Prodrugs: a challenge for the drug development

JB Zawilska, J Wojcieszak, AB Olejniczak - Pharmacological reports, 2013 - Springer
It is estimated that about 10% of the drugs approved worldwide can be classified as
prodrugs. Prodrugs, which have no or poor biological activity, are chemically modified …

Transporter-mediated drug delivery

G Gyimesi, MA Hediger - Molecules, 2023 - mdpi.com
Transmembrane transport of small organic and inorganic molecules is one of the
cornerstones of cellular metabolism. Among transmembrane transporters, solute carrier …

Application of ProTide technology to gemcitabine: a successful approach to overcome the key cancer resistance mechanisms leads to a new agent (NUC-1031) in …

M Slusarczyk, MH Lopez, J Balzarini… - Journal of medicinal …, 2014 - ACS Publications
Gemcitabine is a nucleoside analogue commonly used in cancer therapy but with limited
efficacy due to a high susceptibility to cancer cell resistance. The addition of a …

Pharmaceutical and pharmacological importance of peptide transporters

M Brandsch, I Knütter… - Journal of Pharmacy …, 2008 - Wiley Online Library
Peptide transport is currently a prominent topic in membrane research. The transport
proteins involved are under intense investigation because of their physiological importance …

Amino acids as promoieties in prodrug design and development

BS Vig, KM Huttunen, K Laine, J Rautio - Advanced Drug Delivery Reviews, 2013 - Elsevier
Prodrugs are biologically inactive agents that upon biotransformation in vivo result in active
drug molecules. Since prodrugs might alter the tissue distribution, efficacy and the toxicity of …

Prodrugs of nucleoside analogues for improved oral absorption and tissue targeting

F Li, H Maag, T Alfredson - Journal of pharmaceutical sciences, 2008 - Elsevier
Nucleoside analogues are widely used for the treatment of antiviral infections and
anticancer chemotherapy. However, many nucleoside analogues suffer from poor oral …

Amino acids in the development of prodrugs

N Vale, A Ferreira, J Matos, P Fresco, MJ Gouveia - Molecules, 2018 - mdpi.com
Although drugs currently used for the various types of diseases (eg, antiparasitic, antiviral,
antibacterial, etc.) are effective, they present several undesirable pharmacological and …

[HTML][HTML] Recent advances in understanding proton coupled peptide transport via the POT family

S Newstead - Current opinion in structural biology, 2017 - Elsevier
Highlights•Recent crystal structures reveal insights into ligand promiscuity within the POT
family.•Selectivity pockets play important roles in peptide recognition and …

The role and pathophysiological relevance of membrane transporter PepT1 in intestinal inflammation and inflammatory bowel disease

SA Ingersoll, S Ayyadurai… - American Journal …, 2012 - journals.physiology.org
Intestinal inflammation is characterized by epithelial disruption, leading to loss of barrier
function and the recruitment of immune cells, including neutrophils. Although the …

Human PEPT1 pharmacophore distinguishes between dipeptide transport and binding

BS Vig, TR Stouch, JK Timoszyk, Y Quan… - Journal of Medicinal …, 2006 - ACS Publications
The human intestinal oligopeptide transporter (PEPT1) facilitates the absorption of
dipeptides, tripeptides, and many peptidomimetic drugs. In this study, a large number of …