Article
Medicine, Research & Experimental
Xueying Li, Wanhua Qiu, Lu Deng, Jingjing Lin, Wenting Huang, Yuchen Xu, Mulan Zhang, Nigel C. Jones, Runxuan Lin, Huiqin Xu, Li Lin, Peijun Li, Xinshi Wang
Summary: 11 beta-HSD1 participates in the pathogenesis of epilepsy and associated cognitive impairment by elevating neuronal excitability and contributing to apoptosis and hippocampal neuronal damage. Inhibition of 11 beta-HSD1 represents a promising strategy to treat epilepsy and cognitive comorbidity.
JOURNAL OF TRANSLATIONAL MEDICINE
(2022)
Article
Chemistry, Medicinal
Emanuele M. Gargano, Abdelrahman Mohamed, Ahmed S. Abdelsamie, Giuseppe F. Mangiatordi, Hanna Drzewiecka, Pawel P. Jagodzinski, Arcangela Mazzini, Chris J. van Koppen, Matthias W. Laschke, Orazio Nicolotti, Angelo Carotti, Sandrine Marchais-Oberwinkler, Rolf W. Hartmann, Martin Frotscher
Summary: Facing the clinical challenge of NSCLC, there is a genuine need for new therapeutic approaches. The discovery of 17 beta-HSD1 inhibitor 1 through rational design of compound libraries and biological screening shows promise in fighting NSCLC with high selectivity. Further in vivo studies can be pursued based on its pharmacological profile.
ACS MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Endocrinology & Metabolism
Rafal Podgorski, Marta Suminska, Marta Rachel, Marta Fichna, Piotr Fichna, Artur Mazur
Summary: This study describes the urinary profile of glucocorticoid metabolites and enzyme activity in the development and metabolism of cortisol in patients with cystic fibrosis (CF) for the first time. The activity of enzymes involved in cortisol metabolism is altered in CF patients, suggesting adrenal insufficiency or dysregulation of the HPA axis. CF also impairs nutrition and energy balance, leading to adaptive mechanisms due to limited secretion of adrenal steroids and subsequently reduced metabolites in urine.
FRONTIERS IN ENDOCRINOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Christoph P. Sager, Susanne Weber, Matthias Negri, Pauline Banachowicz, Gabriele Moeller, Jerzy Adamski, Rolf W. Hartmann, Sandrine Marchais-Oberwinkler
Summary: This study aimed to determine the topology of 17 beta-Hydroxystemid dehydrogenase type 2 (17β-HSD2) by constructing a homology model in complex with NAD(+) and 17 beta-estradiol, which was confirmed to be of high quality through site-directed mutagenesis. The model identified key amino acids involved in ligand or internal structure stabilization, providing a basis for further experiments and drug design studies.
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
(2021)
Article
Medicine, Research & Experimental
Matthew D. Taves, Shizuka Otsuka, Michaela A. Taylor, Kaitlynn M. Donahue, Thomas J. Meyer, Margaret C. Cam, Jonathan D. Ashwell
Summary: Glucocorticoids, produced by the enzyme 1113-hydroxysteroid dehydrogenase type 1 (1113-HSD1), play a role in tumor progression by suppressing the immune response. Inhibition of 1113-HSD1 reduces tumor growth and increases sensitivity to immunotherapy. Targeting 1113-HSD1 may be beneficial in cancer therapy.
JOURNAL OF CLINICAL INVESTIGATION
(2023)
Article
Chemistry, Medicinal
David M. Burns, Chunhong He, Yun-Long Li, Jincong Zhuo, Ding-Quan Qian, Lihua Chen, Ravi Jalluri, Sharon Diamond, Maryanne B. Covington, Yanlong Li, Richard Wynn, Peggy Scherle, Swamy Yeleswaram, Gregory Hollis, Steve Friedman, Brian Metcalf, Wenqing Yao
Summary: 1113-HSD1 is the primary enzyme responsible for activating cortisone to cortisol. Dysregulation of 1113-HSD1 has been associated with metabolic syndrome and type 2 diabetes mellitus. Designing a steroid mimetic scaffold can inhibit the activity of 1113-HSD1.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Biochemistry & Molecular Biology
Francisco Cortes-Benitez, Jenny Roy, Martin Perreault, Rene Maltais, Donald Poirier
Summary: The new synthesized androsterone derivative showed improved inhibitory activity in rat testes microsomal fraction but not in whole cells. Additionally, structural modification increased metabolic stability and demonstrated significant cytotoxicity against various cancer cell lines. Furthermore, both the lead compound and the derivative showed better binding energy than NADP+ at the cofactor-binding site according to molecular dynamics simulations.
