☆ 4.5 Editorial Material

And in the end-Telmisartan directly binds to PPARγ

HYPERTENSION RESEARCH (2012)

Journal

HYPERTENSION RESEARCH

Volume 35, Issue 7, Pages 704-705

Publisher

NATURE PUBLISHING GROUP

DOI: 10.1038/hr.2012.35

Keywords

Ask authors/readers for more resources

Protocol

Community support

Reagent

Community support

Authors

I am an author on this paper

Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.5

Not enough ratings

Secondary Ratings

Novelty

Significance

Scientific rigor

Rate this paper

Propofol directly binds to and inhibits TLR7

Sophia Koutsogiannaki, Weiming Bu, Wiriya Maisat, Mariel Manzor, Zhikuan Zhang, Umeharu Ohto, Roderic G. Eckenhoff, Koichi Yuki

Summary: Sedatives/anesthetics can modulate immune functions, but their effect on TLR7 function is not well understood. This study found that propofol attenuates TLR7 activation and reduces immune response triggered by TLR7 agonist.

FASEB JOURNAL (2022)

Add to Collection

Article Pharmacology & Pharmacy

Telmisartan Potentiates Insulin Secretion via Ion Channels, Independent of the AT1 Receptor and PPARγ

Tao Liu, Lijuan Cui, Huan Xue, Xiaohua Yang, Mengmeng Liu, Linping Zhi, Huanhuan Yang, Zhihong Liu, Min Zhang, Qing Guo, Peifeng He, Yunfeng Liu, Yi Zhang

Summary: This study found that telmisartan exhibited an insulin secretagogue role in rat islets, distinct from other ARBs, possibly by affecting ion channels to promote insulin secretion.

FRONTIERS IN PHARMACOLOGY (2021)

Add to Collection

Article Pharmacology & Pharmacy

Paeoniflorin directly binds to TNFR1 to regulate podocyte necroptosis in diabetic kidney disease

Xian Wang, Xue-qi Liu, Ling Jiang, Yue-bo Huang, Han-xu Zeng, Qi-jin Zhu, Xiang-ming Qi, Yong-gui Wu

Summary: This study found elevated necroptosis in DKD patients and demonstrated that PF can regulate podocyte necroptosis by targeting TNFR1, providing a new potential target for treating DKD.

FRONTIERS IN PHARMACOLOGY (2022)

Add to Collection

Article Multidisciplinary Sciences

Chemoproteomics reveals berberine directly binds to PKM2 to inhibit the progression of colorectal cancer

Shi-Hai Yan, Li-Mu Hu, Xue-Hui Hao, Jiang Liu, Xi-Ying Tan, Zhi-Rong Geng, Jing Ma, Zhi-Lin Wang

Summary: This study revealed the direct binding target protein of berberine in colorectal cancer cells, which is pyruvate kinase isozyme type M2 (PKM2). Berberine inhibits the progression of colorectal cancer through hydrophobic interaction and pi-pi interaction, and it also inhibits the reprogramming of glucose metabolism.

ISCIENCE (2022)

Add to Collection

Article Pharmacology & Pharmacy

Celastrol directly binds with VAMP7 and RAB7 to inhibit autophagy and induce apoptosis in preadipocytes

Chenshu Liu, Na Li, Meixiu Peng, Kan Huang, Dongxiao Fan, Zhengde Zhao, Xiuyi Huang, Yunchong Liu, Sifan Chen, Zilun Li

Summary: Obesity is a common chronic metabolic disease, and inducing apoptosis in preadipocytes and adipocytes is a potential strategy for its treatment. Celastrol was found to induce apoptosis in preadipocytes through a mitochondrial mediated pathway. It was further discovered that celastrol inhibits autophagy by preventing the fusion of autophagosomes and lysosomes, leading to cell apoptosis.

FRONTIERS IN PHARMACOLOGY (2023)

Add to Collection

Editorial Material Biochemistry & Molecular Biology

Two steps, one ligand: How PPARγ binds small-molecule agonists

James J. Siclari, Kevin H. Gardner

Summary: In this study, insights into the binding mechanism of artificial agonists to the PPARg nuclear receptor were presented, supporting a two-step model with induced fit and conformational selection aspects. This mechanism may have implications for drug development in related receptors.

