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Development of New Drugs for an Old Target — The Penicillin Binding Proteins
2012
Molecules
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We present transition state analogs such as boronic acids, which can covalently bind to the active serine residue in the catalytic site. ...
Some of these novel inhibitors are active against major pathogens, including methicillin-resistant Staphylococcus aureus (MRSA) and thus open avenues new for the discovery of novel antibiotics. ...
Transition State Analogs Transition state analog inhibitors ( Figure 2 ) have been found to be efficient inhibitors of serine β-lactamases [6, 21, 22] as previously observed for serine proteases [64 ...
doi:10.3390/molecules171112478
pmid:23095893
fatcat:yvy6shbyufgmfowuxf35gsdoia
Biochemical and Structural Analysis of Inhibitors Targeting the ADC-7 Cephalosporinase of Acinetobacter baumannii
2014
Biochemistry
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The ADC-7/BATSI complex provides insight into recognition of non-β-lactam inhibitors by ADC enzymes and offers a starting point for the structure-based optimization of this class of novel β-lactamase inhibitors ...
Currently, β-lactamase inhibitors are structurally similar to β-lactam substrates and are not effective inactivators of this class C cephalosporinase. ...
(B) Clavulanic acid, a β-lactam-based β-lactamase inhibitor (BLI). (C) Novel boronic acid transition state analog inhibitors (BATSIs). ...
doi:10.1021/bi500887n
pmid:25380506
pmcid:PMC4263437
fatcat:dpin2jksfrfmlgdfndry55teu4
Carbapenemases
[chapter]
2018
Growing and Handling of Bacterial Cultures [Working Title]
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Carbapenems are stable against wide range of serine-based β-lactamases including extended-spectrum β-lactamases (ESBLs), plasmid-mediated AmpC β-lactamases or against strains with inducible and derepressed ...
expression of chromosomal AmpC β-lactamases. ...
There are also several inhibitor-based tests using different inhibitors (EDTA and phenantroline as inhibitors of MBLs, phenylboronic acid as inhibitor of KPC) in combination with carbapenem (e.g., meropenem ...
doi:10.5772/intechopen.76282
fatcat:4lgtmbp6cbdpdlfcfz44g2hiaq
Click Chemistry in Lead Optimization of Boronic Acids as β-Lactamase Inhibitors
2015
Journal of Medicinal Chemistry
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Boronic acid transition state inhibitors (BATSIs) represent one of the most promising class of βlactamase inhibitors. ...
The K i value of the best compound (13a) was as low as 4 nM with significant reduction of bacterial resistance to the combination of cefotaxime/ 13a. ...
Acknowledgments
Funding The Cleveland Department of Veterans Affairs, the Veterans Affairs Merit Review Program award number 1I01BX001974, and the Geriatric Research Education and Clinical Center VISN ...
doi:10.1021/acs.jmedchem.5b00341
pmid:26102369
pmcid:PMC5744665
fatcat:ybzl5wuv2fhkxjs24t5mdonn6i
Effects of Phenotype and Genotype on Methods for Detection of Extended-Spectrum- -Lactamase-Producing Clinical Isolates of Escherichia coli and Klebsiella pneumoniae in Norway
2006
Journal of Clinical Microbiology
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Inhibitor-based test for KPC: The CDT using boronic acid (usually 3-aminophenyulboronic acid) as inhibitor for class A carbapenemases is currently the most extensively used and evaluated method for detection ...
Inhibitor-based test for MBLs: The ability of EDTA (ethylene diamine tetra-acetic acid) and dipicolinic acid as metal chelating agents for the detection of MBL-producing Enterobacteriaceae has been evaluated ...
doi:10.1128/jcm.01319-06
pmid:17079502
pmcid:PMC1828980
fatcat:u3kjemdfcbhzfl3c3edbgcg3oy
NDM Metallo-β-Lactamases and Their Bacterial Producers in Health Care Settings
2019
Clinical Microbiology Reviews
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SUMMARY New Delhi metallo-β-lactamase (NDM) is a metallo-β-lactamase able to hydrolyze almost all β-lactams. ...
Evidence-based guidelines on prevention and control of carbapenem-resistant Gram-negative bacteria are available, although none are specific for NDM-positive strains. ...
These studies are mainly aimed at CRE as a whole, most of which have serine-based -lactamases, such as KPC and OXA-48, rather than NDM. ...
doi:10.1128/cmr.00115-18
pmid:30700432
pmcid:PMC6431124
fatcat:snaihbmlpjdzxb7xugkd6mbi34
Insights into the Antimicrobial Potential of Dithiocarbamate Anions and Metal-Based Species
2021
Inorganics
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Overuse and poor disposal of antibacterial agents abet the emergence of bacterial resistance mechanisms. There is a clear need for new approaches for the development of antibacterial therapeutics. ...
This bibliographic review of the literature points to the exciting potential of dithiocarbamate-based therapeutics in the crucial battle against bacteria. ...
Unlike other serine-containing beta-lactamases (Classes A, C, and D), the activity of MBLs is not susceptible to beta-lactam inhibitors such as clavulanic acid, sulbactam, and tazobactam [138] . ...
doi:10.3390/inorganics9060048
fatcat:irmf4w2nmrahnpl745356bnm3q
Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors
2013
Journal of the American Chemical Society
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Fragment-based ligand design and covalent targeting of noncatalytic cysteines have been employed to develop potent and selective kinase inhibitors. ...
