MKK4 Inhibitors—Recent Development Status and Therapeutic Potential
L Katzengruber, P Sander, S Laufer - International Journal of Molecular …, 2023 - mdpi.com
MKK4 (mitogen-activated protein kinase kinase 4; also referred to as MEK4) is a dual-
specificity protein kinase that phosphorylates and regulates both JNK (c-Jun N-terminal …
specificity protein kinase that phosphorylates and regulates both JNK (c-Jun N-terminal …
Genetic and cellular contributions to liver regeneration
The regenerative capabilities of the liver represent a paradigm for understanding tissue
repair in solid organs. Regeneration after partial hepatectomy in rodent models is well …
repair in solid organs. Regeneration after partial hepatectomy in rodent models is well …
Optimization of Covalent MKK7 Inhibitors via Crude Nanomole-Scale Libraries
P Gehrtz, S Marom, M Bührmann… - Journal of medicinal …, 2022 - ACS Publications
High-throughput nanomole-scale synthesis allows for late-stage functionalization (LSF) of
compounds in an efficient and economical manner. Here, we demonstrated that copper …
compounds in an efficient and economical manner. Here, we demonstrated that copper …
GZ17-6.02 kills prostate cancer cells in vitro and in vivo
L Booth, JL Roberts, C West, P Dent - Frontiers in Oncology, 2022 - frontiersin.org
GZ17-6.02 is undergoing clinical evaluation in solid tumors and lymphoma. We defined the
biology of GZ17-6.02 in prostate cancer cells and determined whether it interacted with the …
biology of GZ17-6.02 in prostate cancer cells and determined whether it interacted with the …
Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality
A systematic strategy to develop dual-warhead inhibitors is introduced to circumvent the
limitations of conventional covalent inhibitors such as vulnerability to mutations of the …
limitations of conventional covalent inhibitors such as vulnerability to mutations of the …
Covalent drugs based on small molecules and peptides for disease theranostics
YJ Zhang, JX Liang, YS Xu, YX Liu, Y Cui… - Biomaterials …, 2024 - pubs.rsc.org
Biomacromolecules, such as proteins, nucleic acids and polysaccharides, are widely
distributed in the human body, and some of them have been recognized as the targets of …
distributed in the human body, and some of them have been recognized as the targets of …
Repurposing of FDA approved kinase inhibitor bosutinib for mitigation of radiation induced damage via inhibition of JNK pathway
Radiotherapy is a common modality for cancer treatment. However, it is often associated
with normal tissue toxicity in 20–80% of the patients. Radioprotectors can improve the …
with normal tissue toxicity in 20–80% of the patients. Radioprotectors can improve the …
Rational design, optimization, and biological evaluation of novel MEK4 inhibitors against pancreatic adenocarcinoma
AJ Kwong, TND Pham, HE Oelschlager… - ACS Medicinal …, 2021 - ACS Publications
Growth, division, and development of healthy cells relies on efficient response to
environmental survival cues. The conserved mitogen-activated protein kinase (MAPK) family …
environmental survival cues. The conserved mitogen-activated protein kinase (MAPK) family …
Chemical proteomic identification of functional cysteines with atypical electrophile reactivities
Cysteine-directed covalent ligands have emerged as a versatile category of chemical
probes and drugs that leverage thiol nucleophilicity to form permanent adducts with proteins …
probes and drugs that leverage thiol nucleophilicity to form permanent adducts with proteins …
Rational Design of Highly Potent and Selective Covalent MAP2K7 Inhibitors
The mitogen-activated protein kinase signaling cascade is conserved across eukaryotes,
where it plays a critical role in the regulation of activities including proliferation …
where it plays a critical role in the regulation of activities including proliferation …