No products in the cart.
Site specific biological coupling of engineered antibodies and Enzymatic method
Virus-like particles (VLP) Platforms for immunogens, vaccines and drug carriers
Antibody-drug Conjugate (ADC): Pre-made ADC benchmark, MOA, Production and QC
Neutralizing antibodies of virus (SARS2, HIV, HBV, Rabies, RSV, Ebola, Influenza)
Immunoglobulin Fc receptors for Fc&Fc Receptor binding assay
ILIBRA-HuEasy Monoclonal antibody (mab) humanization service (fully humanized ab)
Single domain antibody (Nanobody)
SOCAIL MEDIA
Site specific biological coupling of engineered antibodies
Advances in bioorthogonal chemistry and protein engineering contribute to the generation of more uniform ADCs. Although there are many attachment methods available on natural monoclonal antibodies, site-specific biological coupling on engineered antibodies can more effectively control Dar and avoid changing the affinity for antigen binding. In this way, natural or unnatural amino acids are added at some positions to obtain homogeneous products with excellent pharmacokinetic and pharmacodynamic characteristics.
Enzymatic method
The attachment of payloads can be achieved in a very selective manner by inserting specific amino acid tags into the antibody sequence. These tags are recognized by specific enzymes, such as formylglycine generating enzyme (FGE), microbial transglutaminase (MTG), transpeptidase or tyrosinase, so that site-specific coupling can be performed.
Aaron et al. Explored a new site-specific coupling of aldehyde labeled proteins. The technique utilizes a gene encoded pentapeptide sequence (Cys-X-Pro-X-Arg), in which cysteine residues are recognized by FGE and co translated and oxidized to formylglycine during protein expression in cells. In this way, the engineered antibody is selectively coupled with aldehyde specific linker by hips (hydrazino Pictet – Spengler) chemical method.
Microbial transglutaminase (MTGase) strategies are also often developed for location-specific coupling. MTGase catalyzes the formation of peptide bonds between the glutamine side chain at the 295 position of the glycosylated antibody and the primary amine of the substrate. Compared with other enzyme strategies, MTG is a flexible technology and does not require peptide donors to achieve coupling. As long as the acyl receptor contains a primary amine, there is no structural restriction.
Glutamine residues naturally exist in the Fc region of each heavy chain of the McAb. After deglycosylation at position 295, glutamine residues are coupled through MTGase mediated reaction to produce a uniform ADC with Dar = 2. In order to improve the efficiency, the linker with branched chain can be coupled to double the Dar, and the mutation of asparagine at position 297 to glutamine can also increase the DAR.
NBE therapeutics developed S-based Staphylococcus aureus transpeptidase A-mediated coupling. Their strategy uses transpeptidase a (srtA) to cut the amide bond between threonine and glycine residues in the motif of lpxtg (X = any amino acid) pentapeptide. It then catalyzes the coupling of glycine related payloads with the newly formed C-terminal to form peptide bonds at physiological temperature and pH.
The method was applied to different antibodies, such as anti-CD30 and anti-HER2, and maytanine and MMAE were coupled with 5-glycine labeled linkers. Both ADCs showed similar in vitro cytotoxicity to classical coupling. Trastuzumab maytanine produced by enzymatic method completely matched kadcyla in vivo test.In another example, the ADC of efficient anthracycline toxin derivative pnu-159682 was generated by transpeptidase method. Interestingly, through this technology, the coupling efficiency is even higher than that of adcetris and kadcyla analogues. In addition, the prepared pnu-159682 ADC has high stability in vitro and in vivo, and shows more efficacy than the ADC containing tubulin targeting payload.
