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Lecture 13: Finishing up - recap of lecture themes

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The course began with an examination of biomolecular structure, specifically focusing on amino acids, their classification, chirality, and the diverse interactions that govern them. By integrating concepts from physics such as Lennard-Jones potentials, electrostatics, and torsions, the lecture established a framework for determining which molecular states are probable based on free energy rather than just enthalpy. This shift was crucial for understanding the hydrophobic effect and entropy, allowing for a deeper analysis of protein folding and ligand binding as local phase transitions. The ability to interpret structural stability through these thermodynamic lenses enabled surprisingly accurate predictions using simple calculations, which could be significantly enhanced by computer simulations involving large systems with realistic environments like water. As the discussion progressed, the focus expanded from individual states to the kinetics of how structures form and transition between different configurations. While protein folding served as a primary example, the principles of kinetics applied universally to other processes such as ligand binding at specific sites. The lecture also highlighted the role of bioinformatics, which analyzes sequence data rather than direct structural information. This approach is effective because four billion years of evolution has encoded physical interaction rules into protein sequences, allowing researchers to infer structural properties and stability directly from genetic data. This evolutionary context explains why certain folds are structurally stable and have been selected over time, bridging the gap between computational analysis and biological reality. In the final stages of the course, these various disciplines—physical knowledge of protein structure, bioinformatics, and simulation techniques—were combined to advance drug discovery through methods like molecular docking. Docking acts as a powerful tool for predicting binding energies and exploring partition functions without the need for extensive simulations, making it widely used in both academic research and pharmaceutical industries. The curriculum concluded with an exploration of protein design, where scientists explicitly incorporate amino acid properties and Boltzmann distributions to explore regions of the energy landscape that evolution has not yet visited. This forward-looking approach represents a synthesis of theoretical physics, biological data, and computational power, offering new ways to engineer molecules and understand complex biological systems beyond what nature has currently produced.
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so we started out a few weeks ago studying biomolecular structure and in particular the amino acids why they have their properties they have what amino acids how we classify them and how they give rise to the diversity and also the chirality that i touched upon today with d and l amino acids from there we went on to looking at the molecular structure and in particular all the interactions lennard jones electrostatics torsions everything we then went back to physics because based on those interactions we needed tools that enable to say what states are probable what states are less probable that then led to the hydrophobic effect where we particularly introduced entropy right and that i was able to go from there to talk about free energy instead of just enthalpy which is an exceptionally important concept that kept coming back to the class we went on to instead of just starting pairs of states studying the entire partition function all possible states and from that we could start to talk about things in terms of stability of different states sure i used water as the primary example here but this is equally true for protein folding as i showed you a few lectures ago and even things like ligand binding you can think of this as a very small local phase transition for that ligand we used that to interpret protein structures in particular small parts of the structure in terms of free energy rather than just entropy that enabled us to explain roughly how fast they form and everything which is so in hand in task too that we can make surprisingly good predictions based just on paper and pen although if we combine that with a computer we're able to study much larger systems where we can have a realistic environment water tens of thousands of atoms and make actual predictions about actual systems that we can compare to experiments not only that we could use so-called free energy calculation methods to make specific predictions about how good should it be for a molecule to bind in a specific place in the molecule or in your case what to the probability of the binding energy for c non b in a particular site we looked quite a lot about protein structure first the fibrous and the water soluble proteins then the membrane proteins and also the lipids that surround the membrane proteins we focused even more than on what are these structures what do we have them we group them in folds we started to reason why the faults we see are structurally stable and why evolution has selected for those faults we're going to come back to the evolution and a few lines here we then went on to study not just the states the faults we have but how they form that is the kinetics when we're moving from one state to another now we primarily used folding as the simple universal examples here but as i showed you today this was equally true for the ligand binding to some of those binding sites so don't think that this is a narrow example limited to research and protein folding it's not what you learned about the kinetics is universally true based on the importance of the evolution here though in lecture 11 we focused on bioinformatics which on the one hand is a completely different approach just focusing on on sequence and data instead of structure but the reason why that works so well is that four billion years of evolution has encoded all the physical interactions here in the protein structures we see and that means that i can compare the sequence to effectively compare the structures it's really cool that it works and the only reason why that does work is evolution last lecture we then combined both the physical knowledge the protein structure the bioinformatics and a bit of the simulation to come up with drug discovery and particularly using docking effectively as poor man's way of doing a simulation or studying the partition function it is a remarkably powerful tool that is used throughout both academia and pharmaceutical companies today and the last hour we have now finished up by trying to combine that with simulations and particularly how we can use protein design where we now even more explicitly try to include the amino acid properties and the boltzmann distribution to go to the places of the map where evolution has not yet been it's been a great pleasure for me to take you through this class lots of work preparing these recordings but it's very fun so let me thank you for watching it this far and in particular if you're in stockholm i hope to get a chance to see in the future thanks