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TitleA covalent PFKL activator suppresses tumor growth.
Journal, issue, pagesNat Chem Biol, Year 2026
Publish dateAug 5, 2026
AuthorsXiaoding Jiang / Eric M Lynch / Congcong Lyu / Crystal N Wilson / Lauren E Salay / Hayden T Hess / Scott N Lyons / Mu-Jie Lu / Shuangyu Luo / Gibae Kim / Hsin-Ru Chan / Wesley J Wolfe / Lauren G Zacharias / Thomas P Mathews / Yi-Chih Lin / Bradley A Webb / Justin M Kollman / Xiaolu A Cambronne / Ku-Lung Hsu /
PubMed AbstractGlycolysis fuels vital cellular functions, and its dysregulation has been implicated in cancer, neurodegeneration, antibiotic resistance and diabetes. The glycolytic dependency of cancer, known as ...Glycolysis fuels vital cellular functions, and its dysregulation has been implicated in cancer, neurodegeneration, antibiotic resistance and diabetes. The glycolytic dependency of cancer, known as the Warburg effect, represents a key vulnerability for development of targeted anticancer agents; however, the development of such agents remains challenging owing to metabolic heterogeneity and resistance. Here we developed a covalent phosphofructokinase-1 liver type (PFKL) activator that couples glycolytic activation with delivery of a cytotoxic carnitine palmitoyltransferase 2 (CPT2)-targeting payload to cancer cells in vitro and in vivo. The electrophile-drug conjugate site-specifically and proteome-wide selectively modifies K677 in the allosteric effector site to stabilize the R-state tetramer of PFKL, while concomitantly releasing a CPT2-selective inhibitor to destabilize cell metabolism. The delivery mechanism of electrophile-drug conjugates is analogous to that of antibody-drug conjugates, but differentiated by their selective covalent targeting of intracellular proteins.
External linksNat Chem Biol / PubMed:42557312
MethodsEM (single particle)
Resolution3.2 Å
Structure data

71076

9p0j

EMDB-71076, PDB-9p0j:
Human liver phosphofructokinase-1 bound to XJ-4-85
Method: EM (single particle) / Resolution: 3.2 Å

Chemicals

PDB-1c4x:
2-HYDROXY-6-OXO-6-PHENYLHEXA-2,4-DIENOATE HYDROLASE (BPHD) FROM RHODOCOCCUS SP. STRAIN RHA1

ChemComp-FBP:
1,6-di-O-phosphono-beta-D-fructofuranose

ChemComp-ADP:
ADENOSINE-5'-DIPHOSPHATE / ADP, energy-carrying molecule*YM

ChemComp-F6P:
6-O-phosphono-beta-D-fructofuranose

PDB-1cfq:
ANTI-P24 (HIV-1) FAB FRAGMENT CB41

Source
  • homo sapiens (human)
KeywordsTRANSFERASE / phosphofructokinase-1 / liver / PFKL / activator

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