Recent advances in stereoselective C-glycoside synthesis
Y Du, RJ Linhardt, IR Vlahov - Tetrahedron, 1998 - Elsevier
9914 9915 9915 9917 9918 9919 9920 9922 9923 9923 9924 9924 9925 9925 9926 9927
9928 9928 9928 9932 9932 9932 9934 9934 9936 9937 9937 9938 9938 9938 9939 9941 …
9928 9928 9928 9932 9932 9932 9934 9934 9936 9937 9937 9938 9938 9938 9939 9941 …
Evaluation of disulfide reduction during receptor-mediated endocytosis by using FRET imaging
Despite functional evidence for disulfide bond-reducing activity in endosomal compartments,
the mechanistic details pertaining to such process (eg, kinetics and sites of disulfide …
the mechanistic details pertaining to such process (eg, kinetics and sites of disulfide …
Synthesis and Biological Evaluation of EC20: A New Folate-Derived, 99mTc-Based Radiopharmaceutical
A new peptide derivative of folic acid was designed to efficiently coordinate 99m Tc. This new
chelate, referred to as EC20, was found to bind cultured folate receptor (FR)-positive tumor …
chelate, referred to as EC20, was found to bind cultured folate receptor (FR)-positive tumor …
Engineering folate–drug conjugates to target cancer: from chemistry to clinic
IR Vlahov, CP Leamon - Bioconjugate chemistry, 2012 - ACS Publications
The folate receptor (FR) is a potentially useful biological target for the management of many
human cancers. This membrane protein binds extracellular folates with very high affinity and…
human cancers. This membrane protein binds extracellular folates with very high affinity and…
Preclinical Evaluation of EC145, a Folate-Vinca Alkaloid Conjugate
…, T Smith, LC Xu, M Vetzel, P Kleindl, IR Vlahov… - Cancer research, 2007 - AACR
We recently developed a new group of folate-conjugated Vinca alkaloids, one of which, EC145,
emerged as a candidate for clinical development. Brief treatment of nude mice bearing ∼…
emerged as a candidate for clinical development. Brief treatment of nude mice bearing ∼…
Design and regioselective synthesis of a new generation of targeted chemotherapeutics. Part 1: EC145, a folic acid conjugate of desacetylvinblastine monohydrazide
IR Vlahov, HKR Santhapuram, PJ Kleindl… - Bioorganic & medicinal …, 2006 - Elsevier
An efficient synthesis of the folate receptor (FR) targeting conjugate EC145 is described.
EC145 is a water soluble derivative of the vitamin folic acid and the potent cytotoxic agent, …
EC145 is a water soluble derivative of the vitamin folic acid and the potent cytotoxic agent, …
Characterization of the pH of folate receptor-containing endosomes and the rate of hydrolysis of internalized acid-labile folate-drug conjugates
Despite the widely accepted assumption that most endosomal compartments are acidic,
evaluation of the efficiency of pH-dependent drug release from a ligand-targeted drug conjugate …
evaluation of the efficiency of pH-dependent drug release from a ligand-targeted drug conjugate …
Folate-conjugated rapamycin slows progression of polycystic kidney disease
JM Shillingford, CP Leamon, IR Vlahov… - Journal of the …, 2012 - journals.lww.com
Activation of the mammalian target of rapamycin (mTOR) signaling pathway is aberrant in
autosomal-dominant polycystic kidney disease (ADPKD). The mTOR inhibitors, such as …
autosomal-dominant polycystic kidney disease (ADPKD). The mTOR inhibitors, such as …
Preclinical antitumor activity of a novel folate-targeted dual drug conjugate
We have designed a new type of tumor-targeted agent by tethering two different drug
molecules, with distinct biological mechanisms of action, to the same ligand. This compound, …
molecules, with distinct biological mechanisms of action, to the same ligand. This compound, …
Synthesis and biological evaluation of EC72: a new folate-targeted chemotherapeutic
A novel folate conjugate of mitomycin C, herein referred to as EC72, was designed and
evaluated for biological activity against FR-positive cells and tumors. EC72 was produced by …
evaluated for biological activity against FR-positive cells and tumors. EC72 was produced by …