[HTML][HTML] Design and synthesis of novel antimicrobial agents
Z Breijyeh, R Karaman - Antibiotics, 2023 - mdpi.com
The necessity for the discovery of innovative antimicrobials to treat life-threatening diseases
has increased as multidrug-resistant bacteria has spread. Due to antibiotics' availability over …
has increased as multidrug-resistant bacteria has spread. Due to antibiotics' availability over …
[PDF][PDF] Protein crystallography and drug discovery: recollections of knowledge exchange between academia and industry
TL Blundell - IUCrJ, 2017 - journals.iucr.org
The development of structure-guided drug discovery is a story of knowledge exchange
where new ideas originate from all parts of the research ecosystem. Dorothy Crowfoot …
where new ideas originate from all parts of the research ecosystem. Dorothy Crowfoot …
Arginine-deprivation–induced oxidative damage sterilizes Mycobacterium tuberculosis
Reactive oxygen species (ROS)-mediated oxidative stress and DNA damage have recently
been recognized as contributing to the efficacy of most bactericidal antibiotics, irrespective of …
been recognized as contributing to the efficacy of most bactericidal antibiotics, irrespective of …
Fragment-Based Approach to Targeting Inosine-5′-monophosphate Dehydrogenase (IMPDH) from Mycobacterium tuberculosis
A Trapero, A Pacitto, V Singh, M Sabbah… - Journal of medicinal …, 2018 - ACS Publications
Tuberculosis (TB) remains a major cause of mortality worldwide, and improved treatments
are needed to combat emergence of drug resistance. Inosine 5′-monophosphate …
are needed to combat emergence of drug resistance. Inosine 5′-monophosphate …
Structure-guided fragment-based drug discovery at the synchrotron: screening binding sites and correlations with hotspot mapping
Structure-guided drug discovery emerged in the 1970s and 1980s, stimulated by the three-
dimensional structures of protein targets that became available, mainly through X-ray crystal …
dimensional structures of protein targets that became available, mainly through X-ray crystal …
Fragment-Based Design of Mycobacterium tuberculosis InhA Inhibitors
M Sabbah, V Mendes, RG Vistal… - Journal of medicinal …, 2020 - ACS Publications
Tuberculosis (TB) remains a leading cause of mortality among infectious diseases
worldwide. InhA has been the focus of numerous drug discovery efforts as this is the target of …
worldwide. InhA has been the focus of numerous drug discovery efforts as this is the target of …
Development of Inhibitors of SAICAR Synthetase (PurC) from Mycobacterium abscessus Using a Fragment-Based Approach
S Charoensutthivarakul, SE Thomas… - ACS infectious …, 2022 - ACS Publications
Mycobacterium abscessus (Mab) has emerged as a challenging threat to individuals with
cystic fibrosis. Infections caused by this pathogen are often impossible to treat due to the …
cystic fibrosis. Infections caused by this pathogen are often impossible to treat due to the …
[HTML][HTML] A fragment-based approach to assess the ligandability of ArgB, ArgC, ArgD and ArgF in the L-arginine biosynthetic pathway of Mycobacterium tuberculosis
P Gupta, SE Thomas, SA Zaidan, MA Pasillas… - Computational and …, 2021 - Elsevier
The L-arginine biosynthesis pathway consists of eight enzymes that catalyse the conversion
of L-glutamate to L-arginine. Arginine auxotrophs (argB/argF deletion mutants) of …
of L-glutamate to L-arginine. Arginine auxotrophs (argB/argF deletion mutants) of …
Mycobacterial genomics and structural bioinformatics: opportunities and challenges in drug discovery
Of the more than 190 distinct species of Mycobacterium genus, many are economically and
clinically important pathogens of humans or animals. Among those mycobacteria that infect …
clinically important pathogens of humans or animals. Among those mycobacteria that infect …
[HTML][HTML] Biosynthesis of Galactan in Mycobacterium tuberculosis as a Viable TB Drug Target?
Z Konyariková, K Savková, S Kozmon, K Mikušová - Antibiotics, 2020 - mdpi.com
While target-based drug design has proved successful in several therapeutic areas, this
approach has not yet provided compelling outcomes in the field of antibacterial agents. This …
approach has not yet provided compelling outcomes in the field of antibacterial agents. This …