Full Text Journal Articles by
Author Amgad Albohy


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Synthesis, in vitro biological investigation, and molecular dynamics simulations of thiazolopyrimidine based compounds as corticotrophin releasing factor receptor-1 antagonists.

Hossam R Elgiushy, Nageh A Abou-Taleb, George G Holz, Oleg G Chepurny, Ioannis Pirmettis, Sotirios Kakabakos, Vlasios Karageorgos, George Liapakis, Amgad Albohy, Khaled A M Abouzid, Sherif F Hammad,

Corticotrophin releasing factor receptor-1 (CRFR1) is a potential target for treatment of depression and anxiety through modifying stress response. A series of new thiazolo[4,5-d]pyrimidine derivatives were designed, prepared and biologically evaluated as potential CRFR1 antagonists. Four compounds produced more than fifty percent inhibition in the [<sup>125</sup>I]-Tyr<sup>0</sup>-sauvagine specific binding assay. Assessment ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 114:105079]

Cited: 0 times

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Transforming iodoquinol into broad spectrum anti-tumor leads: Repurposing to modulate redox homeostasis.

Ibrahim Chaaban, Haidy Hafez, Ibrahim AlZaim, Cynthia Tannous, Hanan Ragab, Aly Hazzaa, Salma Ketat, Asser Ghoneim, Mohamed Katary, Mohammad M Abd-Alhaseeb, Fouad A Zouein, Amgad Albohy, Ahmed Noby Amer, Ahmed F El-Yazbi, Ahmed S F Belal,

We managed to repurpose the old drug iodoquinol to a series of novel anticancer 7-iodo-quinoline-5,8-diones. Twelve compounds were identified as inhibitors of moderate to high potency on an inhouse MCF-7 cell line, of which 2 compounds (5 and 6) were capable of reducing NAD level in MCF-7 cells in concentrations ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 113:105035]

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Discovery of potent thieno[2,3-d]pyrimidine VEGFR-2 inhibitors: Design, synthesis and enzyme inhibitory evaluation supported by molecular dynamics simulations.

Eman Z Elrazaz, Rabah A T Serya, Nasser S M Ismail, Amgad Albohy, Dalal A Abou El Ella, Khaled A M Abouzid,

Vascular endothelial growth factor receptor (VEGFR) is one of the well-known targets that control angiogenesis and cancer progression. In this study, we are reporting the design, synthesis and biological evaluation of a series of 4-substituted thieno[2,3-d]pyrimidine derivatives as VEGFR-2 inhibitors. The design of these compounds was based on interactions extracted ... Read more >>

Bioorg Chem (Bioorganic chemistry)
[2021, 113:105019]

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Bioactivity Potential of Marine Natural Products from Scleractinia-Associated Microbes and In Silico Anti-SARS-COV-2 Evaluation.

Eman Maher Zahran, Amgad Albohy, Amira Khalil, Alyaa Hatem Ibrahim, Heba Ali Ahmed, Ebaa M El-Hossary, Gerhard Bringmann, Usama Ramadan Abdelmohsen,

Marine organisms and their associated microbes are rich in diverse chemical leads. With the development of marine biotechnology, a considerable number of research activities are focused on marine bacteria and fungi-derived bioactive compounds. Marine bacteria and fungi are ranked on the top of the hierarchy of all organisms, as they ... Read more >>

Mar Drugs (Marine drugs)
[2020, 18(12):]

Cited: 5 times

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In vivo antiulcer activity, phytochemical exploration, and molecular modelling of the polyphenolic-rich fraction of Crepis sancta extract.

Sherif S Ebada, Nariman A Al-Jawabri, Fadia S Youssef, Amgad Albohy, Sa'ed M Aldalaien, Ahmad M Disi, Peter Proksch,

Bioactivity-guided investigation of the methanol extract of Crepis sancta aerial parts, collected off Al-Tafilah, South Jordan, was applied, and in this study, the extract was explored for its phytochemical components and in vivo antiulcer activity. In addition, a docking study involving the purified compounds with the newly crystalized gastric proton ... Read more >>

Inflammopharmacology (Inflammopharmacology)
[2020, 28(1):321-331]

Cited: 6 times

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Mapping substrate interactions of the human membrane-associated neuraminidase, NEU3, using STD NMR.