Using this strategy, we identify electrophilic fragments with sufficient ligand efficiency and selectivity to serve as starting points for the first reported inhibitors of the MSK1 C-terminal kinase domain ...
The approach is especially wellsuited to the reversible, and hence thermodynamically driven, inhibitors discovered for β-lactamase and RSK2. ...
doi:10.1021/ja401221b
pmid:23540679
pmcid:PMC3665406
fatcat:d6dcnik7kreqdgsmlg5hwbvyce
Scientific Opinion on Carbapenem resistance in food animal ecosystems
2013
EFSA Journal
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Carbapenems are broad-spectrum β-lactam antimicrobials used for the treatment of serious infections in humans. ...
Biochemical and phenotypic tests for the confirmatory identification of CP bacteria are available. ...
Based on their hydrolytic mechanism, carbapenemases are classified into two distinct groups, the serine carbapenemases (with an active site serine) and the metallo-β-lactamases (MBL) (with Zinc [Zn] ions ...
doi:10.2903/j.efsa.2013.3501
fatcat:azurwicq5jfqhic32bwle4vgai
Design, Synthesis, and Utility of Defined Molecular Scaffolds
2021
Organics
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Diverse derivatizable structures—here termed "scaffolds" comprised of "hubs"—provide the foundation for systematic covalent organization of a rich variety of building blocks. ...
The review covers the history of the field up through 2020, briefly touching on statistically derivatized carriers employed in immunology as counterpoints to the rationally assembled and derivatized scaffolds ...
triggerable cross-linking; (C) the carbacephem antibiotic Loracarbef as a covalent labeling agent for a mutant β-lactamase, which as part of a fusion protein can bear another molecule (e.g., an enzyme ...
doi:10.3390/org2030013
fatcat:kqyohaybivd2jawctszfbqvlju
Boron Chemicals in Drug Discovery and Development: Synthesis and Medicinal Perspective
2022
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In this review, we collectively represent the current boron-containing drug candidates, boron-containing retinoids, benzoxaboroles, aminoboronic acid, carboranes, and BODIPY, for the treatment of different ...
Indeed, the spectrum of boron-based entities as drug candidates against many diseases has grown tremendously since the first clinically tested boron-based drug, Velcade. ...
Acknowledgments: B.D. acknowledges N.I.H. for support R01AI132614-01A1, R21 AA027374-01, 1R01NS109423-01A1.
Conflicts of Interest: The authors declare no conflict of interest. ...
doi:10.3390/molecules27092615
pmid:35565972
pmcid:PMC9104566
fatcat:o2x4ndq5bzawzgrbwifktjpnsi
Poster presentations
2017
International Journal of Antimicrobial Agents
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Antimicrobial susceptibility was determined by the disk diffusion method, based on performance standards of the Clinical Laboratory Standard Institute in 2016. ...
A propensity-score-matched analysis was performed to control for the baseline characteristics at bacteremia onset between the Gram-positive and Gram-negative groups. ...
Acknowledgements: THis study was supported by the Korea Centers for Disease . Keywords: Staphylococcus aureus, vancomycin resistance, VRSA, VISA ...
doi:10.1016/s0924-8579(17)30342-4
fatcat:37t5vj7gwrdvri57w3mquptxzq
A fragment-based approach to the identification of novel ketopantoate reductase inhibitors
2017
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This thesis also describes the risks of false positives in fragment-based identification of KPR inhibitors. ...
In this study, a fragment-based lead design (FBLD) approach was used to identify small molecule inhibitors of KPR. ...
His enthusiasm for research is inspiring and his breadth of knowledge in chemistry and more generally astounds me. This has taught me to appreciate science and research so much more. ...
doi:10.4225/03/58980e0ceddef
fatcat:ipreemfhtvb5vl5t7xhh6lgoku
Strategies to evade resistance: combining biophysical and biochemical approaches to discover compounds addressing new bacterial target systems
[article]
2016
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Biophysical and biochemical test systems are used for identification and characterization of the first hit molecules. ...
The high content of CYP enzymes encoded in the genome provides a promising base for new drug targets. CYP121 is essential for growth in vitro; CYP125 plays an important role for survival in vivo. ...
Bacterial strain used in this study was E. coli K12 BL21 DE3 for protein expression.
ACKNOWLEDGEMENTS We thank S. Amann and C. Scheid for their help in performing all HPLC-MS/MS-based assays. ...
doi:10.22028/d291-23182
fatcat:tggq2giiazf2raqrvqci7fbpzi
I: Catalytic Direct C-H Arylation of Pyrazoles. II: Toward Modulation of Neuroplasticity with Small Molecules
2017
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Part II of this thesis addresses two separate targets to modulate neuroplasticity. In Chapter 2, the TrkB receptor as a potential target for pharmacological modulation is examined. ...
model based on our results is presented. ...
Acknowledgements ** **** 229 results will be discussed, and future work to narrow down the specific receptor(s) involved in GDNF release by isoquinuclidines will be discussed in Section IV.4 of this chapter ...
doi:10.7916/d8794bx2
fatcat:ncvuhwndp5dmpnyxl4aeagmt5a
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