STRUCTURE (2021)

Add to Collection

Article Biochemistry & Molecular Biology

PpEBB1 directly binds to the GCC box-like element of auxin biosynthesis related genes

Xuehui Zhao, Binbin Wen, Chen Li, Li Liu, Xiude Chen, Dongmei Li, Li Ling, Xiling Fu

Summary: The study found that PpEBB1 plays an important role in promoting bud break, potentially regulating the expression of related genes by binding to specific gene promoters in peach and Arabidopsis, thereby affecting auxin biosynthesis. In addition, PpMIEL1 may affect the stability of PpEBB1 through ubiquitination.

PLANT SCIENCE (2021)

Add to Collection

Article Nutrition & Dietetics

Shikonin Binds and Represses PPARγ Activity by Releasing Coactivators and Modulating Histone Methylation Codes

Ui-Hyun Park, HyeSook Youn, Eun-Joo Kim, Soo-Jong Um

Summary: Shikonin, a natural ingredient produced by Lithospermum erythrorhizon, has anti-inflammatory, anti-cancer, and anti-obesity effects. It modulates adipocyte differentiation by regulating adipogenesis-related genes and histone modification. This finding highlights the potential of shikonin in treating obesity-related disorders.

NUTRIENTS (2023)

Add to Collection

Article Multidisciplinary Sciences

Ssu72 phosphatase directly binds to ZAP-70, thereby providing fine-tuning of TCR signaling and preventing inflammation

Jae Sung Ko, Dongjin Jeong, Jaemoon Koh, Hyeryeon Jung, Kyeong Cheon Jung, Yoon Kyung Jeon, Hye Young Kim, Eugene C. Yi, Ho Lee, Chang-Woo Lee, Doo Hyun Chung

Summary: Ssu72 regulates the fine-tuning of TCR signaling by acting as a tyrosine phosphatase for ZAP-70. Ssu72 deficiency leads to hyperresponsiveness in T cells upon TCR stimulation due to increased ZAP-70 phosphorylation, which can be restored by reducing ZAP-70 phosphorylation levels. Additionally, Cd4-CreSsu72fl/fl mice show defects in thymic development and alterations in peripheral T cell populations, with a predisposition for spontaneous inflammation.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2021)

Add to Collection

Article Cardiac & Cardiovascular Systems

Metformin Directly Binds to MMP-9 to Improve Plaque Stability

Xianda Chen, Shuaixing Wang, Wenli Xu, Mingming Zhao, Youyi Zhang, Han Xiao

Summary: Vulnerable atherosclerotic plaque rupture is the main cause of myocardial infarction and stroke. Metformin, commonly used for type 2 diabetes, has been found to improve plaque vulnerability, but its mechanism is unknown. This study showed that metformin directly interacts with MMP-9, reducing its activity and driving its degradation. In a carotid artery plaque model, metformin treatment decreased local MMP-9 protein level and circulating MMP-9 activity, preserved collagen content in plaque, and reduced plaque vulnerability index.

JOURNAL OF CARDIOVASCULAR DEVELOPMENT AND DISEASE (2023)

Add to Collection

Article Chemistry, Multidisciplinary

The SARS-CoV-2 Spike Glycoprotein Directly Binds Exogeneous Sialic Acids: A NMR View

Luca Unione, Maria J. Moure, Maria Pia Lenza, Iker Oyenarte, June Ereno-Orbea, Ana Arda, Jesus Jimenez-Barbero

Summary: The interaction between the SARS CoV2 spike glycoprotein and two sialic acid-containing trisaccharides has been demonstrated, with the sialic acid binding site located at the N-terminal domain.

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION (2022)

Add to Collection

Article Biochemistry & Molecular Biology

Salicylic acid directly binds to ribosomal protein S3 and suppresses CDK4 expression in colorectal cancer cells

Ayaka Imai, Mano Horinaka, Yuichi Aono, Yosuke Iizumi, Hideki Takakura, Hisako Ono, Shusuke Yasuda, Keiko Taniguchi, Emi Nishimoto, Hideki Ishikawa, Michihiro Mutoh, Toshiyuki Sakai

Summary: Colorectal cancer is a serious public health issue. Aspirin has potential as a preventive drug for colorectal cancer. This study identified ribosomal protein S3 (RPS3) as a target protein of aspirin and revealed the negative regulation of RPS3 function by salicylic acid.

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS (2022)

Add to Collection

Article Biochemistry & Molecular Biology

The CLIP-170 N-terminal domain binds directly to both F-actin and microtubules in a mutually exclusive manner

Yueh-Fu O. Wu, Rachel A. Miller, Emily O. Alberico, Yaobing A. P. Huang, Annamarie T. Bryant, Nora T. Nelson, Erin M. Jonasson, Holly Goodson

Summary: Research has shown that CLIP-170 can directly bind to F-actin, and this direct interaction plays an important role in environments with high concentrations of actin. Binding of CLIP-170 to F-actin affects the stability of microtubules, thus influencing the coordinated cooperation between actin and microtubule cytoskeletons within the cell.

