Search Results - "Dömling, Alexander S S"

Identification and characterization of a small molecule that activates thiosulfate sulfurtransferase and stimulates mitochondrial respiration by Al‐Dahmani, Zeyana M., Hadian, Mojgan, Ruiz‐Moreno, Angel J., Maria, Sabogal‐Guaqueta Angelica, Batista, Fernando A., Zhang, Ran, Luo, Yang, Sadremomtaz, Afsaneh, Straat, Robin, Spoor, Mette, Dolga, Amalia M., Dekker, Frank J., S S, Alexander Dömling, Goor, Harry, Groves, Matthew R.

“…The enzyme Thiosulfate sulfurtransferase (TST, EC 2.8.1.1), is a positive genetic predictor of diabetes type 2 and obesity. As increased TST activity protects…”
Get full text

Discovery of Small-Molecule Allosteric Inhibitors of PfATC as Antimalarials by Wang, Chao, Zhang, Bidong, Krüger, Arne, Du, Xiaochen, Visser, Lidia, Dömling, Alexander S S, Wrenger, Carsten, Groves, Matthew R

“…The discovery and development of new drugs against malaria remain urgent. Aspartate transcarbamoylase (ATC) has been suggested to be a promising target for…”
Get full text

Inhibitors of Aspartate Transcarbamoylase Inhibit Mycobacterium tuberculosis Growth by Du, Xiaochen, Sonawane, Vidhisha, Zhang, Bidong, Wang, Chao, Ruijter, Bram, Dömling, Alexander S. S., Reiling, Norbert, Groves, Matthew R.

“…Aspartate transcarbamoylase (ATCase) plays a key role in the second step of de novo pyrimidine biosynthesis in eukaryotes and has been proposed to be a target…”
Get full text

A Systematic Protein Refolding Screen Method using the DGR Approach Reveals that Time and Secondary TSA are Essential Variables by Wang, Yuanze, van Oosterwijk, Niels, Ali, Ameena M., Adawy, Alaa, Anindya, Atsarina L., Dömling, Alexander S. S., Groves, Matthew R.

“…Refolding of proteins derived from inclusion bodies is very promising as it can provide a reliable source of target proteins of high purity. However, inclusion…”
Get full text

Pharmacological Rationale for Targeting IL-17 in Asthma by Rahmawati, Siti Farah, Te Velde, Maurice, Kerstjens, Huib A M, Dömling, Alexander S S, Groves, Matthew Robert, Gosens, Reinoud

“…Asthma is a respiratory disease that currently affects around 300 million people worldwide and is defined by coughing, shortness of breath, wheezing, mucus…”
Get full text

A fragment-based approach identifies an allosteric pocket that impacts malate dehydrogenase activity by Reyes Romero, Atilio, Lunev, Serjey, Popowicz, Grzegorz M., Calderone, Vito, Gentili, Matteo, Sattler, Michael, Plewka, Jacek, Taube, Michał, Kozak, Maciej, Holak, Tad A., Dömling, Alexander S. S., Groves, Matthew R.

“…Malate dehydrogenases (MDHs) sustain tumor growth and carbon metabolism by pathogens including Plasmodium falciparum . However, clinical success of MDH…”
Get full text

Molecular Target Validation of Aspartate Transcarbamoylase from Plasmodium falciparum by Torin 2 by Bosch, Soraya S, Lunev, Sergey, Batista, Fernando A, Linzke, Marleen, Kronenberger, Thales, Dömling, Alexander S. S, Groves, Matthew R, Wrenger, Carsten

“…Malaria is a tropical disease that kills about half a million people around the world annually. Enzymatic reactions within pyrimidine biosynthesis have been…”
Get full text

Oligomeric protein interference validates druggability of aspartate interconversion in Plasmodium falciparum by Batista, Fernando A., Bosch, Soraya S., Butzloff, Sabine, Lunev, Sergey, Meissner, Kamila A., Linzke, Marleen, Romero, Atilio R., Wang, Chao, Müller, Ingrid B., Dömling, Alexander S. S., Groves, Matthew R., Wrenger, Carsten

“…The appearance of multi‐drug resistant strains of malaria poses a major challenge to human health and validated drug targets are urgently required. To define a…”
Get full text

Small‐Molecule Allosteric Inhibitors of Human Aspartate Transcarbamoylase Suppress Proliferation of Bone Osteosarcoma Epithelial Cells by Wang, Chao, Zhang, Bidong, Cong, Yingying, Du, Xiaochen, Chen, Siyao, Visser, Lidia, Ruiz‐Moreno, Angel J., Zhang, Lili, Reggiori, Fulvio, Dömling, Alexander S. S., Groves, Matthew R.

