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Recent Pat Anticancer Drug Discov 2021 Apr 13. Epub 2021 Apr 13.

Department of Building Services Engineering，The Hong Kong Polytechnic University, Kowloon, Hong Kong. China.

Background: Epidermal growth factor receptor and anaplastic lymphoma kinase play key role in tumorigenesis and disease progression. Currently, targeted therapy is a better approach for cancer therapy compared with traditional chemotherapy. EGFR-based/ALK-based target therapies are key targets for drug development in cancer therapy. Read More

Gene Ther 2021 Apr 13. Epub 2021 Apr 13.

Division of Medical Biotechnology, Paul Ehrlich Institute, Langen, Germany.

Clinical development of chimeric antigen receptor (CAR)-T-cell therapy has been enabled by advances in synthetic biology, genetic engineering, clinical-grade manufacturing, and complex logistics to distribute the drug product to treatment sites. A key ambition of the CARAMBA project is to provide clinical proof-of-concept for virus-free CAR gene transfer using advanced Sleeping Beauty (SB) transposon technology. SB transposition in CAR-T engineering is attractive due to the high rate of stable CAR gene transfer enabled by optimized hyperactive SB100X transposase and transposon combinations, encoded by mRNA and minicircle DNA, respectively, as preferred vector embodiments. Read More

Bioorg Chem 2021 Mar 29;112:104876. Epub 2021 Mar 29.

BioOrg NMR Lab, Department of Biotechnology and Biosciences, University of Milano-Bicocca, P.zza della Scienza, 2, 20126 Milan, Italy. Electronic address:

We describe the development of an on-cell NMR method for the rapid screening of FimH ligands and the structural identification of ligand binding epitopes. FimH is a mannose-binding bacterial adhesin expressed at the apical end of type 1 pili of uropathogenic bacterial strains and responsible for their d-mannose sensitive adhesion to host mammalian epithelial cells. Because of these properties, FimH is a key virulence factor and an attractive therapeutic target for urinary tract infection. Read More

Expert Opin Drug Discov 2021 Apr 12:1-13. Epub 2021 Apr 12.

Target Identification., BenevolentAI, United Kingdom of Great Britain and Northern Ireland.

Introduction: Knowledge graphs have proven to be promising systems of information storage and retrieval. Due to the recent explosion of heterogeneous multimodal data sources generated in the biomedical domain, and an industry shift toward a systems biology approach, knowledge graphs have emerged as attractive methods of data storage and hypothesis generation.

Areas Covered: In this review, the author summarizes the applications of knowledge graphs in drug discovery. Read More

Angew Chem Int Ed Engl 2021 Apr 11. Epub 2021 Apr 11.

Technical University Darmstadt, Clemens-Schöpf-Institute of Organic Chemistry and Biochemistry, Alarich-Weiss-Strasse 4, 64287, Darmstadt, GERMANY.

Subtype selectivity represents a recurring challenge in many drug discovery campaigns. A typical example is the FK506 binding protein 51 (FKBP51), which has emerged as an attractive drug target for mood disorders, obesity and chronic pain. The most advanced FKBP51 ligands of the SAFit class are highly selective vs. Read More

Front Oncol 2021 25;11:654817. Epub 2021 Mar 25.

CCBIO, Centre for Cancer Biomarkers, Department of Clinical Science, Precision Oncology Research Group, University of Bergen, Bergen, Norway.

Acute myeloid leukemia (AML) is an aggressive heterogeneous blood cancer derived from hematopoietic stem cells. Tumor-stromal interactions in AML are of importance for disease development and therapy resistance, and bone marrow stroma seem like an attractive therapeutic target. Of particular interest is colony stimulating factor 1 receptor (CSF1R, M-CSFR, c-FMS, CD115) and its role in regulating plasticity of tumor-associated macrophages. Read More

Front Immunol 2021 25;12:636222. Epub 2021 Mar 25.

Department of Periodontics, Dental College of Georgia at Augusta University, Augusta, GA, United States.

Dendritic cell (DC)-derived exosomes (DC EXO), natural nanoparticles of endosomal origin, are under intense scrutiny in clinical trials for various inflammatory diseases. DC EXO are eobiotic, meaning they are well-tolerated by the host; moreover, they can be custom-tailored for immune-regulatory or -stimulatory functions, thus presenting attractive opportunities for immune therapy. Previously we documented the efficacy of immunoregulatory DCs EXO (regDCs EXO) as immunotherapy for inflammatory bone disease, in an model. Read More

Bioorg Chem 2021 Mar 29;111:104877. Epub 2021 Mar 29.

Chemistry Department, Faculty of Science, Suez Canal University, Ismailia 41522, Egypt. Electronic address:

Liver cancer is the most common type of cancer in many countries. New studies and statistics show rising liver cancer worldwide, so it is essential to seek new agents for this type of cancer. PIM1 has an attractive target in the discovery of cancer medications as it is very much expressed in a variety of malignancies and influences such as tumorigenesis, cell cycle progression, cellular proliferation, apoptosis, and cell migration. Read More

J Virol Methods 2021 Apr 8:114150. Epub 2021 Apr 8.

Janssen Research and Development, Turnhoutseweg 30, 2340 Beerse, Belgium. Electronic address:

Hepatitis B Virus (HBV) core protein has multiple functions in the viral life cycle and is an attractive target for new anti-viral therapies. Capsid assembly modulators (CAMs) target the core protein and induce the formation of either morphologically normal (CAM-N) or aberrant structures (CAM-A), both devoid of genomic material. To date a diverse family of CAM-N chemotypes has been identified, but in contrast, described CAM-As are based on the heteroaryldihydropyrimidine (HAP) scaffold. Read More

Cell Chem Biol 2021 Mar 31. Epub 2021 Mar 31.

School of Biochemistry, University of Bristol, University Walk, Bristol BS8 1TD, UK. Electronic address:

Synthetic peptides are attractive candidates to manipulate protein-protein interactions inside the cell as they mimic natural interactions to compete for binding. However, protein-peptide interactions are often dynamic and weak. A challenge is to design peptides that make improved interactions with the target. Read More

J Biol Chem 2021 Jan 8;296:100263. Epub 2021 Jan 8.

Institut für Biochemie und Biotechnologie, Charles-Tanford-Proteinzentrum, Martin-Luther-Universität Halle-Wittenberg, Halle (Saale), Germany; ZIK HALOmem, Charles-Tanford-Proteinzentrum, Martin-Luther-University Halle-Wittenberg, Halle (Saale), Germany. Electronic address:

The development of a targeted therapy would significantly improve the treatment of periodontitis and its associated diseases including Alzheimer's disease, rheumatoid arthritis, and cardiovascular diseases. Glutaminyl cyclases (QCs) from the oral pathogens Porphyromonas gingivalis, Tannerella forsythia, and Prevotella intermedia represent attractive target enzymes for small-molecule inhibitor development, as their action is likely to stabilize essential periplasmic and outer membrane proteins by N-terminal pyroglutamination. In contrast to other microbial QCs that utilize the so-called type I enzymes, these oral pathogens possess sequences corresponding to type II QCs, observed hitherto only in animals. Read More