Search engine for discovering works of Art, research articles, and books related to Art and Culture
Javascript must be enabled to continue!
Protein-Protein Interaction Inhibitors Targeting the Eph-Ephrin System with a Focus on Amino Acid Conjugates of Bile Acids
View through CrossRef
The role of the Eph-ephrin system in the etiology of pathological conditions has been consolidated throughout the years. In this context, approaches directed against this signaling system, intended to modulate its activity, can be strategic therapeutic opportunities. Currently, the most promising class of compounds able to interfere with the Eph receptor-ephrin protein interaction is composed of synthetic derivatives of bile acids. In the present review, we summarize the progresses achieved, in terms of chemical expansions and structure-activity relationships, both in the steroidal core and the terminal carboxylic acid group, along with the pharmacological characterization for the most promising Eph-ephrin antagonists in in vivo settings.
Title: Protein-Protein Interaction Inhibitors Targeting the Eph-Ephrin System with a Focus on Amino Acid Conjugates of Bile Acids
Description:
The role of the Eph-ephrin system in the etiology of pathological conditions has been consolidated throughout the years.
In this context, approaches directed against this signaling system, intended to modulate its activity, can be strategic therapeutic opportunities.
Currently, the most promising class of compounds able to interfere with the Eph receptor-ephrin protein interaction is composed of synthetic derivatives of bile acids.
In the present review, we summarize the progresses achieved, in terms of chemical expansions and structure-activity relationships, both in the steroidal core and the terminal carboxylic acid group, along with the pharmacological characterization for the most promising Eph-ephrin antagonists in in vivo settings.
Related Results
Predictive value of random sample urine bile acids corrected by creatinine in liver disease
Predictive value of random sample urine bile acids corrected by creatinine in liver disease
Bile acids, in a random sample of urine, discriminated normal controls from liver disease, with a probability similar to fasting plasma bile acids (p < 0.01 and p < 0.001, de...
Metabolic Soft Spot and Pharmacokinetics: Functionalization of C-3 Position of an Eph–Ephrin Antagonist Featuring a Bile Acid Core as an Effective Strategy to Obtain Oral Bioavailability in Mice
Metabolic Soft Spot and Pharmacokinetics: Functionalization of C-3 Position of an Eph–Ephrin Antagonist Featuring a Bile Acid Core as an Effective Strategy to Obtain Oral Bioavailability in Mice
UniPR129, an L-β-homotryptophan conjugate of the secondary bile acid lithocholic acid (LCA), acts as an effective protein-protein interaction (PPI) inhibitor of the Eph–ephrin syst...
The Mutant Eisai Hyperbilirubinemic Rat Is Resistant to Bile Acid-Induced Cholestasis and Cytotoxicity
The Mutant Eisai Hyperbilirubinemic Rat Is Resistant to Bile Acid-Induced Cholestasis and Cytotoxicity
We investigated bile flow and biliary excretion of bile acids in the Eisai hyperbilirubinemic rat, a Sprague–Dawley mutant rat with conjugated hyperbilirubinemia, using both
...
BILE SALT METABOLISM AS INFLUENCED BY PURE AMINO ACIDS AND CASEIN DIGESTS
BILE SALT METABOLISM AS INFLUENCED BY PURE AMINO ACIDS AND CASEIN DIGESTS
A non-protein diet supplemented with vitamins fed to a bile fistula dog caused marked reduction in cholic acid and taurocholic acid formation.
A mixture of pure amin...
SYNTHESIS OF AMINO ACIDS FROM SUBSTITUTED CYANOACETIC ESTERS
SYNTHESIS OF AMINO ACIDS FROM SUBSTITUTED CYANOACETIC ESTERS
Nine α-amino acids, namely, dl-α-aminoundecylic acid, dl-α-aminostearic acid, dl-α-amino-β-methylcaproic acid, dl-α-amino-β-ethylvaleric acid, dl-α-amino-β-methylenanthic acid, dl-...
AcrB is essential for bile acid tolerance in Helicobacter pylori
AcrB is essential for bile acid tolerance in Helicobacter pylori
Resistance to bile acids is a necessary ability for bacteria that live in the gastrointestinal tract, such as Helicobacter pylori. The role of the bacterial drug efflux system is i...
Therapeutic potential of SGLT-2 inhibitors and DDP4 inhibitors in elderly patients with type 2 diabetes mellitus and benign prostatic hyperplasia
Therapeutic potential of SGLT-2 inhibitors and DDP4 inhibitors in elderly patients with type 2 diabetes mellitus and benign prostatic hyperplasia
Background. Benign prostatic hyperplasia (BPH) has recently been linked to diabetes mellitus and insulin resistance. This study aims to explore whether the use of either sodium-glu...