Anil Koul
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View article: Structural insights into MERS and SARS coronavirus membrane proteins
Structural insights into MERS and SARS coronavirus membrane proteins Open
The membrane (M) protein of coronaviruses is essential for maintaining structural integrity during membrane virion budding and viral pathogenesis. Given its high conservation in lineages within the betacoronavirus genus, such as sarbecovir…
View article: A small-molecule SARS-CoV-2 inhibitor targeting the membrane protein
A small-molecule SARS-CoV-2 inhibitor targeting the membrane protein Open
The membrane (M) protein of betacoronaviruses is well conserved and has a key role in viral assembly 1,2 . Here we describe the identification of JNJ-9676, a small-molecule inhibitor targeting the coronavirus M protein. JNJ-9676 demonstrat…
View article: Identification of a broad-spectrum flavivirus inhibitor targeting NS2A, a previously unidentified target
Identification of a broad-spectrum flavivirus inhibitor targeting NS2A, a previously unidentified target Open
Flaviviruses, such as dengue virus (DENV), Zika virus (ZIKV), West Nile virus (WNV), Japanese encephalitis virus (JEV), and yellow fever virus (YFV), constitute a significant public health concern with billions of people at risk of infecti…
View article: Therapeutic efficacy of JNJ-49214698, an RSV fusion inhibitor, in RSV-infected neonatal lambs
Therapeutic efficacy of JNJ-49214698, an RSV fusion inhibitor, in RSV-infected neonatal lambs Open
Respiratory syncytial virus (RSV) is a leading cause of respiratory infection, hospitalization and death in infants worldwide. No fully effective RSV therapy using direct antivirals is marketed. Since clinical efficacy data from naturally …
View article: Insights into the use of cytochrome bc1 inhibitors for future therapeutic strategies for tuberculosis
Insights into the use of cytochrome bc1 inhibitors for future therapeutic strategies for tuberculosis Open
Recent efforts to improve tuberculosis (TB) treatment options have focused on developing molecules with novel mechanisms of action and identifying optimal treatment regimens. Inhibition of Mycobacterium tuberculosis cytochrome bc1 oxidase …
View article: An open-access dashboard to interrogate the genetic diversity of Mycobacterium tuberculosis clinical isolates
An open-access dashboard to interrogate the genetic diversity of Mycobacterium tuberculosis clinical isolates Open
Tuberculosis (TB) remains one of the leading infectious disease killers in the world. The ongoing development of novel anti-TB medications has yielded potent compounds that often target single sites with well-defined mechanisms of action. …
View article: Targeting de novo purine biosynthesis for tuberculosis treatment
Targeting de novo purine biosynthesis for tuberculosis treatment Open
Tuberculosis remains the leading cause of death from an infectious disease, responsible for 1.3 million deaths annually. Here, we report the discovery of a first-in-class small molecule inhibitor targeting PurF, the first enzyme in the myc…
View article: JNJ-7184, a respiratory syncytial virus inhibitor targeting the connector domain of the viral polymerase
JNJ-7184, a respiratory syncytial virus inhibitor targeting the connector domain of the viral polymerase Open
Respiratory syncytial virus (RSV) can cause pulmonary complications in infants, elderly and immunocompromised patients. While two vaccines and two prophylactic monoclonal antibodies are now available, treatment options are still needed. JN…
View article: A small-molecule SARS-CoV-2 inhibitor targeting the membrane protein
A small-molecule SARS-CoV-2 inhibitor targeting the membrane protein Open
The membrane (M) protein of betacoronaviruses is well-conserved and plays a key role in viral assembly. Here, we describe the discovery of JNJ-9676, a novel small molecule targeting the coronaviral (CoV) M protein. JNJ-9676 demonstrates in…
View article: Penetratin inhibits α-synuclein fibrillation and improves locomotor functions in mice model of Parkinson’s disease
Penetratin inhibits α-synuclein fibrillation and improves locomotor functions in mice model of Parkinson’s disease Open
Parkinson’s disease (PD) is the second most common neurodegenerative disease. The presence of lewy bodies, primarily consisting of α-synuclein (α-syn) aggregates is one of the common features seen in the substantia nigra region of the brai…
View article: Discovery of 3-({5-Chloro-1-[3-(methylsulfonyl)propyl]-1<i>H</i>-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2<i>H</i>-imidazo[4,5-<i>c</i>]pyridin-2-one (JNJ-53718678), a Potent and Orally Bioavailable Fusion Inhibitor of Respiratory Syncytial Virus
Discovery of 3-({5-Chloro-1-[3-(methylsulfonyl)propyl]-1<i>H</i>-indol-2-yl}methyl)-1-(2,2,2-trifluoroethyl)-1,3-dihydro-2<i>H</i>-imidazo[4,5-<i>c</i>]pyridin-2-one (JNJ-53718678), a Potent and Orally Bioavailable Fusion Inhibitor of Respiratory Syncytial Virus Open
Respiratory syncytial virus (RSV) is a seasonal virus that infects the lungs and airways of 64 million children and adults every year. It is a major cause of acute lower respiratory tract infection and is associated with significant morbid…
View article: Design, Synthesis, and Biological Evaluation of Novel Indoles Targeting the Influenza PB2 Cap Binding Region
Design, Synthesis, and Biological Evaluation of Novel Indoles Targeting the Influenza PB2 Cap Binding Region Open
In the search for novel influenza inhibitors we evaluated 7-fluoro-substituted indoles as bioisosteric replacements for the 7-azaindole scaffold of Pimodivir, a PB2 (polymerase basic protein 2) inhibitor currently in clinical development. …
View article: Targeting Energy Metabolism in <i>Mycobacterium tuberculosis</i> , a New Paradigm in Antimycobacterial Drug Discovery
Targeting Energy Metabolism in <i>Mycobacterium tuberculosis</i> , a New Paradigm in Antimycobacterial Drug Discovery Open
Drug-resistant mycobacterial infections are a serious global health challenge, leading to high mortality and socioeconomic burdens in developing countries worldwide. New innovative approaches, from identification of new targets to discover…
View article: Synthesis, characterization and biological activity of fluorescently labeled bedaquiline analogues
Synthesis, characterization and biological activity of fluorescently labeled bedaquiline analogues Open
Labeling the tuberculosis drug bedaquiline with a fluorescent alkynyl-BODIPY moiety does not disrupt its antibacterial properties.