Table 1

GRP-R mRNA nucleotide and amino acid mutations identified in human colon cancer cell lines with binding inhibition constants as determined against natively expressed receptors

Cell LineMutationsKi
NucleotideAmino AcidLocationOther Lines?
nM
CaCo-2  C455TSilentNH2 1.5  ± 0.3
•C851TSilentIC-2DLD-1
HT-29
•C1061TSilentTM-5DLD-1
HT-29
T-84
DLD-1 C504AH36NNH2 N.B.
T539CSilentTM-1
A818GSilentIC-2
•C851TSilentIC-2CaCo-2
HT-29
A1023GI209VEC-3
•C1061TSilentTM-5CaCo-2
HT-29
T-84
•T1348AV317ETM-7
H-498 A498GN31DNH2 N.B.
A513GV40ITM-1
Insertion1-a Stop CodonIC-2
H-716 T854CH152QIC-22.3  ± 0.7
A1005GN203SEC-2
HT-29 C695TSilentEC-21.9  ± 0.4
•C851TSilentIC-2CaCo-2
DLD-1
•C1061TSilentTM-5CaCo-2
DLD-1
LoVo-E2•C926TSilentTM-4SW-4801.5  ± 0.2
•T930CF178LEC-2SW-480
T1057CV220ATM-5
SNU/C5•C831AP145YIC-2T-84N.B.
C881ASilentTM-4
SW-480 A496TD33VNH2 2.0  ± 0.3
•C926TSilentTM-4LoVo-E2
•T930CF178LEC-2LoVo-E2
T-84•C831AP145YIC-2SNU/C5N.B.
T862CM155YTM-4
•C1061TSilentTM-5CaCo-2
DLD-1
HT-29
T1068CS224YTM-5
T1108CSilentIC-3

Nucleotides and amino acids in single-letter code. Nucleotide numbering is from the site of translation initiation, whereas that for amino acid numbering is from the site of translation initiation (i.e., ATG = +1). Entries preceded by a bullet point identify mutations seen in more than one cell line. Binding data is for a minimum of three separate transfections as described under Experimental Procedures, with data presented as means ± S.E.

    • N.B., no specific binding to the cell line observed.

    • ↵1-a  Insertion of a 32-nucleotide segment resulting in a frameshift and ultimately a stop codon.