Amgad Albohy, Michele R Richards, Christopher W Cairo,

Saturation transfer difference (STD) nuclear magnetic resonance (NMR) is a powerful technique which can be used to investigate interactions between proteins and their substrates. The method identifies specific sites of interaction found on a small molecule ligand when in complex with a protein. The ability of STD NMR to provide ... Read more >>

Glycobiology (Glycobiology)
[2015, 25(3):284-293]

Cited: 2 times

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Identification of selective inhibitors for human neuraminidase isoenzymes using C4,C7-modified 2-deoxy-2,3-didehydro-N-acetylneuraminic acid (DANA) analogues.

Yi Zhang, Amgad Albohy, Yao Zou, Victoria Smutova, Alexey V Pshezhetsky, Christopher W Cairo,

In the past two decades, human neuraminidases (human sialidases, hNEUs) have been found to be involved in numerous pathways in biology. The development of selective and potent inhibitors of these enzymes will provide critical tools for glycobiology, help to avoid undesired side effects of antivirals, and may reveal new small-molecule ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2013, 56(7):2948-2958]

Cited: 15 times

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Identification of Selective Nanomolar Inhibitors of the Human Neuraminidase, NEU4.

Amgad Albohy, Yi Zhang, Victoria Smutova, Alexey V Pshezhetsky, Christopher W Cairo,

The human neuraminidase enzymes (hNEU) play important roles in human physiology and pathology. The lack of potent and selective inhibitors toward these enzymes has limited our understanding of their function and the development of therapeutic applications. Here we report the evaluation of a panel of compounds against the four human ... Read more >>

ACS Med Chem Lett (ACS medicinal chemistry letters)
[2013, 4(6):532-537]

Cited: 12 times

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Substrate recognition of the membrane-associated sialidase NEU3 requires a hydrophobic aglycone.

Mahendra S Sandbhor, Naoto Soya, Amgad Albohy, R Blake Zheng, Jonathan Cartmell, David R Bundle, John S Klassen, Christopher W Cairo,

The human neuraminidases (NEU) consist of a family of four isoforms (NEU1-NEU4). Members of this enzyme family are proposed to have important roles in health and disease through regulation of the composition of cellular sialosides. The NEU3 isoform is a membrane-associated enzyme that cleaves glycolipid substrates. However, few reports have ... Read more >>

Biochemistry (Biochemistry)
[2011, 50(32):6753-6762]

Cited: 18 times

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Inhibitor selectivity of a new class of oseltamivir analogs against viral neuraminidase over human neuraminidase enzymes.

Amgad Albohy, Sankar Mohan, Ruixiang Blake Zheng, B Mario Pinto, Christopher W Cairo,

The viral neuraminidase enzyme is an established target for anti-influenza pharmaceuticals. However, viral neuraminidase inhibitors could have off-target effects due to interactions with native human neuraminidase enzymes. We report the activity of a series of known inhibitors of the influenza group-1 neuraminidase enzyme (N1 subtype) against recombinant forms of the ... Read more >>

Bioorg Med Chem (Bioorganic & medicinal chemistry)
[2011, 19(9):2817-2822]

Cited: 16 times

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Inhibition of human neuraminidase 3 (NEU3) by C9-triazole derivatives of 2,3-didehydro-N-acetyl-neuraminic acid.

Yao Zou, Amgad Albohy, Mahendra Sandbhor, Christopher W Cairo,

We report the synthesis of a series of C9 and N5Ac modified analogs of 2,3-didehydro-N-acetyl-neuraminic acid (DANA) and their inhibitory potency for the human neuraminidase 3 (NEU3) enzyme. We were able to generate a small library of compounds through the synthesis of azide derivatives of DANA, followed by Cu-catalyzed azide-alkyne ... Read more >>

Bioorg Med Chem Lett (Bioorganic & medicinal chemistry letters)
[2010, 20(24):7529-7533]

Cited: 10 times

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Insight into substrate recognition and catalysis by the human neuraminidase 3 (NEU3) through molecular modeling and site-directed mutagenesis.

Amgad Albohy, Matthew D Li, Ruixiang Blake Zheng, Chunxia Zou, Christopher W Cairo,

The mammalian neuraminidase (NEU) enzymes are found in diverse cellular compartments. Members of the family, such as NEU2 and NEU1, are cytosolic or lysosomal, while NEU3 and NEU4 are membrane-associated. NEU enzymes that act on substrates in the plasma membrane could modulate cellular signaling, cell surface glycoforms and the composition ... Read more >>

Glycobiology (Glycobiology)
[2010, 20(9):1127-1138]

Cited: 21 times

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