JOURNAL OF STEROID BIOCHEMISTRY AND MOLECULAR BIOLOGY
(2021)
Article
Chemistry, Medicinal
Colin Zhang, Meizhong Xu, Chunhong He, Jincong Zhuo, David M. Burns, Ding-Quan Qian, Qiyan Lin, Yun-Long Li, Lihua Chen, Eric Shi, Costas Agrios, Linkai Weng, Vaqar Sharief, Ravi Jalluri, Yanlong Li, Peggy Scherle, Sharon Diamond, Deborah Hunter, Maryanne Covington, Cindy Marando, Richard Wynn, Kamna Katiyar, Nancy Contel, Kris Vaddi, Swamy Yeleswaram, Gregory Hollis, Reid Huber, Steve Friedman, Brian Metcalf, Wenqing Yao
Summary: 1113-HSD1 is the primary enzyme responsible for converting cortisone to cortisol, dysregulation of which leads to metabolic syndrome and type 2 diabetes. INCB13739 is a small molecule inhibitor of 1113-HSD1 that has been proven effective in controlling glucose levels and reducing cardiovascular risk factors in patients with type 2 diabetes.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Endocrinology & Metabolism
Estelle Bonnet, Mathias Winter, Delphine Mallet, Ingrid Plotton, Claire Bouvattier, Maryse Cartigny, Laetiti Martinerie, Michel Polak, Anne Bachelot, Frederic Huet, Sabine Baron, Muriel Houang, Sylvie Soskin, Anne Lienhardt, Jerome Bertherat, Cyril Amouroux, Aurore Bouty, Lise Duranteau, Remi Besson, Alaa El Ghoneimi, Dinane Samara-Boustani, Francois Becmeur, Nicolas Kalfa, Francoise Paris, Francois Medjkane, Aude Brac de la Perriere, Patricia Bretones, Herve Lejeune, Marc Nicolino, Pierre Mouriquand, Daniela-Brindusa Gorduza, Claire-Lise Gay
Summary: This study found that there have been changes in diagnostic practices and clinical management of patients with SRD5A2 or HSD17B3 deficiency since molecular diagnoses became available. Over the past two decades, there has been a trend towards earlier diagnosis and assignment of affected newborns as males, and the influence of initial genital appearance on these decisions has seemingly decreased in recent years.
ENDOCRINE CONNECTIONS
(2023)
Article
Endocrinology & Metabolism
Benedikte von Spreckelsen, Lise Aksglaede, Trine Holm Johannsen, John E. Nielsen, Katharina M. Main, Anne Jorgensen, Rikke Beck Jensen
Summary: This study presents the differences in clinical and hormonal data and analyses of gonadal characteristics in two siblings with 17 beta-HSD3 deficiency. The two patients differed in pubertal development, clinical presentation, hormonal profile, gonadal morphology, and expression of cell lineage markers. Early diagnosis of 17 beta-HSD3 deficiency appears beneficial to ameliorate long-term consequences.
