Recent advances in the development of protein–protein interactions modulators: mechanisms and clinical trials

H Lu, Q Zhou, J He, Z Jiang, C Peng, R Tong… - Signal transduction and …, 2020 - nature.com
Protein–protein interactions (PPIs) have pivotal roles in life processes. The studies showed
that aberrant PPIs are associated with various diseases, including cancer, infectious …

Targeting RAS membrane association: back to the future for anti-RAS drug discovery?

AD Cox, CJ Der, MR Philips - Clinical Cancer Research, 2015 - AACR
RAS proteins require membrane association for their biologic activity, making this
association a logical target for anti-RAS therapeutics. Lipid modification of RAS proteins by a …

Targeting KRAS in metastatic colorectal cancer: current strategies and emerging opportunities

M Porru, L Pompili, C Caruso, A Biroccio… - Journal of Experimental & …, 2018 - Springer
Developing drugs that target KRAS, the most frequently mutated oncogene in cancer, has
not been successful despite much concerted efforts dedicated towards it in the last thirty …

Therapeutic evolution of benzimidazole derivatives in the last quinquennial period

W Akhtar, MF Khan, G Verma… - European journal of …, 2017 - Elsevier
Benzimidazole, a fused heterocycle bearing benzene and imidazole has gained
considerable attention in the field of contemporary medicinal chemistry. The moiety is of …

State-of-the-art strategies for targeting protein–protein interactions by small-molecule inhibitors

C Sheng, G Dong, Z Miao, W Zhang… - Chemical Society …, 2015 - pubs.rsc.org
Targeting protein–protein interactions (PPIs) has emerged as a viable approach in modern
drug discovery. However, the identification of small molecules enabling us to effectively …

Metal–organic framework MIL-101 (Cr) as an efficient heterogeneous catalyst for clean synthesis of benzoazoles

E Niknam, F Panahi, F Daneshgar, F Bahrami… - ACS …, 2018 - ACS Publications
A metal–organic framework [MIL-101 (Cr)] was used as an efficient heterogeneous catalyst
in the synthesis of benzoazoles (benzimidazole, benzothiazole, and benzoxazole), and …

Progress in targeting RAS with small molecule drugs

F McCormick - Biochemical Journal, 2019 - portlandpress.com
RAS proteins have traditionally been deemed undruggable, as they do not possess an
active site to which small molecules could bind but small molecules that target one form of …

Posttranslational modifications of RAS proteins

I Ahearn, M Zhou, MR Philips - Cold Spring …, 2018 - perspectivesinmedicine.cshlp.org
The three human RAS genes encode four proteins that play central roles in oncogenesis by
acting as binary molecular switches that regulate signaling pathways for growth and …

Covalent protein labeling at glutamic acids

P Martín-Gago, EK Fansa, M Winzker, S Murarka… - Cell chemical …, 2017 - cell.com
Covalent labeling of amino acids in proteins by reactive small molecules, in particular at
cysteine SH and lysine NH groups, is a powerful approach to identify and characterize …

Selected approaches to disrupting protein–protein interactions within the MAPK/RAS pathway

SJ Harwood, CR Smith, JD Lawson… - International Journal of …, 2023 - mdpi.com
Within the MAPK/RAS pathway, there exists a plethora of protein–protein interactions (PPIs).
For many years, scientists have focused efforts on drugging KRAS and its effectors in hopes …