resulted in 28 with 2-fold improved binding affinity to AF9 and much decreased peptidic characteristics. Our study provides a proof-of-concept for development of nonpeptidic compounds to inhibit DOT1L activity by targeting its recruitment and the interactions between DOT1L and MLL-oncofusion proteins AF9 and ENL.

Design, synthesis and evaluation of monovalent Smac mimetics that bind to the BIR2 domain of the anti-apoptotic protein XIAP

We report the systematic rational design and synthesis of new monovalent Smac mimetics that bind preferentially to the BIR2 domain of the anti-apoptotic protein XIAP. Characterization of compounds in vitro (including 9i; ML101) led to the determination of key structural requirements for BIR2 binding affinity. Compounds 9h and 9j sensitized TRAIL-resistant breast cancer cells to apoptotic cell death, highlighting the value of these probe compounds as tools to investigate the biology of XIAP.

Synthesis and properties of gramicidin S analogs containing Pro-D-Phe sequence in place of D-Phe-Pro sequence in the β-turn part of the antibiotic

Two analogs of gramicidin S, [L-Pro4, D-Phe5]-gramicidin S and [L-Pro(4,4'), D-Phe(5,5')]-gramicidin S, were synthesized in order to investigate the relationships among positions of Pro residues, antibiotic activity and CD spectra. [

Studies on peptide antibiotic 'gratisin'

According to a primary structure proposed for an antibiotic peptide, gratisin, four peptides containing respectively partial sequences, L-Phe-L-Pro-L-Tyr, D-Phe-L-Pro-L-Tyr, L-Phe-L-Pro-D-Tyr, and D-Phe-L-Pro-D-Tyr, were synthesized by a liquid phase meth