154672-63-6

Upstream product

• 71989-18-9 Fmoc-Glu(OtBu)-OH 
• 100-51-6 benzyl alcohol 
• 100-39-0 benzyl bromide 

Downstream Products

• 154672-64-7 Benzyl ester of α-N-(9-fluorenylmethoxycarbonyl)-γ-N<2-(trimethylsilyl)ethoxy>amide of L-glutamic acid 
• 1053693-02-9 (S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-5-(2-trimethylsilanyl-ethoxyamino)-pentanoic acid benzyl ester 
• 122350-52-1 (4S)-5-benzyloxy-4-(9H-fluoren-9-ylmethoxycarbonylamino)-5-oxopentanoic acid 

Relevant academic research and scientific papers

ANTI-HUMAN VISTA ANTIBODIES AND USE THEREOF

The invention provides anti-VISTA antibody drug conjugates which may be used for targeted delivery of anti-inflammatory agents such as steroids to immune cells, e.g., myeloid cells. The invention also provides methods of using anti-VISTA antibody drug conjugates in the treatment of inflammatory and/or autoimmune conditions and/or for alleviating the toxicity of anti-inflammatory agents such as steroids.

Novel synthesis of cyclic amide-linked analogues of angiotensins II and III

Cyclic amide-linked angiotensin II (ANGII) analogues have been synthesized by novel strategies, in an attempt to test the ring clustering and the charge relay bioactive conformation recently suggested. These analogues were synthesized by connecting side chain amino and carboxyl groups at positions 1 and 8, 2 and 8, 3 and 8, and 3 and 5, N-terminal amino and C-terminal carboxyl groups at positions 1 and 8, 2 and 8, and 4 and 8, and side chain amino to C-terminal carboxyl group at positions 1 and 8. All these analogues were biologically inactive, except for cyclic [Sar1,Asp3,Lys5]ANGII (analogue 10) which had high contractile activity in the rat uterus assay (30% of ANGII) and [Lys1,Tyr(Me)4,Glu8]ANGII (analogue 7) which had weak antagonist activity (PA2 ? 6). Precyclic linear peptides synthesized using 2-chlorotrityl chloride resin and N(α)-Fmoc-amino acids with suitable side chain protection were obtained in high yield and purity and were readily cyclized with benzotriazol-1-yloxytris(dimethylamino)-phosphonium hexafluorophosphate as coupling reagent. Molecular modeling suggests that the ring structure of the potent analogue can be accommodated in the charge relay conformation proposed for ANGII.

'BOP' as a reagent for mild and efficient preparation of esters

A simple procedure for preparation of esters under mild conditions employing the BOP reagent is reported. Acid and base labile protecting groups commonly used with amino acids e.g. t-butyl, Fmoc etc., are well tolerated under these conditions. The mechani