581065-94-3Relevant academic research and scientific papers
Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders
D?lle, Anja,Adhikari, Bikash,Kr?mer, Andreas,Weckesser, Janik,Berner, Nicola,Berger, Lena-Marie,Diebold, Mathias,Szewczyk, Magdalena M.,Barsyte-Lovejoy, Dalia,Arrowsmith, Cheryl H.,Gebel, Jakob,L?hr, Frank,D?tsch, Volker,Eilers, Martin,Heinzlmeir, Stephanie,Kuster, Bernhard,Sotriffer, Christoph,Wolf, Elmar,Knapp, Stefan
, p. 10682 - 10710 (2021/05/29)
Histone H3K4 methylation serves as a post-translational hallmark of actively transcribed genes and is introduced by histone methyltransferase (HMT) and its regulatory scaffolding proteins. One of these is the WD-repeat-containing protein 5 (WDR5) that has also been associated with controlling long noncoding RNAs and transcription factors including MYC. The wide influence of dysfunctional HMT complexes and the typically upregulated MYC levels in diverse tumor types suggested WDR5 as an attractive drug target. Indeed, protein-protein interface inhibitors for two protein interaction interfaces on WDR5 have been developed. While such compounds only inhibit a subset of WDR5 interactions, chemically induced proteasomal degradation of WDR5 might represent an elegant way to target all oncogenic functions. This study presents the design, synthesis, and evaluation of two diverse WDR5 degrader series based on two WIN site binding scaffolds and shows that linker nature and length strongly influence degradation efficacy.
USES OF ANTI-CD3 ANTIBODY FOLATE BIOCONJUGATES
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Paragraph 00357; 00359, (2021/09/03)
Described herein are anti-CD3 antibody folate bioconjugates and uses thereof in the treatment of diseases, conditions, and cancers.
Optimization of IEDDA bioorthogonal system: Efficient process to improve trans-cyclooctene/tetrazine interaction
Béquignat, Jean-Baptiste,Boucheix, Claude,Canitrot, Damien,Chezal, Jean-Michel,Degoul, Fran?oise,Miot-Noirault, Elisabeth,Moreau, Emmanuel,Navarro-Teulon, Isabelle,Quintana, Mercedes,Rondon, Aurélie,Taiariol, Ludivine,Ty, Nancy
supporting information, (2020/07/21)
The antibody pretargeting approach for radioimmunotherapy (RIT) using inverse electron demand Diels-Alder cycloaddition (IEDDA) constitutes an emerging theranostic approach for solid cancers. However, IEDDA pretargeting has not reached clinical trial. The major limitation of the IEDDA strategy depends largely on trans-cyclooctene (TCO) stability. Indeed, TCO may isomerize into the more stable but unreactive cis-cyclooctene (CCO), leading to a drastic decrease of IEDDA efficiency. We have thus developed both efficient and reproducible synthetic pathways and analytical follow up for (PEGylated) TCO derivatives, providing high TCO isomeric purity for antibody modification. We have set up an original process to limit the isomerization of TCO to CCO before the mAbs’ functionalization to allow high TCO/tetrazine cycloaddition.
ANTI-CD3 ANTIBODY FOLATE BIOCONJUGATES AND THEIR USES
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Paragraph 00338; 00349; 00351, (2020/03/23)
Described herein are novel anti-CD3 Folate antibodies and uses thereof in the treatment of diseases or conditions that would benefit from such.
Preparation method, raw material, product and application of photo-crosslinking hydrogel material
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Paragraph 0668; 0669; 0677, (2019/06/07)
The invention provides a preparation method, a raw material, a product and an application of a photo-crosslinking hydrogel material. The preparation method comprises the steps of dissolving a component A, namely a photosensitive high polymer derivative, i
A-amido glycol propionic acid preparation method (by machine translation)
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Paragraph 0021, (2017/10/22)
The invention discloses a-amido glycol propionic acid (NH2 - PEGn - CH2 CH2 C00H, n=1 - 24) of the preparation method, the preparation method in order to mono-disperse small molecular double-hydroxy polyethylene
DIBENZOSILOLE MONOMERS AND POLYMERS AND METHODS FOR THEIR PREPARATION AND USE
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Page/Page column 33, (2016/06/01)
Water-soluble, conjugated polymers containing one or more dibenzosilole monomer residues, as well as compositions, kits, and methods of making and using such polymers are disclosed. Also disclosed are dibenzosilole derivatives substituted with one or more
PROSTATE-SPECIFIC MEMBRANE ANTIGEN ANTIBODY DRUG CONJUGATES
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Paragraph 00510, (2014/01/08)
This invention relates to prostate-specific membrane antigen (PSMA) antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are αPSMA antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the αPSMA antibodies of the invention are conjugated to one or more toxins. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, dolastatin analogs, and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology uses.
ANTI-CD70 ANTIBODY DRUG CONJUGATES
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Paragraph 00524, (2014/01/09)
This invention relates to anti-CD70 antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are αCD70 antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the αCD70 antibodies of the invention are conjugated to one or more toxins. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, including therapeutic, diagnostic, and other biotechnology uses.
COMPOSITIONS CONTAINING, METHODS INVOLVING, AND USES OF NON-NATURAL AMINO ACID LINKED DOLASTATIN DERIVATIVES
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Page/Page column 182, (2013/02/28)
Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology use.
