154524-72-8

Upstream product

• 87413-09-0 Dess-Martin periodane 
• 187526-99-4 (9H-fluoren-9-yl)methyl (S)-(1-(4-(tert-butoxy)phenyl)-3-hydroxypropan-2-yl)carbamate 
• 71989-38-3 Fmoc-Tyr(tBu)-OH 
• 105916-78-7 3-(4-tert-butoxy-phenyl)-2-(9H-fluoren-9-ylmethoxycarbonylamino)-propionic acid benzotriazol-1-yl ester 
• 156939-66-1 Fmoc-Tyr(tBu)-N(CH₃)-OCH₃ 

Downstream Products

• 301544-43-4 [4-(4-tert-butoxy-phenyl)-3-(9H-fluoren-9-ylmethoxycarbonylamino)-2-hydroxy-butyrylamino]-acetic acid ethyl ester 
• 315249-49-1 C₃₄H₅₀N₈O₁₁S 

Relevant academic research and scientific papers

Triazolo-peptidomimetics: novel radiolabeled minigastrin analogs for improved tumor targeting

MG11 is a truncated analog of minigastrin, a peptide with high affinity and specificity toward the cholecystokinin-2 receptor (CCK2R), which is overexpressed by different tumors. Thus, radiolabeled MG11 derivatives have great potential for use in cancer d

Rational Design of Right-Handed Heterogeneous Peptidomimetics as Inhibitors of Protein-Protein Interactions

Peptidomimetics have gained great attention for their function as protein-protein interaction (PPI) inhibitors. Herein, we report the design and investigation of a series of right-handed helical heterogeneous 1:1 α/Sulfono-I-AA peptides as unprecedented inhibitors for p53-MDM2 and p53-MDMX. The most potent helical heterogeneous 1:1 α/Sulfono-I-AA peptides were shown to bind tightly to MDM2 and MDMX, with Kd of 19.3 and 66.8 nM, respectively. Circular dichroism spectra, 2D-NMR spectroscopy, and the computational simulations suggested that these helical sulfono-I-AA peptides could mimic the critical side chains of p53 and disrupt p53/MDM2 PPI effectively. It was noted that these 1:1 α/Sulfono-I-AA peptides were completely resistant to proteolytic degradation, boosting their potential for biomedical applications. Furthermore, effective cellular activity is achieved by the stapled 1:1 α/Sulfono-I-AA peptides, evidenced by significantly enhanced p53 transcriptional activity and much more induced level of MDM2 and p21. The 1:1 α/Sulfono-I-AA peptides could be an alternative strategy to antagonize a myriad of PPIs.

Synthesis and biological activity of peptide α-ketoamide derivatives as proteasome inhibitors

Proteasome activity affects cell cycle progression as well as the immune response, and it is largely recognized as an attractive pharmacological target for potential therapies against several diseases. Herein we present the synthesis of a series of pseudo

Somatostatin-Dopamine Chimeric Analogs

The present invention relates to novel somatostatin-dopamine chimeric analogs and their therapeutic uses for the inhibition, prevention, and/or treatment of neoplasia, neuroendocrine tumors, Cushing's disease/syndrome, and other conditions.

Synthesis of α, β-unsaturated γ-amino esters with unprecedented high (E)-stereoselectivity and their conformational analysis in peptides

Mild, efficient and racemization-free synthesis of N-protected α, β-unsaturated γ-amino esters with unprecedented high E- stereoselectivity is described. This method is found to be compatible with Boc-, Fmoc- and other side chain protecting groups. The crystal conformations of the vinylogous γ-amino esters in monomers and in homo- and mixed dipeptides are studied. Further, the vinylogous homo-dipeptide showed a β-sheet conformation, while mixed α- and α,β-unsaturated γ-hybrid dipeptide adapted an irregular structure in single crystals.

Tin(ii) chloride assisted synthesis of N-protected γ-amino β-keto esters through semipinacol rearrangement

A facile synthetic route for the preparation of N-protected γ-amino β-keto esters from amino aldehydes and ethyl diazoacetate is described. The two component coupling is facilitated by tin(ii) chloride followed by semipinacol rearrangement leading to the product in quantitative yield. The reaction is mild, instantaneous and compatible with Boc-, Fmoc- and Cbz-amino protecting groups.

Solid-phase synthesis and screening of N-acylated polyamine (NAPA) combinatorial libraries for protein binding

Inhibitors for protein-protein interactions are challenging to design, in part due to the unique and complex architectures of each protein's interaction domain. Most approaches to develop inhibitors for these interactions rely on rational design, which re

POLYAMINE COMPOUNDS THAT BIND TAR RNA OF HIV AND METHODS OF TREATING VIRAL DISORDERS

The invention provides for novel polyamine compounds, substituted at the side chains, which can treat various disease states including viral infection, e.g. HIV infection, at low cytotoxicity values.

Nonionic side chains modulate the affinity and specificity of binding between functionalized polyamines and structured RNA

This Communication introduces side-chain-bearing polyamines as molecules for selective recognition of folded RNA structures. The complex folded structures associated with RNA create binding pockets for proteins, and also binding sites for small molecules.

Solid-phase synthesis of peptide vinyl sulfones as potential inhibitors and activity-based probes of cysteine proteases

(Matrix presented) Peptide vinyl sulfones were prepared from 2-chlorotrityl resin-bound phenolic amino vinyl sulfones in high yield and purity. This method enables the convenient synthesis of peptide vinyl sulfones having different amino acids at the Psu