1267808-41-2

Upstream product

• 2483-46-7 Boc-Lys(Boc)-OH 
• 55592-82-0 (S)-(5-tert-butoxycarbonylamino-5-carbamoyl-pentyl)carbamic acid tert-butyl ester 
• 114594-04-6 (S)-benzyl 2-amino-6-((tert-butoxycarbonyl)amino)hexanoate 
• 109-89-7 diethylamine 
• 7087-68-5 N-ethyl-N,N-diisopropylamine 
• 159541-28-3 (S)-6-tert-butoxycarbonylamino-2-(9H-fluoren-9-ylmethoxycarbonylamino)hexanoic acid benzyl ester 
• 30189-36-7 N,N'-di-t-butyloxycarbonyl-(S)-lysine N-hydroxysuccinimide ester 

Relevant academic research and scientific papers

PROCESS FOR GALNAC OLIGONUCLEOTIDE CONJUGATES

The invention comprises a process for the preparation of therapeutically valuable GalNAc cluster oligonucleotide conjugates. The process comprises the coupling of an alkali metal salt, earth alkali metal salt or a tetraalkylammonium salt of an oligonucleotide with a GalNAc cluster compound or with a salt thereof and a subsequent purification.

PROCESSES FOR THE PREPARATION OF GALNAC ACID DERIVATIVES

The invention comprises a new process for the preparation of GalNAc derivatives of the formula I wherein n is an integer between 0 and 10 and its salts, corresponding enantiomers and/ or optical isomers thereof. The GalNAc acid derivative of formula I can be used for the preparation of therapeutically valuable GalNAc oligonucleotide conjugates.

GalNAc CLUSTER PHOSPHORAMIDITE

The invention comprises Gal NAc phosphoramidite derivatives of the formula (I), wherein R1 is a hydroxy protecting group, n is an integer from 0 to 10 and m is an integer from 0 to 20 and its corresponding enantiomers and/ or optical isomers thereof. The invention further comprises a process for the preparation of the Gal NAc phosphoramidite derivatives of the formula (I) and its use in the preparation of therapeutically valuable GalNAc-cluster oligonucleotide conjugates.

Galactose cluster-pharmacokinetic modulator targeting moiety for siRNA

The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cell in vivo. The pharmacokinetic modulator improve in vivo targeting compared to the targeting ligand alone. Targeting ligand-pharmacokinet

COMPOSITIONS FOR TARGETED DELIVERY OF SIRNA

The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide m

GALACTOSE CLUSTER-PHARMACOKINETIC MODULATOR TARGETING MOIETY FOR siRNA

The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to cell in vivo. The pharmacokinetic modulator improve in vivo targeting compared to the targeting ligand alone. Targeting ligand-pharmacokinetic modulator targeting moiety targeted RNAi polynucleotides can be administered in vivo alone or together with co-targeted delivery polymers.

Chemical cell-surface receptor engineering using affinity-guided, multivalent organocatalysts

Catalysts hold promise as tools for chemical protein modification. However, the application of catalysts or catalyst-mediated reactions to proteins has only recently begun to be addressed, mainly in in vitro systems. By radically improving the affinity-guided DMAP (4-dimethylaminopyridine) (AGD) catalysts that we previously reported (Koshi, Y.; Nakata, E.; Miyagawa, M.; Tsukiji, S.; Ogawa, T.; Hamachi, I. J. Am. Chem. Soc.2008, 130, 245.), here we have developed a new organocatalyst-based approach that allows specific chemical acylation of a receptor protein on the surface of live cells. The catalysts consist of a set of 'multivalent DMAP groups (the acyl transfer catalyst) fused to a ligand specific to the target protein. It was clearly demonstrated by in vitro experiments that the catalyst multivalency enables remarkable enhancement of protein acylation efficiency in the labeling of three different proteins: congerin II, a Src homology 2 (SH2) domain, and FKBP12. Using a multivalent AGD catalyst and optimized acyl donors containing a chosen probe, we successfully achieved selective chemical labeling of bradykinin B2 receptor (B2R), a G-protein coupled receptor, on the live cell-surface. Furthermore, the present tool allowed us to construct a membrane protein (B 2R)-based fluorescent biosensor, the fluorescence of which is enhanced (tuned on) in response to the antagonist ligand binding. The biosensor should be applicable to rapid and quantitative screening and assay of potent drug candidates in the cellular context. The design concept of the affinity-guided, multivalent catalysts should facilitate further development of diverse catalyst-based protein modification tools, providing new opportunities for organic chemistry in biological research.

Compositions for Targeted Delivery of siRNA

The present invention is directed compositions for targeted delivery of RNA interference (RNAi) polynucleotides to hepatocytes in vivo. Targeted RNAi polynucleotides are administered together with co-targeted delivery polymers. Delivery polymers provide m