{"entity": "publication", "iuid": "5eccb1ffb7924c30be758141222b894e", "timestamp": "2026-08-09T13:52:31.334Z", "links": {"self": {"href": "https://publications.scilifelab.se/publication/5eccb1ffb7924c30be758141222b894e.json"}, "display": {"href": "https://publications.scilifelab.se/publication/5eccb1ffb7924c30be758141222b894e"}}, "title": "Insight into Functional Membrane Proteins by Solution NMR: The Human Bcl-2 Protein-A Promising Cancer Drug Target.", "authors": [{"family": "Ul Mushtaq", "given": "Ameeq", "initials": "A"}, {"family": "\u00c5d\u00e9n", "given": "J\u00f6rgen", "initials": "J", "orcid": "0000-0002-4480-1219", "researcher": {"href": "https://publications.scilifelab.se/researcher/00206abad0de45eb90dc6bd3d5f3cf22.json"}}, {"family": "Sparrman", "given": "Tobias", "initials": "T", "orcid": "0000-0002-4442-6367", "researcher": {"href": "https://publications.scilifelab.se/researcher/f0d27dbd2f014795b1f7aa164d34bada.json"}}, {"family": "Hedenstr\u00f6m", "given": "Mattias", "initials": "M", "orcid": "0000-0002-0903-6662", "researcher": {"href": "https://publications.scilifelab.se/researcher/2db0f81a369741b0847c6f79746d82aa.json"}}, {"family": "Gr\u00f6bner", "given": "Gerhard", "initials": "G", "orcid": "0000-0001-7380-8797", "researcher": {"href": "https://publications.scilifelab.se/researcher/85bd86ebc85d4653bc880bc9be25bc80.json"}}], "type": "journal article", "published": "2021-03-08", "journal": {"title": "Molecules", "issn": "1420-3049", "issn-l": "1420-3049", "volume": "26", "issue": "5", "pages": "1467"}, "abstract": "Evasion from programmed cell death (apoptosis) is the main hallmark of cancer and a major cause of resistance to therapy. Many tumors simply ensure survival by over-expressing the cell-protecting (anti-apoptotic) Bcl-2 membrane protein involved in apoptotic regulation. However, the molecular mechanism by which Bcl-2 protein in its mitochondrial outer membrane location protects cells remains elusive due to the absence of structural insight; and current strategies to therapeutically interfere with these Bcl-2 sensitive cancers are limited. Here, we present an NMR-based approach to enable structural insight into Bcl-2 function; an approach also ideal as a fragment-based drug discovery platform for further identification and development of promising molecular Bcl-2 inhibitors. By using solution NMR spectroscopy on fully functional intact human Bcl-2 protein in a membrane-mimicking micellar environment, and constructs with specific functions remaining, we present a strategy for structure determination and specific drug screening of functional subunits of the Bcl-2 protein as targets. Using 19F NMR and a specific fragment library (Bionet) with fluorinated compounds we can successfully identify various binders and validate our strategy in the hunt for novel Bcl-2 selective cancer drug strategies to treat currently incurable Bcl-2 sensitive tumors.", "doi": "10.3390/molecules26051467", "pmid": "33800399", "labels": {"Swedish NMR Centre": "Service", "Chemical Biology Consortium Sweden": "Service"}, "xrefs": [{"db": "pii", "key": "molecules26051467"}, {"db": "pmc", "key": "PMC7962812"}], "notes": [], "created": "2021-07-02T14:04:43.748Z", "modified": "2025-10-17T13:04:28.135Z"}