Solution forms of antitumor cyclic pentapeptides with 3,4-dichlorinated proline residues, astins A and C, from Aster tataricus.
Conformational analysis of antitumor cyclic pentapeptides, astins A (1) and C (3), was made by a combination of NMR and computational techniques. These results indicated that the backbone conformations of 1 and 3, with lower activity than astin B (2), were different from that of 2. The backbone conformation together with a cis 3,4-dichlorinated proline residue was considered to play an important role in the antitumor activities of astins.
Morita
H
H
Department of Pharmacognosy, School of Pharmacy, Tokyo University of Pharmacy and Life Science, Japan.
Nagashima
S
S
Takeya
K
K
Itokawa
H
H
D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008956:Models, Chemical; D010456:Peptides, Cyclic / Q000737:chemistry / Q000302:isolation & purification* / Q000494:pharmacology; D018517:Plant Roots / Q000737:chemistry; D011487:Protein Conformation; D012996:Solutions; D013329:Structure-Activity Relationship
D000972:Antineoplastic Agents, Phytogenic; D010456:Peptides, Cyclic; D012996:Solutions; C082413:astin A; C096028:astin C