-transparent.png){kind=logo}
Bombesin (BN)-like peptides (such as GRP, gastrin-releasing peptide) are autocrine growth factors for small cell lung carcinoma (SCLC). BN receptor antagonists can therefore find clinical application in the treatment of this highly malignant disease. The present paper deals with a new class of bombesin analogues carrying a nitrogen mustard at their N-terminus. Due to the irreversible binding to the BN receptor(s), these peptides eventually block the mitogenic effects of the natural ligand(s), regardless of their intrinsic "agonistic" or "antagonistic" structures. In Swiss 3T3 fibroblasts they inhibit [125I]GRP binding in the nanomolar/micromolar range. According to their "agonistic" or "antagonistic" structural features, they do or do not induce [3H]thymidine incorporation and p 115 phosphorylation. In competition experiments, alkylating "antagonists" selectively inhibit BN-induced thymidine incorporation either when given simultaneously with or 24 hours before the BN challenge. Alkylating "agonists" display antagonistic effects only in the sequential treatment.
R de Castiglione, and
L Gozzini, and
M Galantino, and
F Corradi, and
E Arlandini, and
I Molinari, and
M Ciomei
March 1987,
The American journal of physiology,
R de Castiglione, and
L Gozzini, and
M Galantino, and
F Corradi, and
E Arlandini, and
I Molinari, and
M Ciomei
January 1988,
Synapse (New York, N.Y.),
R de Castiglione, and
L Gozzini, and
M Galantino, and
F Corradi, and
E Arlandini, and
I Molinari, and
M Ciomei
January 1991,
Peptides,
R de Castiglione, and
L Gozzini, and
M Galantino, and
F Corradi, and
E Arlandini, and
I Molinari, and
M Ciomei
September 1987,
Journal of medicinal chemistry,
R de Castiglione, and
L Gozzini, and
M Galantino, and
F Corradi, and
E Arlandini, and
I Molinari, and
M Ciomei
September 1990,
The Journal of biological chemistry,
R de Castiglione, and
L Gozzini, and
M Galantino, and
F Corradi, and
E Arlandini, and
I Molinari, and
M Ciomei
September 1990,
The American journal of physiology,
R de Castiglione, and
L Gozzini, and
M Galantino, and
F Corradi, and
E Arlandini, and
I Molinari, and
M Ciomei
January 1986,
NIDA research monograph,
R de Castiglione, and
L Gozzini, and
M Galantino, and
F Corradi, and
E Arlandini, and
I Molinari, and
M Ciomei
April 1993,
European journal of pharmacology,
R de Castiglione, and
L Gozzini, and
M Galantino, and
F Corradi, and
E Arlandini, and
I Molinari, and
M Ciomei
January 1988,
Peptides,
R de Castiglione, and
L Gozzini, and
M Galantino, and
F Corradi, and
E Arlandini, and
I Molinari, and
M Ciomei
April 1976,
Life sciences,
