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Sökning: onr:"swepub:oai:lup.lub.lu.se:88935f5f-2d4d-4f16-bd62-42217f8dd08f" > Novel Selective Gal...

LIBRIS Formathandbok  (Information om MARC21)
FältnamnIndikatorerMetadata
00003937naa a2200433 4500
001oai:lup.lub.lu.se:88935f5f-2d4d-4f16-bd62-42217f8dd08f
003SwePub
008220902s2022 | |||||||||||000 ||eng|
0247 a https://lup.lub.lu.se/record/88935f5f-2d4d-4f16-bd62-42217f8dd08f2 URI
0247 a https://doi.org/10.1021/acs.jmedchem.1c012962 DOI
040 a (SwePub)lu
041 a engb eng
042 9 SwePub
072 7a art2 swepub-publicationtype
072 7a ref2 swepub-contenttype
1001 a Bum-Erdene, Khuchtumuru Griffith University4 aut
2451 0a Novel Selective Galectin-3 Antagonists Are Cytotoxic to Acute Lymphoblastic Leukemia
264 c 2022-04-15
264 1b American Chemical Society (ACS),c 2022
300 a 15 s.
520 a Galectin-3 is a β-galactoside-specific, carbohydrate-recognizing protein (lectin) that is strongly implicated in cancer development, metastasis, and drug resistance. Galectin-3 promotes migration and ability to withstand drug treatment of B-cell precursor acute lymphoblastic leukemia (BCP-ALL) cells. Due to high amino acid conservation among galectins and the shallow nature of their glycan-binding site, the design of selective potent antagonists targeting galectin-3 is challenging. Herein, we report the design and synthesis of novel taloside-based antagonists of galectin-3 with enhanced affinity and selectivity. The molecules were optimized by in silico docking, selectivity was established against four galectins, and the binding modes were confirmed by elucidation of X-ray crystal structures. Critically, the specific inhibition of galectin-3-induced BCP-ALL cell agglutination was demonstrated. The compounds decreased the viability of ALL cells even when grown in the presence of protective stromal cells. We conclude that these compounds are promising leads for therapeutics, targeting the tumor-supportive activities of galectin-3 in cancer.
650 7a MEDICIN OCH HÄLSOVETENSKAPx Medicinska och farmaceutiska grundvetenskaperx Läkemedelskemi0 (SwePub)301032 hsv//swe
650 7a MEDICAL AND HEALTH SCIENCESx Basic Medicinex Medicinal Chemistry0 (SwePub)301032 hsv//eng
7001 a Collins, Patrick M.u Griffith University4 aut
7001 a Hugo, Matthew W.u Griffith University4 aut
7001 a Tarighat, Somayeh S.u Children's Hospital Los Angeles4 aut
7001 a Fei, Feiu Children's Hospital Los Angeles4 aut
7001 a Kishor, Chandanu Griffith University4 aut
7001 a Leffler, Hakonu Lund University,Lunds universitet,Avdelningen för mikrobiologi, immunologi och glykobiologi - MIG,Institutionen för laboratoriemedicin,Medicinska fakulteten,LUCC: Lunds universitets cancercentrum,Övriga starka forskningsmiljöer,Division of Microbiology, Immunology and Glycobiology - MIG,Department of Laboratory Medicine,Faculty of Medicine,LUCC: Lund University Cancer Centre,Other Strong Research Environments4 aut0 (Swepub:lu)mmb-hle
7001 a Nilsson, Ulf J.u Lund University,Lunds universitet,Centrum för analys och syntes,Kemiska institutionen,Institutioner vid LTH,Lunds Tekniska Högskola,Centre for Analysis and Synthesis,Department of Chemistry,Departments at LTH,Faculty of Engineering, LTH4 aut0 (Swepub:lu)ok2-uni
7001 a Groffen, Johnu Children's Hospital Los Angeles4 aut
7001 a Grice, I. Darrenu Griffith University4 aut
7001 a Heisterkamp, Norau Children's Hospital Los Angeles4 aut
7001 a Blanchard, Helenu Griffith University4 aut
7102 a Griffith Universityb Children's Hospital Los Angeles4 org
7730 t Journal of Medicinal Chemistryd : American Chemical Society (ACS)g 65:8, s. 5975-5989q 65:8<5975-5989x 0022-2623x 1520-4804
8564 u http://dx.doi.org/10.1021/acs.jmedchem.1c01296y FULLTEXT
8564 8u https://lup.lub.lu.se/record/88935f5f-2d4d-4f16-bd62-42217f8dd08f
8564 8u https://doi.org/10.1021/acs.jmedchem.1c01296

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