(WFRF:(Fryknäs Mårten)) srt2:(2020-2024)
Search: (WFRF:(Fryknäs Mårten)) srt2:(2020-2024) > Rational Design of ...
- 9 of 20
- Previous record
- Next record
- To hitlist
| Fältnamn | Indikatorer | Metadata |
|---|---|---|
| 000 | 03316naa a2200457 4500 | |
| 001 | oai:DiVA.org:uu-435956 | |
| 003 | SwePub | |
| 008 | 210302s2020 | |||||||||||000 ||eng| | |
| 024 | 7 | a https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-4359562 URI |
| 024 | 7 | a https://doi.org/10.1002/cmdc.2020004972 DOI |
| 040 | a (SwePub)uu | |
| 041 | a engb eng | |
| 042 | 9 SwePub | |
| 072 | 7 | a ref2 swepub-contenttype |
| 072 | 7 | a art2 swepub-publicationtype |
| 100 | 1 | a Hartmann, Rafaelu Uppsala universitet,Preparativ läkemedelskemi4 aut0 (Swepub:uu)rafha922 |
| 245 | 1 0 | a Rational Design of Azastatin as a Potential ADC Payload with Reduced Bystander Killing. |
| 264 | c 2020-10-16 | |
| 264 | 1 | b Wiley,c 2020 |
| 338 | a electronic2 rdacarrier | |
| 520 | a Auristatins are a class of ultrapotent microtubule inhibitors, whose growing clinical popularity in oncology is based upon their use as payloads in antibody-drug conjugates (ADCs). The most widely utilized auristatin, MMAE, has however been shown to cause apoptosis in non-pathological cells proximal to the tumour ("bystander killing"). Herein, we introduce azastatins, a new class of auristatin derivatives encompassing a side chain amine for antibody conjugation. The synthesis of Cbz-azastatin methyl ester, which included the C2-elongation and diastereoselective reduction of two proteinogenic amino acids as key transformations, was accomplished in 22 steps and 0.76 % overall yield. While Cbz-protected azastatin methyl ester (0.13-3.0 nM) inhibited proliferation more potently than MMAE (0.47-6.5 nM), removal of the Cbz-group yielded dramatically increased IC50 -values (9.8-170 nM). We attribute the reduced apparent cytotoxicity of the deprotected azastatin methyl esters to a lack of membrane permeability. These results clearly establish the azastatins as a novel class of cytotoxic payloads ideally suited for use in next-generation ADC development. | |
| 650 | 7 | a MEDICIN OCH HÄLSOVETENSKAPx Medicinska och farmaceutiska grundvetenskaperx Läkemedelskemi0 (SwePub)301032 hsv//swe |
| 650 | 7 | a MEDICAL AND HEALTH SCIENCESx Basic Medicinex Medicinal Chemistry0 (SwePub)301032 hsv//eng |
| 653 | a Antibodies | |
| 653 | a Cytotoxicity | |
| 653 | a Diastereoselectivity | |
| 653 | a Medicinal chemistry | |
| 653 | a Total synthesis | |
| 700 | 1 | a Fahrner, Raphael4 aut |
| 700 | 1 | a Shevshenko, Denys4 aut |
| 700 | 1 | a Fryknäs, Mårtenu Uppsala universitet,Cancerfarmakologi och beräkningsmedicin4 aut0 (Swepub:uu)mafry516 |
| 700 | 1 | a Larsson, Rolfu Uppsala universitet,Cancerfarmakologi och beräkningsmedicin4 aut0 (Swepub:uu)rolflars |
| 700 | 1 | a Lehmann, Fredrik4 aut |
| 700 | 1 | a Odell, Luke R.u Uppsala universitet,Preparativ läkemedelskemi4 aut0 (Swepub:uu)lucod220 |
| 710 | 2 | a Uppsala universitetb Preparativ läkemedelskemi4 org |
| 773 | 0 | t ChemMedChemd : Wileyg 15:24, s. 2500-2512q 15:24<2500-2512x 1860-7179x 1860-7187 |
| 856 | 4 | u https://doi.org/10.1002/cmdc.202000497y Fulltext |
| 856 | 4 | u https://uu.diva-portal.org/smash/get/diva2:1532502/FULLTEXT01.pdfx primaryx Raw objecty fulltext:print |
| 856 | 4 | u https://doi.org/10.1002/cmdc.202000497 |
| 856 | 4 8 | u https://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-435956 |
| 856 | 4 8 | u https://doi.org/10.1002/cmdc.202000497 |
- 9 of 20
- Previous record
- Next record
- To hitlist
Find more in SwePub
- By the author/editor
- Hartmann, Rafael
- Fahrner, Raphael
- Shevshenko, Deny ...
- Fryknäs, Mårten
- Larsson, Rolf
- Lehmann, Fredrik
- show more...
- Odell, Luke R.
- show less...
- About the subject
-
- MEDICAL AND HEALTH SCIENCES
- MEDICAL AND HEAL ...
- and Basic Medicine
- and Medicinal Chemis ...
- Articles in the publication
- ChemMedChem
- By the university
- Uppsala University
Search outside SwePub
- Extend your search to:
- Google Book Search
- Google Scholar
Kungliga biblioteket hanterar dina personuppgifter i enlighet med EU:s dataskyddsförordning (2018), GDPR. Läs mer om hur det funkar här.
Så här hanterar KB dina uppgifter vid användning av denna tjänst.
- Copyright © LIBRIS - National Library Systems
- LIBRIS.kb.se
