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1966 3
1967 5
1968 5
1969 6
1970 6
1971 3
1972 6
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2009 1735
2010 1927
2011 2090
2012 2247
2013 2336
2014 2453
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59,597 results

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Page 1
Antibody-drug conjugates: Recent advances in linker chemistry.
Su Z, Xiao D, Xie F, Liu L, Wang Y, Fan S, Zhou X, Li S. Su Z, et al. Acta Pharm Sin B. 2021 Dec;11(12):3889-3907. doi: 10.1016/j.apsb.2021.03.042. Epub 2021 Apr 6. Acta Pharm Sin B. 2021. PMID: 35024314 Free PMC article. Review.
The pursuit of ADCs with optimal therapeutic windows has resulted in remarkable progress in the discovery and development of novel linkers. The present review summarizes the advance of the chemical trigger, linker-antibody attachment and linker-payload attach …
The pursuit of ADCs with optimal therapeutic windows has resulted in remarkable progress in the discovery and development of novel linker …
Cleavable linkers in antibody-drug conjugates.
Bargh JD , Isidro-Llobet A , Parker JS , Spring DR . Bargh JD , et al. Chem Soc Rev. 2019 Aug 12;48(16):4361-4374. doi: 10.1039/c8cs00676h. Chem Soc Rev. 2019. PMID: 31294429 Review.
Although ADC linkers can be 'non-cleavable', the vast majority of ADCs in clinical development have specific release mechanisms to allow controlled linker cleavage at the target site and are thus termed 'cleavable'. ...This review summarises the advances in the fiel …
Although ADC linkers can be 'non-cleavable', the vast majority of ADCs in clinical development have specific release mechanisms to al …
Calmodulin's Interdomain Linker Is Optimized for Dynamics Signal Transmission and Calcium Binding.
Sun B, Kekenes-Huskey PM. Sun B, et al. J Chem Inf Model. 2022 Sep 12;62(17):4210-4221. doi: 10.1021/acs.jcim.2c00587. Epub 2022 Aug 22. J Chem Inf Model. 2022. PMID: 35994621
However, a molecular picture of how amino acid differences in the linker influence protein function is still lacking. By using extensive Gaussian-accelerated MD coupled with dynamic network analysis, we reveal the molecular bases underlying the linker's role …
However, a molecular picture of how amino acid differences in the linker influence protein function is still lacking. By using extens …
Lysosomal-Cleavable Peptide Linkers in Antibody-Drug Conjugates.
Balamkundu S, Liu CF. Balamkundu S, et al. Biomedicines. 2023 Nov 16;11(11):3080. doi: 10.3390/biomedicines11113080. Biomedicines. 2023. PMID: 38002080 Free PMC article. Review.
In addition to cathepsin-cleavable linkers, there is also growing interest in legumain-sensitive linkers for ADC development. Increasing plasma stability while maintaining lysosomal cleavability of ADC linkers is an objective of intensive current research. Th …
In addition to cathepsin-cleavable linkers, there is also growing interest in legumain-sensitive linkers for ADC development. …
Exploring linker's sequence diversity to fuse carotene cyclase and hydroxylase for zeaxanthin biosynthesis.
Bouin A, Zhang C, Lindley ND, Truan G, Lautier T. Bouin A, et al. Metab Eng Commun. 2023 Apr 24;16:e00222. doi: 10.1016/j.mec.2023.e00222. eCollection 2023 Jun. Metab Eng Commun. 2023. PMID: 37168436 Free PMC article.
However, the design of a protein fusion and the choice of a linker are often challenging and lack of guidance. To determine the impact of linker parameters on fusion proteins, a library of linkers featuring various lengths, secondary structures, extensions an …
However, the design of a protein fusion and the choice of a linker are often challenging and lack of guidance. To determine the impac …
Linkers: An Assurance for Controlled Delivery of Antibody-Drug Conjugate.
Sheyi R, de la Torre BG, Albericio F. Sheyi R, et al. Pharmaceutics. 2022 Feb 11;14(2):396. doi: 10.3390/pharmaceutics14020396. Pharmaceutics. 2022. PMID: 35214128 Free PMC article. Review.
ADCs consist of recombinant monoclonal antibodies that are covalently bound to cytotoxic chemicals via synthetic linkers. The linker has a key role in ADC outcomes because its characteristics substantially impact the therapeutic index efficacy and pharmacokinetics o …
ADCs consist of recombinant monoclonal antibodies that are covalently bound to cytotoxic chemicals via synthetic linkers. The link …
Transglutaminase-Mediated Conjugations.
Anami Y, Tsuchikama K. Anami Y, et al. Methods Mol Biol. 2020;2078:71-82. doi: 10.1007/978-1-4939-9929-3_5. Methods Mol Biol. 2020. PMID: 31643050
Microbial transglutaminase (MTGase) catalyzes site-specific transpeptidation between a primary amine within linkers and the side chain of glutamine 295 within deglycosylated chimeric, humanized, and human IgG1s, affording homogeneous antibody-drug conjugates (ADCs). ...Her …
Microbial transglutaminase (MTGase) catalyzes site-specific transpeptidation between a primary amine within linkers and the side chai …
Assessing the Role of Calmodulin's Linker Flexibility in Target Binding.
Sun B, Kekenes-Huskey PM. Sun B, et al. Int J Mol Sci. 2021 May 8;22(9):4990. doi: 10.3390/ijms22094990. Int J Mol Sci. 2021. PMID: 34066691 Free PMC article.
Its binding selectivity to many of these targets is partially attributed to the protein's flexible alpha helical linker that connects its N- and C-domains. It is not well established how its linker mediates CaM's binding to regulatory targets yet. ...This effect app …
Its binding selectivity to many of these targets is partially attributed to the protein's flexible alpha helical linker that connects …
Current strategies for the design of PROTAC linkers: a critical review.
Troup RI, Fallan C, Baud MGJ. Troup RI, et al. Explor Target Antitumor Ther. 2020;1(5):273-312. doi: 10.37349/etat.2020.00018. Epub 2020 Oct 30. Explor Target Antitumor Ther. 2020. PMID: 36046485 Free PMC article. Review.
While linker design has historically received limited attention, the PROTAC field is evolving rapidly and currently undergoing an important shift from synthetically tractable alkyl and polyethylene glycol to more sophisticated functional linkers. ...The authors high …
While linker design has historically received limited attention, the PROTAC field is evolving rapidly and currently undergoing an imp …
59,597 results
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