JOURNAL OF BIOLOGICAL CHEMISTRY (2022)

Add to Collection

Article Agriculture, Multidisciplinary

End-to-end deep learning for directly estimating grape yield from ground-based imagery

Alexander G. Olenskyj, Brent S. Sams, Zhenghao Fei, Vishal Singh, Pranav Raja, Gail M. Bornhorst, J. Mason Earles

Summary: This study demonstrates the applicability of nondestructive proximal imaging combined with deep learning for yield estimation in vineyards. The results show that the end-to-end modeling approach can perform comparably to the object detection approach while eliminating the need for hand-labeling.

COMPUTERS AND ELECTRONICS IN AGRICULTURE (2022)

Add to Collection

Article Oncology

Eltrombopag binds SDC4 directly and enhances MAPK signaling and macropinocytosis in cancer cells

Can Cui, Yuting Pan, Chengqian Zhang, Darong Zhu, Ying Xuan, Piliang Hao, Xisong Ke, Xianglian Zhou, Yi Qu

Summary: This study demonstrates the important role of SDC4 in pancreatic cancer cells and its potential as a therapeutic target. It also highlights the unexpected effects of the FDA-approved thrombopoietin receptor agonist ETBP on SDC4-associated signaling pathways and macropinocytosis. Caution should be taken when using ETBP for chemotherapy-induced thrombocytopenia in cancer patients.

AMERICAN JOURNAL OF CANCER RESEARCH (2022)

Add to Collection

Article Multidisciplinary Sciences

Fat-body brummer lipase determines survival and cardiac function during starvation in Drosophila melanogaster

Annelie Blumrich, Georg Vogler, Sandra Dresen, Soda Balla Diop, Carsten Jaeger, Sarah Leberer, Jana Grune, Eva K. Wirth, Beata Hoeft, Kostja Renko, Anna Foryst-Ludwig, Joachim Spranger, Stephan Sigrist, Rolf Bodmer, Ulrich Kintscher

Summary: The study revealed that perturbation of fat body lipolysis in fruit flies can protect the heart from dysfunction induced by starvation, by preserving glycerolipid stores and ensuring adequate energy supply for cardiac ATP synthesis. These findings suggest that inhibiting adipose tissue lipolysis could be a protective mechanism against cardiac dysfunction during periods of catabolic stress.

ISCIENCE (2021)

Add to Collection

Article Cell Biology

eIF5A hypusination, boosted by dietary spermidine, protects from premature brain aging and mitochondrial dysfunction

YongTian Liang, Chengji Piao, Christine B. Beuschel, David Toppe, Laxmikanth Kollipara, Boris Bogdanow, Marta Maglione, Janine Lutzkendorf, Jason Chun Kit See, Sheng Huang, Tim O. F. Conrad, Ulrich Kintscher, Frank Madeo, Fan Liu, Albert Sickmann, Stephan J. Sigrist

Summary: Mitochondrial function declines with age in the brain, and supplementing spermidine levels can delay this decline. The levels of hypusinated eIF5A decline with age in the Drosophila brain, but can be boosted by dietary spermidine. Attenuating eIF5A hypusination affects brain mitochondrial respiration and accelerates aging in locomotion and memory formation in adult Drosophilae, indicating it may be a potential diagnostic and therapeutic avenue for age-induced cognitive decline and neurodegeneration.

CELL REPORTS (2021)

Add to Collection

Article Cell Biology

Hypertrophy-Reduced Autophagy Causes Cardiac Dysfunction by Directly Impacting Cardiomyocyte Contractility

Christiane Ott, Tobias Jung, Sarah Brix, Cathleen John, Iris R. Betz, Anna Foryst-Ludwig, Stefanie Deubel, Wolfgang M. Kuebler, Tilman Grune, Ulrich Kintscher, Jana Grune

Summary: Cardiac remodeling and contractile dysfunction are major causes of hypertrophy-associated heart failure, characterized by accumulation of modified proteins due to impaired autophagy-lysosomal pathway in aged and diseased hearts. Autophagy inducer rapamycin has cardioprotective effects by improving cardiomyocyte autophagy and contractility. Endothelin 1 (ET-1) decreases autophagy and cardiomyocyte contractility, similar to siAtg5-treated cells and TAC-mice, highlighting the crucial role of autophagy in cardiomyocyte contractility and cardiac performance.