Product List
Filters
Sort results
Reset
Apply
Cat No. | Products Name (INN Index) | INN Name | Previous Name | Target | Format | Order |
|---|---|---|---|---|---|---|
Pre-Made Losatuxizumab Vedotin Biosimilar, Whole Mab Adc, Anti-Egfr Antibody: Anti-ERBB/ERBB1/ERRP/HER1/NISBD2/PIG61/mENA therapeutic antibody Drug Conjugate |
losatuxizumab vedotin |
NA |
EGFR |
Whole mAb ADC |
||
Pre-Made Lupartumab Amadotin Biosimilar, Whole Mab Adc, Anti-Lypd3 Antibody: Anti-C4.4A therapeutic antibody Drug Conjugate |
lupartumab amadotin |
NA |
LYPD3 |
Whole mAb ADC |
||
Pre-Made Mipasetamab Uzoptirine Biosimilar, Whole Mab Adc, Anti-Axl Antibody: Anti-ARK/JTK11/Tyro7/UFO therapeutic antibody Drug Conjugate |
mipasetamab uzoptirine |
NA |
AXL |
Whole mAb ADC |
||
Pre-Made Mirvetuximab Soravtansine Biosimilar, Whole Mab Adc, Anti-Folr1 Antibody: Anti-FBP/FOLR/FRalpha/NCFTD therapeutic antibody Drug Conjugate |
mirvetuximab soravtansine |
NA |
FOLR1 |
Whole mAb ADC |
||
Pre-Made Mirzotamab Clezutoclax Biosimilar, Whole Mab Adc, Anti-Cd276 Antibody: Anti-4Ig-B7-H3/B7-H3/B7H3/B7RP-2 therapeutic antibody Drug Conjugate |
mirzotamab clezutoclax |
NA |
CD276 |
Whole mAb ADC |
||
Pre-Made Naratuximab Emtansine Biosimilar, Whole Mab Adc, Anti-Cd37 Antibody: Anti-GP52-40/TSPAN26 therapeutic antibody Drug Conjugate |
naratuximab emtansine |
NA |
CD37 |
Whole mAb ADC |
||
Pre-Made Patritumab Deruxtecan Biosimilar, Whole Mab Adc, Anti-ERBB3/Erbb-3 Antibody: Anti-ErbB-3/FERLK/HER3/LCCS2/MDA-BF-1/VSCN1/c-erbB-3/c-erbB3/erbB3-S/p180-ErbB3/p45-sErbB3/p85-sErbB3 therapeutic |
patritumab deruxtecan |
NA |
ERBB3 |
Whole mAb ADC |
||
Pre-Made Pelgifatamab Corixetan Biosimilar, Whole Mab Adc, Anti-FOLH1/GCPII Antibody: Anti-FGCP/FOLH/GCP2/NAALAD1/PSM/PSMA/mGCP therapeutic antibody Drug Conjugate |
pelgifatamab corixetan |
NA |
FOLH1 |
Whole mAb ADC |
||
Pre-Made Pinatuzumab Vedotin Biosimilar, Whole Mab Adc, Anti-Cd22 Antibody: Anti-SIGLEC-2/SIGLEC2 therapeutic antibody Drug Conjugate |
pinatuzumab vedotin |
NA |
CD22 |
Whole mAb ADC |
||
Pre-Made Pivekimab Sunirine Biosimilar, Whole Mab Adc, Anti-Il3Ra Antibody: Anti-CD123/IL3R/IL3RX/IL3RY/hIL-3Ra therapeutic antibody Drug Conjugate |
pivekimab sunirine |
NA |
IL3RA |
Whole mAb ADC |
||
Pre-Made Polatuzumab Vedotin Biosimilar, Whole Mab Adc, Anti-Cd79B Antibody: Anti-AGM6/B29/IGB therapeutic antibody Drug Conjugate |
polatuzumab vedotin |
NA |
CD79B |
Whole mAb ADC |
||
Pre-Made Praluzatamab Ravtansine Biosimilar, Whole Mab Adc, Anti-Alcam Antibody: Anti-CD166/MEMD therapeutic antibody Drug Conjugate |
praluzatamab ravtansine |
NA |
ALCAM |
Whole mAb ADC |
||
Pre-Made Rolinsatamab Talirine Biosimilar, Whole Mab Adc, Anti-Prlr Antibody: Anti-HPRL/MFAB/RI-PRLR/hPRLrI therapeutic antibody Drug Conjugate |
rolinsatamab talirine |
NA |
PRLR |
Whole mAb ADC |
||
Pre-Made Rosopatamab Tetraxetan Biosimilar, Whole Mab Adc, Anti-FOLH1/GCPII Antibody: Anti-FGCP/FOLH/GCP2/NAALAD1/PSM/PSMA/mGCP therapeutic antibody Drug Conjugate |
rosopatamab tetraxetan |
NA |
FOLH1 |
Whole mAb ADC |
||
Pre-Made Rovalpituzumab Tesirine Biosimilar, Whole Mab Adc, Anti-Dll3 Antibody: Anti-SCDO1 therapeutic antibody Drug Conjugate |
rovalpituzumab tesirine |
NA |
DLL3 |
Whole mAb ADC |
||
