Ateneo - UPO

The course introduces the fundamental bioconjugation approaches, what types of bioconjugates exist (i.e. antibody-drug, protein-small molecule, imaging probe-protein or nanoparticle, etc.) and their uses. The formation of a stable bioconjugates through covalent bonding and / or capable of releasing a bioactive product or probe will be analysed. Cleavable and non-cleavable linkers and their design, development, and synthesis. Site-specific and bioorthogonal bioconjugation. The possible applications of bioconjugates in various research fields (diagnostic, therapeutic, analytical, etc.) will also be considered:

Slides and other material given by the teacher.
G. T. Hermanson, Bioconjugation Techniques, 3rd edition, 2013, Academic Press. ISBN: 978-0-12-382239-0
Chemistry of Bioconjugates: Synthesis, Characterization, and Biomedical Applications. R. Narain (Editor), Wiley, 2014, ISBN: 978-1-118-35914-3

The course aims to provide the student with basic knowledge on bioconjugation chemistry by examining important classes of functional groups and selective synthetic strategies. Students will acquire the principles of modern bioconjugation strategies: i. e. click chemistry, site-specific and bioorthogonal reactions.
Special attention will be given to the ability of understanding the approach to use according to the type of biological vector and / or nanoparticle and of designing the most suitable bioconjugate for the application.
Communication skills: the students will be able to use a suitable vocabulary and symbolism in relation to bioconjugation chemistry. Learning skills and ability in making judgements about the topics covered in the course.

Contents of the Organic and Pharmaceutical Chemistry courses of the Batchelor Degree.

Classroom lectures will be delivered with three teaching methods depending on the topic covered. A) Traditional lessons in which some theoretical contents will be illustrated and the classroom will be asked to discuss collectively and apply directly during classroom exercises. B) Project work in which small groups of students will be involved in solving problems related to the synthesis of various compounds. C) Problem solving starting from problems reported in the literature.
During the lectures, the reference literature details for the various topics will be provided to enable further investigation and encourage the student to read the primary literature.
Lecture slides and bibliographical references will be uploaded on DiR and made available to the student.

The teacher is available to the student for any clarification or explanation of the topics covered during the course.
Ongoing learning will be assessed through classroom exercises and collegial discussions.
Students with physical disabilities, Learning Disabilities or Special Education Needs can request specific services and tools via the Staff Sviluppo e Coordinamento Carriere e Servizi alle Studentesse e ale/gli studentesse/studenti, consulting the University webpage: https://www.uniupo.it/en/services/servicesstudents-physical-or-learning-disabilities
Students with disabilities, learning disabilities or special education needs, once they have contacted the University Staff, can refer to the tutor in charge of the course to define the examination modalities, concerning academic aspects.

The exam consists of a written examination consisting of exercises and/or theoretical questions on the entire program of the course.
The evaluation will take place on the basis of the correct solution of the exercises and on the efficacy of the answers and by testing the level of the learning objectives previously described. The passing grade is achieved by demonstrating that the student has understood the subject and is able to use the basic concepts of the topics covered during the course.
Other parameters of judgment are: the ability to organize and clearly expose the answer and the acquisition of the appropriate terminology. Excellence can be achieved by demonstrating a strong ability to link-compare different topics covered during the course.

Introduction to the fundamental bioconjugation approaches, what types of bioconjugates exist (i. e. antibody-drug, protein-small molecule, imaging probe-protein or nanoparticle, etc) and their uses.
Definition of functional groups suitable for the conjugation of bifunctional chelating agents or drugs to biomolecules (peptides, proteins, polysaccharides, polynucleotides) or protein vectors to nanoparticles. Analysis of the conjugation approaches through the formation of a stable bioconjugate and / or capable of releasing a bioactive product or the probe. Use of homo- and hetero-bifunctional linkers, cleavable and non-cleavable for bioconjugation. Analysis of the probes that can be used for bioconjugation.
New organic synthetic strategies for bioconjugation:
1) use of Click Chemistry reactions for bioconjugation: Huisgen's 1,3-dipolar cycloaddition, Staudinger Ligation, Inverse Electronic Demand Diels-Alder reaction;
2) native chemical ligation;
3) site-specific labeling techniques to deliver proteins to the site of interest;
4) bioorthogonal reactions and in vivo bioconjugation.
5) Use of enzymes in bioconjugation reactions.

Objective 1: Knowledge and understanding.
The course aims to provide students with robust theoretical knowledge on issues related to the bioconjugation of small molecules to biological vectors.
Objective 2: Applying knowledge and understanding.
The student will develop a robust knowledge and ability to apply the basic principles necessary to approach the bioconjugation protocols. They will know the basic techniques necessary for the planning and design of valid approaches for the preparation of imaging probes and / or drugs conjugated to biological vectors.
Objective 3: Making judgements.
The student will acquire the ability to compare and evaluate the problems related to bioconjugation protocols. The acquired knowledge will allow the student to orient himself in the problems related to the prediction of possible critical points in the design and development of biotechnological processes.
Objective 4: communication skills.
The student will be able to discuss with advanced technical language, the problems related to the development of bio-conjugates.
Objective 5: Learning skills
At the end of the lessons the student will be able to retrieve the main online resources, scientific and institutional, useful for staying updated on the evolution of the scientific debate and addressing various research issues.