CELLS (2021)

Add to Collection

Article Cardiac & Cardiovascular Systems

Pharmacological inhibition of adipose tissue adipose triglyceride lipase by Atglistatin prevents catecholamine-induced myocardial damage

Arne Thiele, Katja Luettges, Daniel Ritter, Niklas Beyhoff, Elia Smeir, Jana Grune, Julia S. Steinhoff, Michael Schupp, Robert Klopfleisch, Michael Rothe, Nicola Wilck, Hendrik Bartolomaeus, Anna K. Migglautsch, Rolf Breinbauer, Erin E. Kershaw, Gernot F. Grabner, Rudolf Zechner, Ulrich Kintscher, Anna Foryst-Ludwig

Summary: The specific inhibitor of ATGL, Atglistatin, can alleviate catecholamine-induced cardiac damage by exerting anti-fibrotic and anti-apoptotic effects. These effects are likely mediated by non-cardiac tissues.

CARDIOVASCULAR RESEARCH (2022)

Add to Collection

Article Biochemistry & Molecular Biology

Low-Dose Empagliflozin Improves Systolic Heart Function after Myocardial Infarction in Rats: Regulation of MMP9, NHE1, and SERCA2a

Jana Goerg, Manuela Sommerfeld, Bettina Greiner, Dilyara Lauer, Yasemin Seckin, Alexander Kulikov, Dmitry Ivkin, Ulrich Kintscher, Sergey Okovityi, Elena Kaschina

Summary: The study found that low-dose empagliflozin can increase cardiac contractility in normoglycemic rats and improve heart function early after myocardial infarction. These effects are achieved through the down-regulation of MMP9 and NHE1, as well as the up-regulation of SERCA2a, indicating a potential treatment option to improve cardiovascular outcomes post-MI.

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES (2021)

Add to Collection

Review Pharmacology & Pharmacy

Novel non-steroidal mineralocorticoid receptor antagonists in cardiorenal disease

Ulrich Kintscher, George L. Bakris, Peter Kolkhof

Summary: This review provides information on the molecular pharmacology and relevant clinical data of a new class of non-steroidal MRAs, discussing their cardiorenal outcomes. These compounds have an improved benefit-risk profile in treating cardiovascular diseases, and finerenone has a novel indication.

BRITISH JOURNAL OF PHARMACOLOGY (2022)

Add to Collection

Article Endocrinology & Metabolism

Wt1 haploinsufficiency induces browning of epididymal fat and alleviates metabolic dysfunction in mice on high-fat diet

Karin M. Kirschner, Anna Foryst-Ludwig, Sabrina Gohlke, Chen Li, Roberto E. Flores, Ulrich Kintscher, Michael Schupp, Tim J. Schulz, Holger Scholz

Summary: The study shows that WT1 has a role as a white adipocyte determination factor in intra-abdominal WAT by suppressing thermogenic genes. Reducing the expression of WT1 in these fat depots may represent a novel treatment strategy for metabolic diseases.

DIABETOLOGIA (2022)

Add to Collection

Article Cardiac & Cardiovascular Systems

Spontaneous Degenerative Aortic Valve Disease in New Zealand Obese Mice

Christiane Ott, Kathleen Pappritz, Niklas Hegemann, Cathleen John, Sarah Jeuthe, Cameron S. McAlpine, Yoshiko Iwamoto, Jonathan H. Lauryn, Jan Klages, Robert Klopfleisch, Sophie Van Linthout, Fil Swirski, Matthias Nahrendorf, Ulrich Kintscher, Tilman Grune, Wolfgang M. Kuebler, Jana Grune

Summary: NZO mice have been identified as a novel murine model to develop spontaneously degenerative AoV disease, aortic stenosis, and associated end organ damages of both ventricles and the lung, closely mimicking the clinical scenario of degenerative AoV disease.

JOURNAL OF THE AMERICAN HEART ASSOCIATION (2021)

Add to Collection

Article Multidisciplinary Sciences

Depletion of cardiac cardiolipin synthase alters and diastolic function

Elia Smeir, Sarah Leberer, Annelie Blumrich, Georg Vogler, Anastasia Vasiliades, Sandra Dresen, Carsten Jaeger, Yoann Gloaguen, Christian Klose, Dieter Beule, P. Christian Schulze, Rolf Bodmer, Anna Foryst-Ludwig, Ulrich Kintscher

Summary: The study found that cardiolipin synthase (CLS) affects cardiac function and plays an important role in regulating cardiac function, while CL72:8 is significantly decreased in cardiac samples from heart failure patients. Therefore, targeting CLS may be an effective approach for treating heart failure.