Pre-Made Sacituzumab Govitecan Biosimilar, Whole Mab Adc, Anti-Tacstd2 Antibody: Anti-EGP-1/EGP1/GA733-1/GA7331/GP50/M1S1/TROP2 therapeutic antibody Drug Conjugate |
sacituzumab govitecan |
NA |
TACSTD2 |
Whole mAb ADC |
||
Pre-Made Samrotamab Vedotin Biosimilar, Whole Mab Adc, Anti-Lrrc15 Antibody: Anti-LIB therapeutic antibody Drug Conjugate |
samrotamab vedotin |
NA |
LRRC15 |
Whole mAb ADC |
||
Pre-Made Serclutamab Talirine Biosimilar, Whole Mab Adc, Anti-Egfr Antibody: Anti-ERBB/ERBB1/ERRP/HER1/NISBD2/PIG61/mENA therapeutic antibody Drug Conjugate |
serclutamab talirine |
NA |
EGFR |
Whole mAb ADC |
||
Pre-Made Sirtratumab Vedotin Biosimilar, Whole Mab Adc, Anti-Slitrk6 Antibody: Anti-DFNMYP therapeutic antibody Drug Conjugate |
sirtratumab vedotin |
NA |
SLITRK6 |
Whole mAb ADC |
||
Pre-Made Sofituzumab Vedotin Biosimilar, Whole Mab Adc, Anti-Muc16 Antibody: Anti-CA125 therapeutic antibody Drug Conjugate |
sofituzumab vedotin |
NA |
MUC16 |
Whole mAb ADC |
View the Knowledge base of Antibody-drug Conjugate (ADC):
– The Landscape of Antibody-drug Conjugate (ADC): Production, Mechanisms of Action (MOA), FDA approved-antibodies, and Functional assay
– What is antibody-drug conjugate (ADC)?
– Antibody-drug conjugate (ADC) in clinical application (Approved/BLA, phaseI/II/III)
– Main elements of antibody-drug conjugate (ADC)： Antibodies and their targets
– Main elements of antibody-drug conjugate (ADC)：Linker (cleavable/non-cleavable, structure and mechanism)
– Main elements of antibody-drug conjugate (ADC)：Toxins/Payloads (Classification and function)
– Toxins/Payloads (Classification and function) of Microtubule destroying drug
– Toxins/Payloads (Classification and function) of DNA damage drugs
– Toxins/Payloads (Classification and function) of Innovative drugs
– Biological coupling technology Chemical based specific in situ antibody modification
– Endogenous coupling of amino acids and Disulfide re bridging strategy
– Glycan coupling
– Site specific biological coupling of engineered antibodies and Enzymatic method
– Biological coupling with engineered unnatural amino acids
– Review for ADC production, quality control and functional assay
– Product data of ADC
– What is antibody-drug conjugate (ADC)?
– Antibody-drug conjugate (ADC) in clinical application (Approved/BLA, phaseI/II/III)
– Main elements of antibody-drug conjugate (ADC)： Antibodies and their targets
– Main elements of antibody-drug conjugate (ADC)：Linker (cleavable/non-cleavable, structure and mechanism)
– Main elements of antibody-drug conjugate (ADC)：Toxins/Payloads (Classification and function)
– Toxins/Payloads (Classification and function) of Microtubule destroying drug
– Toxins/Payloads (Classification and function) of DNA damage drugs
– Toxins/Payloads (Classification and function) of Innovative drugs
– Biological coupling technology Chemical based specific in situ antibody modification
– Endogenous coupling of amino acids and Disulfide re bridging strategy
– Glycan coupling
– Site specific biological coupling of engineered antibodies and Enzymatic method
– Biological coupling with engineered unnatural amino acids
– Review for ADC production, quality control and functional assay
– Product data of ADC
