PTP1B as a drug target: recent developments in PTP1B inhibitor discovery
S Zhang, ZY Zhang - Drug discovery today, 2007 - Elsevier
Protein tyrosine phosphatase 1B (PTP1B) is an effective target for the treatment of both type
2 diabetes and obesity; however, targeting PTP1B for drug discovery is challenging because …
2 diabetes and obesity; however, targeting PTP1B for drug discovery is challenging because …
Recent updates on development of protein-tyrosine phosphatase 1B inhibitors for treatment of diabetes, obesity and related disorders
S Singh, AS Grewal, R Grover, N Sharma, B Chopra… - Bioorganic …, 2022 - Elsevier
The aim of this review was to discuss an overview of type 2 diabetes; biology of PTP1B; role
of PTP1B in metabolic disorders; and recent updates in the development of PTP1B inhibitors …
of PTP1B in metabolic disorders; and recent updates in the development of PTP1B inhibitors …
Recent advances in the discovery of competitive protein tyrosine phosphatase 1B inhibitors for the treatment of diabetes, obesity, and cancer
AP Combs - Journal of medicinal chemistry, 2010 - ACS Publications
Many eukaryote cellular functions are regulated by precise control of the phosphorylation
levels of proteins involved in a variety of signal transduction processes. Protein tyrosine …
levels of proteins involved in a variety of signal transduction processes. Protein tyrosine …
Tethering: fragment-based drug discovery
DA Erlanson, JA Wells… - Annu. Rev. Biophys …, 2004 - annualreviews.org
▪ Abstract The genomics revolution has provided a deluge of new targets for drug discovery.
To facilitate the drug discovery process, many researchers are turning to fragment-based …
To facilitate the drug discovery process, many researchers are turning to fragment-based …
The critical role of passive permeability in designing successful drugs
Passive permeability is a key property in drug disposition and delivery. It is critical for
gastrointestinal absorption, brain penetration, renal reabsorption, defining clearance …
gastrointestinal absorption, brain penetration, renal reabsorption, defining clearance …
An expanded allosteric network in PTP1B by multitemperature crystallography, fragment screening, and covalent tethering
Allostery is an inherent feature of proteins, but it remains challenging to reveal the
mechanisms by which allosteric signals propagate. A clearer understanding of this intrinsic …
mechanisms by which allosteric signals propagate. A clearer understanding of this intrinsic …
Inhibitors of protein tyrosine phosphatases: Next‐generation drugs?
L Bialy, H Waldmann - Angewandte Chemie International …, 2005 - Wiley Online Library
The protein tyrosine phosphatases (PTPs) constitute a family of closely related key
regulatory enzymes that dephosphorylate phosphotyrosine residues in their protein …
regulatory enzymes that dephosphorylate phosphotyrosine residues in their protein …
The two faces of PTP1B in cancer
L Lessard, M Stuible, ML Tremblay - … et Biophysica Acta (BBA)-Proteins and …, 2010 - Elsevier
PTP1B is a classical non-transmembrane protein tyrosine phosphatase that plays a key role
in metabolic signaling and is a promising drug target for type 2 diabetes and obesity …
in metabolic signaling and is a promising drug target for type 2 diabetes and obesity …
The Gewald multicomponent reaction
Y Huang, A Dömling - Molecular diversity, 2011 - Springer
The Gewald reaction of sulfur, cyanoacetic acid derivatives, and oxo-component (G-3CR)
yielding highly substituted 2-aminothiophene derivatives has seen diverse applications in …
yielding highly substituted 2-aminothiophene derivatives has seen diverse applications in …
Protein tyrosine phosphatases: structure, function, and implication in human disease
L Tautz, DA Critton, S Grotegut - Phosphatase Modulators, 2013 - Springer
Protein tyrosine phosphorylation is a key regulatory mechanism in eukaryotic cell
physiology. Aberrant expression or function of protein tyrosine kinases and protein tyrosine …
physiology. Aberrant expression or function of protein tyrosine kinases and protein tyrosine …