ISCIENCE (2021)

Add to Collection

Article Cardiac & Cardiovascular Systems

Use of fixed-dose combination antihypertensives in Germany between 2016 and 2020: an example of guideline inertia

Felix Mahfoud, Marita Kieble, Salka Enners, Ulrich Kintscher, Ulrich Laufs, Michael Bohm, Martin Schulz

Summary: The study found that the recommendations for hypertension treatment in the 2018 ESC/ESH guidelines were underutilized in clinical practice, with a decreasing trend in the prescription of FDC products over the years.

CLINICAL RESEARCH IN CARDIOLOGY (2022)

Add to Collection

Article Cardiac & Cardiovascular Systems

Assessment of Myocardial Microstructure in a Murine Model of Obesity-Related Cardiac Dysfunction by Diffusion Tensor Magnetic Resonance Imaging at 7T

David Lohr, Arne Thiele, Max Stahnke, Vera Braun, Elia Smeir, Joachim Spranger, Sebastian Brachs, Robert Klopfleisch, Anna Foryst-Ludwig, Laura M. Schreiber, Ulrich Kintscher, Niklas Beyhoff

Summary: This study aimed to characterize myocardial microstructure and function in an experimental model of obesity-related cardiac dysfunction. The results showed that a high-fat diet induced alterations in myocardial diffusion properties, but did not lead to remodeling of the three-dimensional myofiber arrangement of the left ventricle. Obese mice exhibited reduced diastolic function and longitudinal strain, emphasizing the need for further investigation into the significance of regional patterns in obesity-related cardiac dysfunction.

FRONTIERS IN CARDIOVASCULAR MEDICINE (2022)

Add to Collection

Article Urology & Nephrology

Finerenone Reduces Renal RORγt γδ T Cells and Protects against Cardiorenal Damage

Katja Luettges, Marlies Bode, Jan Niklas Diemer, Juliane Schwanbeck, Eva K. Wirth, Robert Klopfleisch, Kai Kappert, Arne Thiele, Daniel Ritter, Anna Foryst-Ludwig, Peter Kolkhof, Ulrich Otto Wenzel, Ulrich Kintscher

Summary: This study investigated the anti-inflammatory/fibrotic and immunological effects of the nonsteroidal MR antagonist finerenone in a cardiorenal disease model. The results showed that finerenone could alleviate cardiorenal damage, reduce blood pressure, decrease renal inflammatory cell content, and improve cardiac function.

AMERICAN JOURNAL OF NEPHROLOGY (2022)

Add to Collection

Article Multidisciplinary Sciences

Endosomal lipid signaling reshapes the endoplasmic reticulum to control mitochondrial function

Wonyul Jang, Dmytro Puchkov, Paula Samso, YongTian Liang, Michal Nadler-Holly, Stephan J. Sigrist, Ulrich Kintscher, Fan Liu, Kamel Mamchaoui, Vincent Mouly, Volker Haucke

Summary: Cells respond to fluctuating nutrient supply by changing organelle dynamics and metabolism. This study reveals that lipid signaling on the endoplasmic reticulum can control mitochondrial morphology and function, enabling cells to adapt to changing nutrient environments.

SCIENCE (2022)

Add to Collection

Article Biochemistry & Molecular Biology

Differential Regulation of MMPs, Apoptosis and Cell Proliferation by the Cannabinoid Receptors CB1 and CB2 in Vascular Smooth Muscle Cells and Cardiac Myocytes

Bettina Greiner, Manuela Sommerfeld, Ulrich Kintscher, Thomas Unger, Kai Kappert, Elena Kaschina

Summary: Cannabinoids regulate cell glucose uptake, proteolysis, and apoptosis through CB1R and CB2R receptors. The CB2R agonist JWH133 shows the highest protective properties.

BIOMEDICINES (2022)

Add to Collection

Review Peripheral Vascular Disease

ACE2 and SARS-CoV-2: Tissue or Plasma, Good or Bad?

Ulrich O. Wenzel, Ulrich Kintscher

AMERICAN JOURNAL OF HYPERTENSION (2021)

Add to Collection

No Data Available

And in the end-Telmisartan directly binds to PPARγ

Journal

Publisher

NATURE PUBLISHING GROUP

Keywords

Categories

Ask authors/readers for more resources

Protocol

Reagent

Authors

I am an author on this paper

Reviews

Primary Rating

Secondary Ratings

Novelty

Significance

Scientific rigor

Rate this paper

Recommended

Export Citation

Share Paper