“…Aspartate transcarbamoylase (ATC) is the first committed step in de novo pyrimidine biosynthesis in eukaryotes and plants. A potent transition state analog of…”
Get full text

Identification of potential antivirulence agents by substitution-oriented screening for inhibitors of Streptococcus pyogenes sortase A by Wójcik, Magdalena, Eleftheriadis, Nikolaos, Zwinderman, Martijn R.H., Dömling, Alexander S.S., Dekker, Frank J., Boersma, Ykelien L.

“…Antimicrobial resistance resulting in ineffective treatment of infectious diseases is an increasing global problem, particularly in infections with pathogenic…”
Get full text

ANCHOR: a web server and database for analysis of protein-protein interaction binding pockets for drug discovery by Meireles, Lidio M C, Dömling, Alexander S, Camacho, Carlos J

“…ANCHOR is a web-based tool whose aim is to facilitate the analysis of protein-protein interfaces with regard to its suitability for small molecule drug design…”
Get full text

Identification of a non-competitive inhibitor of Plasmodium falciparum aspartate transcarbamoylase by Lunev, Sergey, Bosch, Soraya S., Batista, Fernando A., Wang, Chao, Li, Jingyao, Linzke, Marleen, Kruithof, Paul, Chamoun, George, Dömling, Alexander S.S., Wrenger, Carsten, Groves, Matthew R.

“…Aspartate transcarbamoylase catalyzes the second step of de-novo pyrimidine biosynthesis. As malarial parasites lack pyrimidine salvage machinery and rely on…”
Get full text

High Endurance Elite Athletes Show Age-dependent Lower Levels of Circulating Complements Compared to Low/Moderate Endurance Elite Athletes by Al-Muraikhy, Shamma, Ramanjaneya, Manjunath, Dömling, Alexander S., Bettahi, Ilham, Donati, Francesco, Botre, Francesco, Abou-Samra, Abdul-Badi, Sellami, Maha, Elrayess, Mohamed A

“…Introduction: Aerobic exercise activates the complement system in the peripheral blood. However, the effect of age and high intensity endurance training on the…”
Get full text

Metabolic Signature of Leukocyte Telomere Length in Elite Male Soccer Players by Al-Muraikhy, Shamma, Sellami, Maha, Domling, Alexander S, Rizwana, Najeha, Agouni, Abdelali, Al-Khelaifi, Fatima, Donati, Francesco, Botre, Francesco, Diboun, Ilhame, Elrayess, Mohamed A

“…Biological aging is associated with changes in the metabolic pathways. Leukocyte telomere length (LTL) is a predictive marker of biological aging; however, the…”
Get full text

In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of pyrazole-based small molecule inhibitors of Mdm2/4–p53 interaction by Christner, Susan M., Clausen, Dana M., Beumer, Jan H., Parise, Robert A., Guo, Jianxia, Huang, Yijun, Dömling, Alexander S., Eiseman, Julie L.

“…Purpose The interaction of p53 with its negative regulators Mdm2/4 has been widely studied (Khoury and Domling in Curr Pharm Des 18(30):4668–4678, 2012 ). In…”
Get full text

Crystal structure of truncated human coatomer protein complex subunit ζ1 (Copζ1) by Lunev, Sergey, Semmelink, Marije F. W., Xian, Jia Ling, Ma, Kai Yu, Leenders, Anna J. A., Dömling, Alexander S. S., Shtutman, Michael, Groves, Matthew R.

“…The majority of modern anticancer approaches target DNA/protein targets involved in tumour‐cell proliferation. Such approaches have a major drawback, as…”
Get full text

Discovery of Small-Molecule Allosteric Inhibitors of Pf ATC as Antimalarials by Wang, Chao, Zhang, Bidong, Krüger, Arne, Du, Xiaochen, Visser, Lidia, Dömling, Alexander S S, Wrenger, Carsten, Groves, Matthew R

Get full text

Crystal structure of truncated human coatomer protein complex subunit [zeta]1 (Cop[zeta]1) by Lunev, Sergey, Semmelink, Marije FW, Xian, Jia Ling, Ma, Kai Yu, Leenders, Anna JA, Domling, Alexander SS, Shtutman, Michael, Groves, Matthew R

“…The majority of modern anticancer approaches target DNA/protein targets involved in tumour-cell proliferation. Such approaches have a major drawback, as…”
Get full text

Abstract 4726: Novel small molecule inhibitors of MDM2/4-p53 interaction, YH264 and its ethyl ester YH263: preclinical evaluation by Christner, Susan M., Clausen, Dana M., Beumer, Jan H., Parise, Robert A., Huang, Yi, Dömling, Alexander S., Eiseman, Julie L.

“…Introduction: In p53+/+ cells, expression of MDM2/4 leads to turnover of p53 and inhibition of downstream gene transcription decreasing cell cycle arrest or…”
Get full text