JOURNAL OF PEDIATRIC ENDOCRINOLOGY & METABOLISM
(2022)
Review
Chemistry, Medicinal
Prashant R. Murumkar, Mayank Kumar Sharma, Pradeep Gupta, Niyati M. Patel, Mange Ram Yadav
Summary: The selection of the right protein structure is crucial for the success of drug discovery through structure-based design. This study presents a systematic approach for choosing the appropriate type of protein structure, with case studies on TACE, 11 beta-HSD1, DprE1, and SARS-CoV-2 M-pro enzymes for illustration.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Yaseen A. Al-Soud, Sandrine Marchais-Oberwinkler, Martin Frotscher, Rolf W. Hartmann
ARCHIV DER PHARMAZIE
(2012)
Article
Chemistry, Medicinal
Kuiying Xu, Yaseen A. Al-Soud, Marie Wetzel, Rolf W. Hartmann, Sandrine Marchais-Oberwinkler
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2011)
Article
Chemistry, Multidisciplinary
Najim A. Al-Masoudi, Basil Salih, Yaseen A. Al-Soud
JOURNAL OF COMPUTATIONAL AND THEORETICAL NANOSCIENCE
(2011)
Article
Chemistry, Physical
Na'il Saleh, John Graham, Akef Afaneh, Yaseen A. Al-Soud, Georg Schreckenbach, Fatima T. Esmadi
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY A-CHEMISTRY
(2012)
Article
Cell Biology
Yaseen A. Al-Soud, Emmanuel Bey, Alexander Oster, Sandrine Marchais-Oberwinkler, Ruth Werth, Patricia Kruchten, Martin Frotscher, Rolf W. Hartmann
MOLECULAR AND CELLULAR ENDOCRINOLOGY
(2009)
Article
Biochemistry & Molecular Biology
Yaseen A. Al-Soud, Najim A. Al-Masoudi, Thilo Schuppler, Erik De Clercq, Christophe Pannecouque
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
(2008)
Article
Biochemistry & Molecular Biology
Najim A. Al-Masoudi, Yaseen A. Al-Soud
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
(2008)
Article
Biochemistry & Molecular Biology
Najim A. Al-Masoudi, Bahjat. A. Saeed, Ali H. Essa, Yaseen A. Al-Soud
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
(2009)
Article
Chemistry, Organic
Iftikhar Ali, Baraa Siyo, Yaseen Al-Soud, Alexander Villinger, Peter Langer
SYNTHESIS-STUTTGART
(2012)
Article
Chemistry, Organic
Na'il Saleh, Yaseen A. Al-Soud, Leena Al-Kaabi, Indrajit Ghosh, Werner M. Nau
TETRAHEDRON LETTERS
(2011)
Article
Chemistry, Organic
Yaseen A. Al-Soud, Michael Heydel, Rolf W. Hartmann
TETRAHEDRON LETTERS
(2011)
Article
Chemistry, Inorganic & Nuclear
Yaseen A. Al-Soud, Haitham H. Al-Sa'doni, Sadeekah O. W. Saber, Reem H. M. Al-Shaneek, Najim A. Al-Masoudi, R. Loddo, P. La Colla
ZEITSCHRIFT FUR NATURFORSCHUNG SECTION B-A JOURNAL OF CHEMICAL SCIENCES
(2010)
Article
Chemistry, Inorganic & Nuclear
Yaseen A. Al-Soud, Najim A. Al-Masoudi, Hossam H. Al-Suod, Christophe Pannecouque
ZEITSCHRIFT FUR NATURFORSCHUNG SECTION B-A JOURNAL OF CHEMICAL SCIENCES
(2012)
Article
Biochemistry & Molecular Biology
Yaseen A. Al-Soud, Sadeekah O. W. Saber, Amneh Shtaiwi, Sondos O. Alsawakhneh, Kafa' A. S. Alhelal, Qusay F. A. Salman, Luay Abu-Qatouseh, Monther A. Khanfar, Raed A. Al-Qawasmeh
Summary: Piperazine-tagged imidazole derivatives 3a and 5-11 were synthesized and evaluated for their anticancer activity. Compound 5 showed the highest potency against MCF-7 and PC3 cell lines, binding to the hydrophobic pocket and forming polar contacts with high affinity.
ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Anas J. Rasras, Raed A. Al-Qawasmeh, Mohamed El-Naggar, Ihsan Shehadi, Mahmoud M. Elaasser, Yaseen A. Al-Soud
Summary: A series of aminoacetylenic nitroimidazole piperazine hybrid compounds were synthesized via three-component reaction, and their properties and antibacterial activities were investigated.
ZEITSCHRIFT FUR NATURFORSCHUNG SECTION C-A JOURNAL OF BIOSCIENCES
(2023)