Surface plasmon resonance as a fascinating approach in target-based drug discovery and development
Abstract Surface Plasmon Resonance (SPR) technology has been proven to be a significant
approach for target-based drug discovery and development in the modern era. SPR unfolds …
approach for target-based drug discovery and development in the modern era. SPR unfolds …
Epistasis arises from shifting the rate-limiting step during enzyme evolution of a β-lactamase
Epistasis, the non-additive effect of mutations, can provide combinatorial improvements to
enzyme activity that substantially exceed the gains from individual mutations. Yet the …
enzyme activity that substantially exceed the gains from individual mutations. Yet the …
A review on the mechanistic details of OXA enzymes of ESKAPE pathogens
The production of β-lactamases is a prevalent mechanism that poses serious pressure on
the control of bacterial resistance. Furthermore, the unavoidable and alarming increase in …
the control of bacterial resistance. Furthermore, the unavoidable and alarming increase in …
Discovery of triazolyl derivatives of cucurbitacin B targeting IGF2BP1 against non-small cell lung cancer
FF Shang, Q Lu, T Lin, M Pu, R Xiao… - Journal of Medicinal …, 2023 - ACS Publications
Cucurbitacin B (CuB) is a potent but toxic anticancer natural product. Herein, we designed
and synthesized 2-OH-and 16-OH-modified CuB derivatives to improve their antitumor …
and synthesized 2-OH-and 16-OH-modified CuB derivatives to improve their antitumor …
OXA-48-mediated ceftazidime-avibactam resistance is associated with evolutionary trade-offs
Infections due to carbapenemase-producing Gram-negative pathogens are associated with
limited treatment options and consequently lead to increased mortality and morbidity. In …
limited treatment options and consequently lead to increased mortality and morbidity. In …
Identifying oxacillinase-48 carbapenemase inhibitors using DNA-encoded chemical libraries
Bacterial resistance to β-lactam antibiotics is largely mediated by β-lactamases, which
catalyze the hydrolysis of these drugs and continue to emerge in response to antibiotic use …
catalyze the hydrolysis of these drugs and continue to emerge in response to antibiotic use …
Exploiting the Carboxylate-Binding Pocket of β-Lactamase Enzymes Using a Focused DNA-Encoded Chemical Library
β-Lactamase enzymes hydrolyze and thereby provide bacterial resistance to the important β-
lactam class of antibiotics. The OXA-48 and NDM-1 β-lactamases cause resistance to the …
lactam class of antibiotics. The OXA-48 and NDM-1 β-lactamases cause resistance to the …
In silico fragment-based design identifies subfamily B1 metallo-β-lactamase inhibitors
R Cain, J Brem, D Zollman… - Journal of Medicinal …, 2018 - ACS Publications
Zinc ion-dependent β-lactamases (MBLs) catalyze the hydrolysis of almost all β-lactam
antibiotics and resist the action of clinically available β-lactamase inhibitors. We report how …
antibiotics and resist the action of clinically available β-lactamase inhibitors. We report how …
Progress toward B-cell lymphoma 6 BTB domain inhibitors for the treatment of diffuse large B-cell lymphoma and beyond
Y Ai, L Hwang, AD MacKerell Jr… - Journal of medicinal …, 2021 - ACS Publications
B-cell lymphoma 6 (BCL6) is a master regulator of germinal center formation that produce
antibody-secreting plasma cells and memory B-cells for sustained immune responses. The …
antibody-secreting plasma cells and memory B-cells for sustained immune responses. The …
Discovery of a B-cell lymphoma 6 protein–protein interaction inhibitor by a biophysics-driven fragment-based approach
Y Kamada, N Sakai, S Sogabe, K Ida… - Journal of medicinal …, 2017 - ACS Publications
B-cell lymphoma 6 (BCL6) is a transcriptional factor that expresses in lymphocytes and
regulates the differentiation and proliferation of lymphocytes. Therefore, BCL6 is a …
regulates the differentiation and proliferation of lymphocytes. Therefore, BCL6 is a …