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Kincore-standalone

Installation and environment setup

First, download the repository:

git clone https://github.com/DunbrackLab/Kincore-standalone3

Then, create a virtual environment with the necessary packages to run kincore.

Option 1: use pixi

Install pixi if you haven't already:

curl -fsSL https://pixi.sh/install.sh | bash
cd Kincore-standalone3

That's it. You should now be able to run kincore inside the Kincore-standalone3 directory using pixi run kincore (see below for more details).

Note: the first time you run this command, pixi will create the environment and install all the necessary packages in the Kincore-standalone3 directory.

Option 2: use Anaconda

You can also create an anconda enviroment and install the necessary packages.

conda create --name 'kincore-standalone3' python=3.8 pandas numpy biopython hmmer --channel conda-forge --channel bioconda

Activate the virtual environment

conda activate kincore-standalone3

Running Kincore

Go to the Kincore-standalone3 folder if you haven't already:

cd Kincore-standalone3

Note: any of the following commands can also be run using python kinase_state.py instead of pixi run kincore, provided you have the necessary packages installed (such as hmmsearch) and/or virtual environment active.

Run the help command to see available options:

pixi run kincore -h

Kincore can be run on a single mmCIF or PDB file (can contain multiple models in a single file, e.g., MD trajectories or NMR structures).

pixi run kincore 1OL5.cif
pixi run kincore 1OL5.pdb

Also works on gzipped files:

pixi run kincore 1OL5.cif.gz
pixi run kincore 1OL5.pdb.gz

To run Kincore on more than one structure, give a list of structure filenames instead (full path names recommended for robustness).

pixi run kincore list.txt

Recommended: direct the output of Kincore to a text file so you can access it later. Also, attaching "&" at the end allows kincore to run in the background.

pixi run kincore list.txt > output.txt &

Other ways of running kincore

First, activate your virtual environment inside the Kincore-standalone3 folder

pixi shell

Or (if using Anaconda):

conda activate kincore-standalone3

Now you can run kincore using python kinase_state.py. For example:

python kinase_state.py list.txt > output.txt &

Understanding the output

Each kinase chain occupies at-least 17 lines, with different data listed on each line (18 lines if an autoinhibitory interaction with HRDAsp is detected):

1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Sequence         family CAMK  hmm CAMK     score  273.7   length 405
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Labels           Active   DFGin    DFGAsp-rot-in BLAminus Chelix-in   Saltbr-in   ActLoopNT-in   ActLoopCT-in   HRD-in Spine-in  
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          APEdihe_Labels   APE10-dihe-na APE9-dihe-na APE8-dihe-in APE8-rot-in APE67-dihe-in
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          APEdist_Labels   APE12-dist-in APE11-dist-in APE10-dist-in APE9-dist-in
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          NTdom_Residues   Lys.K162     Glu.E181     Glu4.Q185    HPN7.L196 
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          CTdom_Residues   XHRD.I253    HRD.H254     Arg.R255     HRDAsp.D256  aFasp.D311 
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          DFG_Residues     XDFG.A273    Asp.D274     Phe.F275     Gly.G276     DFG4.W277   DFG6.V279 
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          APE_Residues     APE.E299     APE6.D294    APE7.L293    APE8.T292    APE9.G291   APE10.C290 APE11.L289 APE12.T288
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          HRD_bbDihedrals  HRDHis    -63.28  -60.88 HRDArg   73.60    1.59
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          XDFG_bbDihedrals XDFG     -139.20 -172.08 DFGAsp   52.22   80.16 DFGPhe  -90.83   24.66 DFGGly  -49.87  -44.18
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          APE_bbDihedrals  APE6      -62.23  -14.30 APE7    -43.16  -62.50 APE8   -110.77  140.24 APE9    119.45 -153.19 APE10  -153.42  162.50
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          scDihedrals      DFGAsp    196.46   -3.74 DFGPhe  282.61   72.55 APE8    313.06
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          APE_Distances    APE9_Arg   3.68 APE10_DFG4   5.27 APE11_DFG4  10.96 APE12_DFG4   8.17
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Spine_Distances  Spine1     3.59 Spine2       3.51 Spine3       3.91 MaxSpine     3.91
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Other_Distances  Glu4_Phe   5.58 Lys_Phe     15.10 Lys_Glu      9.45 SaltBr       2.91 DFG6_XHRD   2.93
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Ligands          ADP:1388,MG:1389,MG:1390,MG:1394    ATPlike,Allosteric,Allosteric,Allosteric
1OL5A               0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Actloop          Len   26    Ave 17.70   Min 12.06   Max 28.30

Headers

Each line starts with a row header that identifies the structure file, model number, and chain ID, followed by the conformational state. This information is repeated on each line.

1OL5      0 A    Active_DFGin_BLAminus_SBin_NTin_CTin
Header Meaning
1OL5 Structure file
0 Model number
A Chain ID

Conformational label

The long string in the 4th column Active_DFGin_BLAminus_SBin_NTin_CTin is the overall conformational state of the kinase chain.

