The expanding repertoire of covalent warheads for drug discovery

NV Mehta, MS Degani - Drug Discovery Today, 2023 - Elsevier
The reactive functionalities of drugs that engage in covalent interactions with the
enzyme/receptor residue in either a reversible or an irreversible manner are …

[HTML][HTML] The development of New Delhi metallo-β-lactamase-1 inhibitors since 2018

X Gu, M Zheng, L Chen, H Li - Microbiological Research, 2022 - Elsevier
New Delhi metallo-β-lactamase-1 (NDM-1) can hydrolyze almost all antibiotics of the β-
lactam group, resulting in the generation of multidrug resistant bacteria. Besides its broad …

[PDF][PDF] TIGER NUT (CYPERUS ESCULENTUS): SOURCE OF NATURAL ANTICANCER DRUG? BRIEF REVIEW OF EXISTING LITERATURE.

ES Achoribo, MT Ong - Euromediterranean Biomedical Journal, 2017 - academia.edu
In some parts of the world, Cyperus esculentus L. is widely used as a healthy food for both
humans and animals due to their nutritional and functional properties. Current research and …

A lysine-targeted affinity label for serine-β-lactamase also covalently modifies New Delhi metallo-β-lactamase-1 (NDM-1)

PW Thomas, M Cammarata, JS Brodbelt… - Biochemistry, 2019 - ACS Publications
The divergent sequences, protein structures, and catalytic mechanisms of serine-and
metallo-β-lactamases hamper the development of wide-spectrum β-lactamase inhibitors that …

The role of SERPIN citrullination in thrombosis

R Tilvawala, VV Nemmara, AC Reyes, N Sorvillo… - Cell chemical …, 2021 - cell.com
Aberrant protein citrullination is associated with many pathologies; however, the specific
effects of this modification remain unknown. We have previously demonstrated that serine …

The analysis of the antibiotic resistome offers new opportunities for therapeutic intervention

F Corona, P Blanco, M Alcalde-Rico… - Future medicinal …, 2016 - Taylor & Francis
Most efforts in the development of antimicrobials have focused on the screening of lethal
targets. Nevertheless, the constant expansion of antimicrobial resistance makes the …

Insights into dynamic changes in ADC-7 and P99 cephalosporinases using small angle x-ray scattering (SAXS)

I Kumar, A Sagar, K Dhiman, CR Bethel… - Journal of …, 2024 - Taylor & Francis
To counter the emergence of β-lactamase (BL) mediated resistance, design of new β-
lactamase inhibitors (BLIs) is critical. Many high-resolution crystallographic structures of BL …

[HTML][HTML] Evaluation of the safety profile and antioxidant activity of fatty hydroxamic acid from underutilized seed oil of Cyperus esculentus

A Adewuyi, CA Otuechere, ZO Oteglolade… - Journal of Acute …, 2015 - Elsevier
Objective To evaluate the safety profile and antioxidant activity of fatty hydroxamic acid
(FHA) from the seed oil of Cyperus esculentus (C. esculentus). Methods FHA was …

A new covalent inhibitor of class C β-lactamases reveals extended active site specificity

R Tilvawala, M Cammarata, SA Adediran… - Biochemistry, 2015 - ACS Publications
O-Aryloxycarbonyl hydroxamates have previously been shown to efficiently inactivate class
C β-lactamases by cross-linking serine and lysine residues in the active site. A new …

Kinetics of action of a two-stage pro-inhibitor of serine β-lactamases

R Tilvawala, RF Pratt - Biochemistry, 2013 - ACS Publications
β-Lactamase inhibitors are important in medicine in the protection of β-lactam antibiotics
from β-lactamase-catalyzed destruction. The most effective inhibitors of serine β-lactamases …