Processing and gating defects can be targeted by small molecules called generically correctors and potentiators, respectively.
"Even if it isn't," he adds, "it could still be targeted by small molecules or other drugs".
This chapter discusses how various cellular processes regulating the oncogenesis can be targeted by small molecule inhibitors.
Recent structural and functional studies of the HIV-1 surface envelope glycoprotein gp120 have revealed sites of vulnerability that can be targeted by small molecule and peptide inhibitors, thereby inhibiting HIV-1 infection.
Naturally, 18F would not be the best choice for all targeting agents, but there are several receptors for peptides, such as integrins, somatostatin, bombesin/gastrin-releasing peptide, etc., that could be targeted by small peptides, where a radionuclide with a 2-h half-life, such as 18F, would be ideal [2].
The fact that some receptors are overexpressed in several tumor types and can be targeted by small peptides, proteins or antibodies conjugated to radionuclides has been used in the past for the development of peptide endoradiotherapeutic agents such as 90Y-DOTATOC or radioimmunotherapy of lymphomas with Zevalin.
Post-transcriptional gene silencing (PTGS) involves degradation of mRNAs targeted by small interfering RNAs (siRNAs) [18], [19].
These genes have minimal functional annotation with scores below 3.5 and represent over 75% of genes neither protected by patents nor targeted by small molecule drugs.
3'UTRs are recognized and targeted by small non-coding miRNAs that inhibit translation, promote transcript degradation, and often act as tissue-specific regulators of transcript stability [45].
From the KChannelDB (http://www.receptors.org/KCN/), we extracted 111 KIC genes, 14 of which were targeted by small molecule drugs according to DrugBank.
However, analyzing GPCRs not targeted by small molecule drugs revealed that the majority had remained weakly characterized with GCI scores for over 60% of genes ranging from 1.5 to 5.4 highlighting opportunity for further study and development of new targets within this highly relevant gene family.
