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Small molecule-drug conjugates: A novel strategy for cancer-targeted treatment.

Abstract：

:Targeted therapy has become an effective strategy of precision medicine for improving cancer treatment. Selectivity improvement is always popular in modern oncology because of decreased side effects in conventional cancer chemotherapy. The use of antibody-drug conjugates (ADC), a robust strategy for targeted therapy, applies antibodies to selectively deliver a potent cytotoxic compound to tumor cells and thus improve the therapeutic efficacy of the chemotherapeutic agents. Three ADC products (trastuzumab emtansine, brentuximab vedotin and inotuzumab ozogamicin) are already on the market, and several compounds are in clinical trials. Compared with ADCs, small molecule-drug conjugates (SMDCs) provide a new, less established perspective for targeted delivery. Nevertheless, SMDCs have several strengths: they have 1) a non-immunogenic nature, 2) much more manageable synthesis, 3) lower molecular weights, which confer a high potential for good cell penetration in solid tumors. SMDCs might therefore be a promising alternative with similar efficacy to ADCs. In this article, we highlight the medicinal chemistry aspects of SMDC design. SMDC targeting ligands, linkers and small-molecule payloads will be discussed. Successful cases of SMDCs used as therapeutic agents and other applications of SMDC will also be included.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Zhuang C,Guan X,Ma H,Cong H,Zhang W,Miao Z

doi

10.1016/j.ejmech.2018.12.035

subject

Has Abstract

pub_date

2019-02-01 00:00:00

pages

883-895

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(18)31072-9

journal_volume

163

pub_type

杂志文章,评审

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