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Chapter  2.   Theoretical background

2.8   QM/MM methods

The  idea  behind  quantum  mechanics  /  molecular  mechanics  methods  (QM/MM)  is  to   retain  the  atomic  degrees  of  freedom  of  the  real  molecular  system  one  wants  to   model,  by  replacing  most  of  the  full  quantum  mechanical  description  with  molecular   mechanics  (an  approximation  to  quantum  mechanics).  The  quantum  mechanical  part   (usually  in  the  center  of  the  system)  thus  describes  the  main  region  of  interest  while   molecular  mechanics  acts  as  an  approximation  to  the  environment  surrounding  the   quantum  mechanical  part.  

 

Almost  all  QM/MM  methods  can  be  described  by  the  additive  equation:80    

 

      EQM/MM  =  EQM(I)  +  EMM(II)  +  EQM-­‐MM(I  ,  II)              

(64)   ∆Gelstat=�ψ|H0− e 2φ rxn|ψ+ e 2 � k Zkφrxnk − �ψ0|H0|ψ0�

Where  EQM/MM  is  the  total  energy  of  the  system,  EQM(I)  is  the  QM  energy  of  the  QM  

region  (I),  EMM  is  the  MM  energy  of  the  MM  region  (II)  and  EQM-­‐MM(I  ,  II)  is  the  QM-­‐MM  

interaction  term  between  the  two  regions.    

The  EQM(I)  term  is  simply  a  normal  quantum  mechanics  calculated  energy  using  any  

suitable  method.  The  only  prerequisite  is  that  the  QM  method  must  be  able  to   perform  energy  and  gradient  calculations  in  the  presence  of  external  point  charges   when  using  the  electrostatic  embedding  scheme  (see  later).  

The  EMM  energy  expression  consists  of  both  bonded  (bonds,  angles  and  dihedrals)  and  

nonbonded  (Lennard-­‐Jones  potential  and  the  Coulomb  potential  of  point  charges)   terms:  

 

 

       

  (65)   where  the  constants  kX,  d0,  θ0,  δ,  ε,  σ,  qA,  qB  are  fitted  so  that  the  force  field  reproduces  

conformational  energies,  interaction  energies  etc.  of  molecular  systems  for  which  the   force  field  is  intended.  Several  parameterised  force  fields  are  available  to  describe   proteins,  for  example  the  CHARMM  force  field81,82  which  is  used  in  this  work.  

 

It  is  the  EQM-­‐MM(I  ,  II)  term  that  essentially  distinguishes  different  QM/MM  methods  

from  one  another  (apart  from  the  use  of  different  force  fields)  as  it  takes  care  of  the   coupling  terms  (bonded,  van  der  Waals  (vdW)  and  electrostatic  interactions)   between  the  different  regions:  

 

      EQM-­‐MM(I  ,  II)  =  EbQM-­‐MM  +  EvdWQM-­‐MM  +  EelQM-­‐MM          

(66)   The  bonded  and  vdW  terms  of  EQM-­‐MM(I,II)  are  described  at  the  MM  level.  The  vdW  

interaction  is  usually  described  by  a  Lennard-­‐Jones  potential,  necessitating  Lennard-­‐ Jones  parameters  for  all  QM  atoms.  In  theory,  every  atom  of  the  QM  region  interacts   with  every  atom  of  the  MM  region,  but  in  practice  only  the  atoms  closest  to  the   boundary  contribute  significantly.    

 

The  electrostatic  QM-­‐MM  interaction,  which  is  the  most  important  term,  can  be   described  by  several  different  methods,  the  models  can  be  classified  by  their   increasing  complexity,  as  mechanical  embedding,  electrostatic  embedding  and   polarised  embedding.  In  the  mechanical  embedding  scheme  the  electrostatic  

interations  between  QM  atoms  and  MM  atoms  is  handled  at  the  MM  level  where  the   MM  charge  model  (usually  rigid  atomic  point  charges)  is  used  to  calculate  the   interaction  between  QM  and  MM  atoms  where  point  charges  for  all  QM  atoms  must   be  defined.  Mechanical  embedding  is  most  often  used  in  a  subtractive  QM/MM   approach  where  the  EMM  term  is  calculated  for  the  whole  system  (I+II)  right  from  the  

beginning.  The  main  problem  with  mechanical  embedding  is  that  the  QM-­‐based   electron  density  is  simplified  into  a  simple  model  of  point  charges  which  is   additionally  not  influenced  directly  by  the  charges  of  the  MM  region  (usually).      

The  electrostatic  embedding  scheme  is  a  natural  extension  to  mechanical  embedding.   The  electrostatic  interaction  is  simply  calculated  at  the  same  time  as  the  EQM(I)  term  

by  incorporating  the  point  charges  of  the  MM  region  as  an  electron  point-­‐charge  term  

EM M = � bonds kd(d−d0)2+ � angles kθ(θ−θ0)2+ � dihedrals kφ[1 +cos(nφ+δ)] + � nonbonded �AB[( σAB rAB) 12 −(σAB rAB) 6)] + 1 4π�0 qAqB rAB

and  a  nucleus  point-­‐charge  into  the  Hamiltonian  of  the  QM  calculation  of  the  QM   region.  The  nucleus  point-­‐charge  term  is  straightforward  and  the  electron  point-­‐ charge  term  is  simply  calculated  in  the  same  way  as  the  electron-­‐nucleus  term  is   calculated.  The  quantum  mechanical  electron  density  is  thus  influenced  by  the   surroundings  directly  and  can  adapt  to  any  changes  occurring  in  the  MM  region.    

