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Literature summary extracted from

  • Christensen, E.M.; Bogner, A.N.; Vandekeere, A.; Tam, G.S.; Patel, S.M.; Becker, D.F.; Fendt, S.M.; Tanner, J.J.
    In crystallo screening for proline analog inhibitors of the proline cycle enzyme PYCR1 (2020), J. Biol. Chem., 295, 18316-18327 .
    View publication on PubMed

Crystallization (Commentary)

EC Number Crystallization (Comment) Organism
1.5.1.2 PYCR1 complexed with N-formyl-L-proline, inhibitor binding is accompanied by conformational changes in the active site, including the translation of an alpha-helix by 1 A Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.5.1.2 cyclopentanecarboxylate
-
 Homo sapiens
1.5.1.2 L-proline
-
 Homo sapiens
1.5.1.2 L-tetrahydro-2-furoic acid
-
 Homo sapiens
1.5.1.2 L-thiazolidine-2-carboxylate
-
 Homo sapiens
1.5.1.2 L-thiazolidine-4-carboxylate
-
 Homo sapiens
1.5.1.2 N-formyl-L-proline competitive. Compound phenocopies the PYCR1 knockdown in MCF10A H-RASV12 breast cancer cells by inhibiting de novo proline biosynthesis and impairing spheroidal growth Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.5.1.2 Homo sapiens P32322
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.5.1.2 1-pyrroline-5-carboxylate + NADH + H+
-
 Homo sapiens L-proline + NAD+
-
 ?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.5.1.2 0.1
-
 pH 7.8, temperature not specified in the publication Homo sapiens N-formyl-L-proline
1.5.1.2 0.44
-
 pH 7.8, temperature not specified in the publication Homo sapiens L-thiazolidine-2-carboxylate
1.5.1.2 0.6
-
 pH 7.8, temperature not specified in the publication Homo sapiens L-thiazolidine-4-carboxylate
1.5.1.2 1.19
-
 pH 7.8, temperature not specified in the publication Homo sapiens cyclopentanecarboxylate
1.5.1.2 1.72
-
 pH 7.8, temperature not specified in the publication Homo sapiens L-proline
1.5.1.2 2.25
-
 pH 7.8, temperature not specified in the publication Homo sapiens L-tetrahydro-2-furoic acid