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Folate‐maytansinoids: Target‐selective drugs of low molecular weight
Author(s) -
Ladino Cynthia A.,
Chari Ravi V.J.,
Bourret Lizabeth A.,
Kedersha Nancy L.,
Goldmacher Victor S.
Publication year - 1997
Publication title -
international journal of cancer
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.475
H-Index - 234
eISSN - 1097-0215
pISSN - 0020-7136
DOI - 10.1002/(sici)1097-0215(19971210)73:6<859::aid-ijc16>3.0.co;2-#
Subject(s) - folate receptor , cytotoxic t cell , receptor , cytotoxicity , cancer research , cell culture , chemistry , drug , biology , in vitro , pharmacology , biochemistry , cancer , cancer cell , genetics
Abstract Folate receptor is over‐expressed in a variety of carcinomas. To design a cytotoxic drug that would selectively target these carcinomas, we synthesized folate‐maytansinoids. These drugs showed high affinity toward folate receptor, appeared to enter cells exclusively via the folate receptor–mediated caveolar pathway and displayed high cytotoxic potency (in the range of 10 −11 to 10 −10 M) and remarkable selectivity for folate receptor–expressing carcinoma cell lines. Folate‐maytansinoids represent a new class of tumor‐specific agents in which the targeting and the cytotoxic function can be altered independently. Int. J. Cancer 73:859–864, 1997. © 1997 Wiley‐Liss, Inc.