Discovery and SAR of a novel selective and orally bioavailable nonpeptide classical competitive inhibitor class of protein-tyrosine phosphatase 1B

HS Andersen, OH Olsen, LF Iversen… - Journal of Medicinal …, 2002 - ACS Publications
Reversible phosphorylation and dephosphorylation of key proteins on tyrosine residues are
important parts of intracellular signaling triggered by hormones and other agents. Recent …

Structure-based design of selective and potent inhibitors of protein-tyrosine phosphatase β

IK Lund, HS Andersen, LF Iversen, OH Olsen… - Journal of Biological …, 2004 - ASBMB
Protein-tyrosine phosphatases (PTPs) are considered important therapeutic targets because
of their pivotal role as regulators of signal transduction and thus their implication in several …

Synthesis and biological activity of a novel class of small molecular weight peptidomimetic competitive inhibitors of protein tyrosine phosphatase 1B

SD Larsen, T Barf, C Liljebris, PD May… - Journal of medicinal …, 2002 - ACS Publications
Protein tyrosine phosphatase 1B (PTP1B) negatively regulates insulin signaling in part by
dephosphorylating key tyrosine residues within the regulatory domain of the β-subunit of the …

Recent development of small molecular specific inhibitor of protein tyrosine phosphatase 1B

S Lee, Q Wang - Medicinal research reviews, 2007 - Wiley Online Library
Protein tyrosine phosphatases (PTPs), a large family of signaling enzymes, play essential
roles in intracellular signal transduction by regulating the cellular level of tyrosine …

Recent discovery and development of protein tyrosine phosphatase inhibitors

HO Kim, MA Blaskovich - Expert Opinion on Therapeutic Patents, 2002 - Taylor & Francis
The protein tyrosine phosphatases (PTPases or PTPs) play an important role in controlling
the status of tyrosine phosphorylation and the regulation of cellular function. The ability to …

Investigation of potential bioisosteric replacements for the carboxyl groups of peptidomimetic inhibitors of protein tyrosine phosphatase 1B: identification of a tetrazole …

C Liljebris, SD Larsen, D Ogg, BJ Palazuk… - Journal of medicinal …, 2002 - ACS Publications
Protein tyrosine phosphatases (PTPs) constitute a diverse family of enzymes that, together
with protein tyrosine kinases, control the level of intracellular tyrosine phosphorylation, thus …

Structure-based design of a low molecular weight, nonphosphorus, nonpeptide, and highly selective inhibitor of protein-tyrosine phosphatase 1B

LF Iversen, HS Andersen, S Branner… - Journal of Biological …, 2000 - ASBMB
Several protein-tyrosine phosphatases (PTPs) have been proposed to act as negative
regulators of insulin signaling. Recent studies have shown increased insulin sensitivity and …

Discovery of a potent, selective protein tyrosine phosphatase 1B inhibitor using a linked-fragment strategy

BG Szczepankiewicz, G Liu, PJ Hajduk… - Journal of the …, 2003 - ACS Publications
Protein tyrosine phosphatase 1B (PTP1B) is an enzyme that downregulates the insulin
receptor. Inhibition of PTP1B is expected to improve insulin action, and the design of small …

Recent advances in the development of allosteric protein tyrosine phosphatase inhibitors for drug discovery

RM Elhassan, X Hou, H Fang - Medicinal research reviews, 2022 - Wiley Online Library
Protein tyrosine phosphatases (PTPs) superfamily catalyzes tyrosine de‐phosphorylation
which affects a myriad of cellular processes. Imbalance in signal pathways mediated by …

Targeting tyrosine phosphatases: time to end the stigma

SM Stanford, N Bottini - Trends in Pharmacological Sciences, 2017 - cell.com
Protein tyrosine phosphatases (PTPs) are a family of enzymes essential for numerous
cellular processes, and several PTPs have been validated as therapeutic targets for human …