Enzyme inhibitor activity, protein dimerization, skeletal system development and pathways in cancer are functionally associated with proteins displaying a high or very high affinity for heparin (KD < 100 nM). Besides their use in investigating molecular recognition and functions, kinetics and affinity ...
Molecules that covalently engage target proteins are widely used as activity-based probes and covalent drugs. The performance of these covalent inhibitors is, however, often compromised by the paradox of efficacy and risk, which demands a balance between reactivity and selectivity. The challenge is mo...
et al. Phosphorylation of CpgA protein enhances both its GTPase activity and its affinity for ribosome and is crucial for Bacillus subtilis growth and morphology. J. Biol. Chem. 287, 20830–20838 (2012). Article CAS PubMed PubMed Central Google Scholar Pompeo, F., Foulquier, E., Serrano...
It is primarily used for the development and validation of computational methods for predicting molecular interactions AB-Bind AB-Bind is a database for antibody binding affinity data. It offers a curated set of experimental binding data and corresponding antibody-protein complex structures AntigenDB ...
New prospects for the applications of single-stranded DNA and RNA as therapeutic agents have been discovered in the recent years. Aptamers are the oligonucleotides that bind to their targets with high affinity and specificity due to the well-defined tertiary structures and spatial charge distribution....
Blockade of NMT1 enzymatic activity inhibits N-myristoylation of VILIP3 protein and suppresses liver cancer progression (NMT1)was identified as a target protein of desloratadine by drug affinity responsive target stability(DARTS)and surface plasmon resonance(SPR)assays.Up... XP Tan,Y He,J Yang,....
Activity-based protein profiling of covalent inhibitors Activity-based protein profiling (ABPP) is a type of chemical proteome method that aims to evaluate the on-target and off-target activities of a covalent drug. In ABPP, activity-based probes (ABPs) are used to visualize the target protein...
JUN proteins can both homo- and hetero-dimerize, whereas FOS proteins only form hetero-dimers, which, particularly for JUN/FOS, are more stable and have greater transcriptional activity [9,10]. Intriguingly, c-FOS and FOSB contain transcriptional activation domains which are lacking in FRA-1 and...
and distinct phosphorylation and de-phosphorylation mechanisms have evolved to control the activity ofprotein kinasesthrough a reversible alteration inenzyme conformation. The structural plasticity of theprotein kinasedomain is key to its function, allowing the enzyme to cycle from an inactive unphosphorylat...
Figure 4: Presence and catalytic activity of PP4 are required to regulate mitotic centromere integrity. (a) A proportion of CENP-C is mislocalized from the centromeres and accumulated along the spindle and spindle poles inflfl-depleted mitotic cells.kanRNAi is used as a negative control. The ...