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 …

Genetic and cellular contributions to liver regeneration

R Liang, YH Lin, H Zhu - Cold Spring Harbor …, 2022 - cshperspectives.cshlp.org
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 …

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 …

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 …

Molecular Bidents with Two Electrophilic Warheads as a New Pharmacological Modality

Z Li, J Jiang, SB Ficarro, TS Beyett, C To… - ACS Central …, 2024 - ACS Publications
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 …

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 …

Repurposing of FDA approved kinase inhibitor bosutinib for mitigation of radiation induced damage via inhibition of JNK pathway

B Singh, RS Patwardhan, D Pal, DK Maurya… - Toxicology and Applied …, 2024 - Elsevier
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 …

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 …

Chemical proteomic identification of functional cysteines with atypical electrophile reactivities

K Litwin, VM Crowley, RM Suciu, DL Boger… - Tetrahedron letters, 2021 - Elsevier
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 …

Rational Design of Highly Potent and Selective Covalent MAP2K7 Inhibitors

DR Kim, MJ Orr, AJ Kwong, KK Deibler… - ACS Medicinal …, 2023 - ACS Publications
The mitogen-activated protein kinase signaling cascade is conserved across eukaryotes,
where it plays a critical role in the regulation of activities including proliferation …