title: Establishing the principle of reversibility in peptide/protein and small-molecule therapy.
abstract: Several important pharmacological features can be integrated into injected drugs to enhance their therapeutic efficacy following administration. Short-lived peptide/protein drugs should be converted into long-lived species in vivo to avoid multiple injections. Circulating levels of anticancer agents need to be maintained within a narrow therapeutic range for prolonged period. Water-insoluble drugs must be turned into soluble species and blood-brain barrier-impermeable agents need to be modified to cross it following peripheral administrations. The derivatization requiring for achieving those desirable pharmacological features typically result in biologically/pharmacologically inactive products, unless those derivatizations can be carried out in a reversible fashion.
authors: Department of Biological Chemistry, Weizmann Institute of Science, Rehovot 76100, Israel. yoram.shechter@weizmann.ac.il
authors: Yoram
authors: Y
authors: Shechter
authors: Keren
authors: K
authors: Sasson
authors: Yonit
authors: Y
authors: Marcus
authors: Sara
authors: S
authors: Rubinraut
authors: Vered
authors: V
authors: Lev-Goldman
authors: Mati
authors: M
authors: Fridkin
mesh_terms: D000595:Amino Acid Sequence; D006801:Humans; D008969:Molecular Sequence Data; D010455:Peptides / Q000008:administration & dosage* / Q000737:chemistry; D011506:Proteins / Q000008:administration & dosage* / Q000737:chemistry
chemical_list: D010455:Peptides; D011506:Proteins