POTENT, SELECTIVE INHIBITORS OF PROTEIN TYROSINE PHOSPHATASE 1B USING A SECOND PHOSPHOTYROSINE BINDING SITE, complexed with compound 19.

2-[(4-{2-ACETYLAMINO-2-[4-(1-CARBOXY-3-METHYLSULFANYL-PROPYLCARBAMOYL)-BUTYLCARBAMOYL]-ETHYL}-2-ETHYL-PHENYL)-OXALYL-AM INO]-BENZOIC ACID

Potent, Selective Inhibitors of Protein Tyrosine Phosphatase 1B

Protein-tyrosine phosphatase, non-receptor type 1

MEMEKEFEQIDKSGSWAAIYQDIRHEASDFPCRVAKLPKNKNRNRYRDVSPFDHSRIKLHQEDNDYINASLIKMEEAQRS
YILTQGPLPNTCGHFWEMVWEQKSRGVVMLNRVMEKGSLKCAQYWPQKEEKEMIFEDTNLKLTLISEDIKSYYTVRQLEL
ENLTTQETREILHFHYTTWPDFGVPESPASFLNFLFKVRESGSLSPEHGPVVVHCSAGIGRSGTFCLADTCLLLMDKRKD
PSSVDIKKVLLEMRKFRMGLIQTADQLRFSYLAVIEGAKFIMGDSSVQDQWKELSHEDLEPPPEHIPPPPRPPKRILEPH
N

Precipation buffer 100 mM Hepes, 0.2 M Magnesium Acetate, 14% PEG8000, pH 7.10, VAPOR DIFFUSION, HANGING DROP, temperature 277K

Potent, Selective Protein Tyrosine Phosphatase inhibitors using a Linked-Fragment Strategy

Potent, Selective Protein Tyrosine Phosphatase inhibitors using a Linked-Fragment Strategye

Potent, Selective Inhibitors of Protein Tyrosine Phosphatase 1B, complexed with compound

PDB ENTRY 1TYR AND INITIAL INTERNAL REFINEMENT

Residue CYS215, listed in remark 500, corresponds to the active site CYS which is known to be in a strained conformation in this class of enzymes.

PROTEIN TYROSINE PHOSPHATASE FOLD, OXAMIC ACID INHIBITOR BOUND TO P-LOOP, HYDROLASE