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Table 1 Acquired and occurring mutations identified in NAMPT inhibitor resistant cell lines and parental line HCT-116.

From: Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase

 

Mutation

Change in protein sequence

Position

HCT-116

1025A>G

K342R

b-sheet 11

HCT-116/TP201565

1025A>G

K342R

b-sheet 11

 

1163A>G

Q388R

Dimer interface

 

572A>G

H191R

APO866 binding site

HCT-116/APO866

1025A>G

K342R

b-sheet 11

 

572A>G

H191R

APO866 binding site

NYH/CHS

278-280del

D93del

Dimer interface

NYH/APO866

278-280del

D93del

Dimer interface

  1. The structural position of the mutations has been determined from a published crystal structure of NAMPT [14]. All mutations are located in one allele only. In HCT-116/TP201565 the mutations K342R and Q388R are located on the same allele.