Van Leeuwenhoek Lecture on BioScience

Thursday, January 31, 2019
Gorlaeus laboratories, new entrance (Bètacampus), LUMY 04.28
Einsteinweg 55, 2333 CC Leiden

Covalent inhibitor drugs: From serendipity to rational technology

BioScience Initiative (see website)

From 15.45 onwards: tea/coffee/biscuits
Drinks after the lecture

Speaker: Tjeerd Barf (Oss, Acerta Pharma)

Tjeerd Barf is one of the founders of Acerta Pharma. He has extensive experience in pharmaceutical Research and Development and contributed to delivery of several clinical candidates in the metabolic disease, autoimmune and oncology space. He successfully exploited the covalent binding paradigm for kinases, resulting in the discovery of acalabrutinib. Tjeerd joined the pharmaceutical industry in 1997 and served in various project and line management roles at Pharmacia & Upjohn, Biovitrum, Organon, Schering-Plough and MSD. He holds a PhD in Medicinal Chemistry and MSc in Organic Chemistry from the University of Groningen.

Covalent binding technology aims to equip drug-like small molecules with a suitable chemical reactive group. This reactive group adducts specific protein targets of which the (over)activity is believed to be central to the control of a certain disease. After reaction, the drug is covalently bound to the protein, resulting in long-lasting inhibition. Consequently, only the regeneration (de novo synthesis) of the protein can restore its function. Whereas continuous circulation of conventional reversible binding drugs is generally essential , the presence of covalent drugs – once bound to the protein – is not needed to exert the beneficial effects. The target family of kinases, despite the lack of obvious reactive amino acid counterparts, can be exploited using the covalent binding technology as witnessed by the recent successful discovery of covalent BTK inhibitor acalabrutinib for the retreatment of certain blood cancers.

Please keep the following dates free in your diary (all Thursdays at 16h.):

  • February 21 2019, Jan-Willem Veening (Lausanne, Fundamental Microbiology)
  • March 28 2019, Richard Smith (Düsseldorf, Max Planck Inst. for Plant Breeding)
  • April 11 2019, Valerian Dolja (Oregon State University, Genome Research and BioComputing)
  • May 23 2019, Pamela Yeh (UCLA, Ecology and Evolutionary Biology)
  • June 27 2019, Nick Lane (London University College, Evolutionary Biochemistry)
  • September 26 2019, Rob Phillips (Pasadena, Caltech, Biology and Biological Engineering)

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