A  polarised  embedding  scheme  takes  electrostatic  embedding  one  step  further  by   using  a  MM  charge  model  that  can  be  polarised  as  well  (by  the  QM  electron  density),   sometimes  involving  completely  mutual  polarisation  in  which  case  a  self-­‐consistent   cycle  is  required  at  each  QM/MM  energy  evaluation.  Several  different  polarised   embedding  approaches  have  been  suggested:  polarised  point  dipoles  scheme  where   assigned  atomic  polarisabilities  induce  point  dipoles,  Drude  oscillator/shell/charge-­‐ on-­‐spring  models  where  an  additional  opposite-­‐sign  point  charge  is  attached  to  the   MM  atom  connected  by  a  harmonic  spring  creating  a  dipole,  fluctuating  charges  and   more.80  

 

Electrostatic  embedding  and  polarised  embedding  QM/MM  can  also  be  looked  at  in   the  general  context  of  effective  embedding  potentials.  The  QM  system  is  embedded  by   an  embedding  potential,  just  like  the  effective  potentials  in  the  single  electron  

HF/Kohn-­‐Sham  equations.  In  electrostatic/polarised  embedding  QM/MM,  the   embedding  potential  is  (usually)  a  simple  Coulomb  point  charge  potential  (the  point   charge  approximating  the  multi-­‐particle  atom),  an  approximation  to  the  real  smeared   out  Coulomb  multi-­‐particle  term  of  the  surroundings.  Continuum  solvation  models   can  also  be  seen  as  embedding  potentials.  A  higher-­‐order  multipole  potential  goes  a   step  further  towards  the  real  potential  but  still  neglects  exchange-­‐repulsion  effects   that  can  in  principle  be  included  as  well  in  an  embedding  potential.  The  most   complicated  embedding  potentials  are  those  involving  whole  electron  densities,   usually  frozen,  as  in  the  frozen  density  embedding  methods.83-­‐86  

 

A  specific  problem  remains  that  concerns  the  division  of  the  system  into  QM  and  MM   regions.  Covalent  bonds  often  end  up  being  cut  by  the  QM-­‐MM  boundary,  especially   for  systems  such  as  proteins.  As  the  dangling  bond  of  the  QM  region  needs  to  be   saturated,  one  of  the  simplest  solutions  is  to  include  link  atoms  (usually  H)  as  part  of   the  QM  region  in  the  QM  energy  calculation.  Since  the  added  link  atoms  constitute  an   additional  energy  term,  it  should  be  corrected  for,  in  practice  though,  this  is  rarely   done.  However,  since  the  link  atom  will  be  very  close  to  the  first  MM  atom  at  the   boundary,  a  strong  artificial  electrostatic  interaction  will  be  present.  One  approach  to   solve  this  problem  is  called  charge-­‐shifting  which  removes  the  charge  from  the  MM   atom  and  divides  it  among  the  nearest  bonded  MM  atoms.87,88  

 

Other  methods  to  deal  with  the  QM-­‐MM  boundary  are  boundary-­‐atom  schemes   where  the  MM  atom  involved  in  the  cut  is  transformed  into  a  special  boundary  atom   which  mimics  both  the  QM  interaction  and  the  MM  interaction,  and  localised-­‐orbital   schemes  where  hybrid  orbitals  are  placed  at  the  boundary  (saturating  the  dangling   bond)  and  frozen  so  that  they  are  not  part  of  the  SCF  iterations.80  

 

QM/MM  calculations  can  nowadays  be  performed  using  many  different  programs,   often  these  are  quantum  chemistry  programs  that  have  incorporated  some  molecular   mechanics  functionality  or  the  other  way  around.    

Chemshell,  on  the  other  hand,  is  a  computational  chemistry  program  which  is   neither.88,89  It  uses  a  modular  approach  that  links  together  different  external  

programs  through  a  programmable  interface  based  on  the  Tool  Command  Language   (Tcl).  The  main  speciality  of  the  program  is  in  hybrid  QM/MM  simulations  where  in   principle  any  quantum  chemistry  program  can  be  linked  to  any  molecular  mechanics   program  to  perform  QM/MM  calculations  where  the  Chemshell  program  is  

responsible  for  the  geometry  optimisations/molecular  dynamics  simulations,  the   QM/MM  coupling  and  the  data  management.  The  program  allows  one  to  do  geometry   optimisation  and  molecular  dynamics  simulations  on  small  to  large  chemical  systems   using  a  variety  of  different  quantum  chemistry  programs  and  molecular  mechanics   programs  through  pre-­‐programmed  interfaces.  

   

Chapter  3.  Modelling  environmental  effects  on  chemical  shift  and