1024602-82-1Relevant academic research and scientific papers
NOVEL CONJUGATION CHEMISTRY FOR CATALYTIC ANTTIBODY 38C2
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Paragraph 0092; 00105, (2021/04/30)
The present invention provides modified catalytic antibody 38C2 with arylation of the reactive lysine residue (Lys99). The Lys99 residue is arylated with a heteroaryl methyl sulfonyl compound such as methylsulfone phenyl oxadi azole (MS- PODA). The invention also provides antibody conjugated agents (e.g., antibody drug conjugates) that contain an agent moiety that is site-specifically conjugated to 38C2 via a methyl sulfonyl compound. Further provided in the invention are methods of making the antibody conjugated agents and therapeutic applications of the antibody conjugated agents.
PROCESSES FOR PREPARING PEPTIDE CONJUGATES AND LINKERS
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Paragraph 0173-0181, (2015/02/19)
The present invention provides a process for preparing a compound of Formula 5b, as well as intermediates thereof, and novel classes of compounds useful in process for preparing these and similar compounds.
Chromatography- and lyophilization-free synthesis of a peptide- linker conjugate
Magano, Javier,Bock, Brandon,Brennan, John,Farrand, Douglas,Lovdahl, Michael,Maloney, Mark T.,Nadkarni, Durgesh,Oliver, Wendy K.,Pozzo, Mark J.,Teixeira, John J.,Wang, Jian,Rizzo, John,Tumelty, David
, p. 142 - 151 (2014/05/20)
An optimized and scalable process to manufacture peptide-linker conjugate 1 is reported that avoids the chromatographic purification and lyophilization that are typically required for the isolation of this type of compound. An operationally simple protoco
Development of a long acting human growth hormone analog suitable for once a week dosing
Palanki, Moorthy S.S.,Bhat, Abhijit,Bolanos, Ben,Brunel, Florence,Del Rosario, Joselyn,Dettling, Danielle,Horn, Mark,Lappe, Rodney,Preston, Ryan,Sievers, Annette,Stankovic, Nebojsa,Woodnut, Gary,Chen, Gang
, p. 402 - 406 (2013/02/23)
Human growth hormone was conjugated to a carrier aldolase antibody, using a novel linker by connecting a disulphide bond in growth hormone to a lysine-94 amine located on the Fab arm of the antibody. The resulting CovX body showed reduced affinity towards human growth hormone receptor, reduced cell-based activity, but improved pharmacodynamic properties. We have demonstrated that this CovX-body, given once a week, showed comparable activity as growth hormone given daily in an in vivo hypophysectomized rat model.
Development of novel linkers to conjugate pharmacophores to a carrier antibody
Palanki, Moorthy S.S.,Bhat, Abhijit,Lappe, Rodney W.,Liu, Bin,Oates, Bryan,Rizzo, John,Stankovic, Nebojsa,Bradshaw, Curt
, p. 4249 - 4253 (2012/07/17)
We have developed modified maleimide novel linkers with improved chemical stability that could potentially be used in conjugating various pharmacophores such as oligo nucleotides, peptides, and proteins to antibodies to afford novel biologics with well-de
