This month’s newsletter focuses upon the most downloaded articles of 2015. There were a great number of incredibly interesting and highly downloaded articles this year, covering a wide range of topics. The top 4 articles are given as free downloads in this newsletter. They cover concepts in peptide therapeutics, bispecific antibodies, non-antibody scaffold drugs and collaborative drug development.
The first article, by Keld Fosgerau and Torsten Hoffmann of Zealand Pharma A/S, Smedeland 36, Glostrup, 2600 Copenhagen, Denmark entitled: “Peptide therapeutics: current status and future directions” and they discuss the current status, strengths, and weaknesses of peptides as medicines and the emerging new opportunities in peptide drug design and development.
The second article, from Roland E. Kontermann and Ulrich Brinkmann of the Institute of Cell Biology and Immunology, University of Stuttgart, Stuttgart, Germany and Roche Pharma Research and Early Development (pRED), Large Molecule Research, Roche Innovation Center Penzberg, Penzberg, Germany entitled: “Bispecific antibodies” discuss how Bispecific antibodies (bsAbs) combine the functionality of two antibodies in one molecule. Two bsAb-drugs are currently on the market (one recently approved) and more are in clinical development. Driven by large pharma, bsAbs are emerging as next-generation biologics.
Third, is the review from Rodrigo Vazquez-Lombardi, Tri Giang Phan, Carsten Zimmermann, David Lowe, Lutz Jermutus and Daniel Christ of The Garvan Institute of Medical Research, Sydney, Australia; The University of New South Wales, Faculty of Medicine, St Vincent’s Clinical School, Sydney, Australia; The University of San Diego, School of Business Administration, San Diego, CA 92110, USA; MedImmune Ltd., Granta Park, Cambridge, UK and Trinity Hall, University of Cambridge, UK, entitled, “Challenges and opportunities for non-antibody scaffold drugs”. The authors describe how the first candidates from this promising class of small, non-antibody protein scaffolds are now moving into clinical development and practice. Challenges remain, and scaffolds will need to be further tailored toward applications where they provide real advantages over established therapeutics to succeed in a rapidly evolving drug development landscape.
Finally, is the article from Anna Karawajczyk, Fabrizio Giordanetto, Jorg Benningshof, Daniel Hamza, Tuomo Kalliokoski, Kees Pouwer, Remy Morgentin, Adam Nelson, Gerhard Müller, Alexander Piechot and Dimitrios Tzalis, of Taros Chemicals GmbH & Co. Dortmund, Germany; Mercachem, Nijmegen, The Netherlands; Sygnature Discovery, BioCity, Nottingham UK; Lead Discovery Center Dortmund, Germany; Syncom BV, Groningen, The Netherlands; Edelris, Lyon, France; The School of Chemistry, University of Leeds, UK and The Astbury Centre for Structural Molecular Biology, University of Leeds, UK. The article discusses how, in HTS campaigns, many compounds are tested, yet they represent only a small proportion of available chemical space. Since the chemical space to be sampled in research programs is practically infinite and sparsely populated, significant efforts and resources need to be invested in the generation and maintenance of a competitive compound collection. The European Lead Factory (ELF) project is addressing this challenge by leveraging the diverse experience and know-how of academic groups and small and medium enterprises (SMEs) engaged in synthetic and/or medicinal chemistry. Here, we describe the novelty, diversity, structural complexity, physicochemical characteristics and overall attractiveness of this first batch of ELF compounds for HTS purposes.
Steve Carney was born in Liverpool, England and studied Biochemistry at Liverpool University, obtaining a BSc.(Hons) and then read for a PhD on the Biochemistry and Pathology of Connective Tissue Diseases in Manchester University, in the Departments of Medical Biochemistry and Histopathology. On completion of his PhD he moved to the Kennedy Institute of Rheumatology, London, where he worked with Professor Helen Muir FRS and Professor Tim Hardingham, on the biochemistry of experimental Osteoarthritis. He joined Eli Lilly and Co. and held a number of positions in Biology R&D, initially in the Connective Tissue Department, but latterly in the Neuroscience Department. He left Lilly to take up his present position as Managing Editor, Drug Discovery Today, at Elsevier. Currently, he also holds an honorary lectureship in Drug Discovery at the University of Surrey, UK. He has authored over 50 articles in peer-reviewed journals, written several book chapters and has held a number of patents.