Label Meaning
Active The activation loop and αC-helix pass all of the criteria for active kinases
DFGin The DFG Phe (or equivalent residue) is flipped "in" towards the αC-helix
BLAminus The backbone dihedrals of the first three residues of the XDFG motif occupy the Ramchandran regions B, L, and A, and the χ1 dihedral of the DFG Phe sidechain (or equivalent residue) is gauche-minus
SBin A salt bridge is formed between the αC-helix Glu and β3-strand Lys
NTin The N-terminus of the activation loop (near the DFG motif) is hydrogen bonded to the HRD loop
CTin The C-terminus of the activation loop (near the APE motif) adopts the appropriate structure for binding protein substrates

Data

The 5th column contains another header that tells you what kind of data follows it. Residues with structural parameters that go into determining the state of the activation loop C-terminus are labeled APEi where i is the ith residue counting backwards from the end of the APE motif.

Row 1: Sequence

Label Meaning
family CAMK 1OL5 chain A belongs to the CAMK family
hmm CAMK Membership to the CAMK family was determined via the HMM filename "CAMK.hmm" located in the "HMMs" subdirectory. There are extra HMMs for unusual kinases, such as BUB, PEAK, and TP53RK that are members of the OTHER family.
score 273.7 HMM score of the chain A sequence for CAMK.hmm
length 405 Length of the sequence

Row 2: Labels

Label Meaning
Active The activation loop and αC-helix pass all of the criteria for active kinases
DFGin The DFG Phe (or equivalent residue) is flipped "in" towards the αC-helix
DFGAsp-rot-in The χ1 rotamer of the DFG Asp residue is trans, allowing it to bind ATP and Mg
BLAminus The backbone dihedrals of the first three residues of the XDFG motif occupy the Ramachandran regions B, L, and A, and the χ1 dihedral of the DFG Phe sidechain (or equivalent residue) is gauche-minus
Saltbr-in A salt bridge is formed between the αC-helix Glu and β3-strand Lys
ActLoopNT-in The N-terminus of the activation loop (near the DFG motif) is hydrogen bonded to the HRD loop
ActLoopCT-in The N-terminus of the activation loop (near the DFG motif) is hydrogen bonded to the HRD loop
HRD-in Backbone dihedral states for the HRD His and HRD Arg residues are active-like.
Spine-in The regulatory spine is formed.

Row 3: APEdihe_Labels

Label Meaning
APE10dihe-na Backbone dihedral state of the 10th residue from the end of the APE motif (in the C-terminus of the activation loop). 1OL5 chain A belongs to the CAMK family, not TYR, so dihedral criteria for this residue are not applicable to determining the Active/Inactive state.
APE9dihe-na Backbone dihedral state for the 9th residue from the end of the APE motif. Labeled "NA" for the same reason as APE10dihe.
APE8dihe-in Backbone dihedral state for the 8th residue from the end of the APE motif is active-like, hence the label "APE8dihe-in" (in analogy to how DFG-"in" is an active-like conformation of the DFG motif).
APE8rot-in Sidechain rotamer state for the 8th residue from the end of the APE motif is active-like.
APE67dihe-in Backbone dihedral states for the 6th and 7th residues from the end of the APE motif are active-like.

Row 4: APEdist_Labels

Label Meaning
APE12-dist-in Distance between CB of the APE12 residue and CA of the DFG4 residue is active-like.
APE11-dist-in Distance between CB of the APE11 residue and CA of the DFG4 residue is active-like.
APE10-dist-in Distance between CB of the APE10 residue and CA of the DFG4 residue is active-like.
APE9-dist-in Distance between CA of the APE9 residue and backbone carbonyl oxygen of the HRD Arg residue is active-like.

Row 5: NTdom_Residues

Residues in the N-terminal domain (N-terminal lobe)

Nomenclature Description
Lys The conserved Lys in the β3-strand (or equivalent residue).
Glu The conserved Glu in the αC-helix (or equivalent residue).
Glu4 The 4th residue from the Glu in the αC-helix.
HPN7 The 7th residue from the beginning of the HPN motif, located in the β4-strand (part of the regulatory spine).

Row 6: CTdom_Residues

Residues in the C-terminal domain (C-terminal lobe)

Nomenclature Description
XHRD The "X" residue immediately before the HRD motif.
HRD The conserved His (or sometimes Tyr) residue at the beginning of the HRD motif.
Arg The 2nd residue from the beginning of the HRD motif / the "R" of the HRD motif (or equivalent residue).
HRDAsp The 3nd residue from the beginning of the HRD motif / the "D" of the HRD motif (or equivalent residue).
aFasp The conserved Asp in the αF-helix.

Row 7: DFG_Residues

Residues in the Activation Loop N-terminal segment (ActLoopNT), starting with the XDFG motif (X-Asp-Phe-Gly)

Nomenclature Description
XDFG The "X" residue immediately before the DFG motif.
Asp The beginning of the DFG motif / the "D" of the DFG (or equivalent residue).
Phe The 2nd residue from the beginning of the DFG motif / the "F" of the DFG (or equivalent residue).
Gly The 3nd residue from the beginning DFG motif / the "G" of the DFG (or equivalent residue).
DFG4 The 4th residue from the beginning DFG motif, counting forwards from the "D" of the DFG.
DFG6 The 6th residue from the beginning DFG motif.

Row 8: APE_Residues

Residues in the Activation Loop C-terminal segment (ActLoopCT), ending with the APE motif (Ala-Pro-Glu). ActLoopCT residues are enumerated backwards (C-term. to N-term.) starting with Glu of APE ("APE1" or just "APE").

Nomenclature Description
APE The end of the APE motif / the Glu ("E") of the APE (or equivalent residue).
APE6 The 6th residue from the end of the APE motif, counting backwards starting from the "E" of the APE.
APE7 The 7th residue from the end of the APE motif.
APE8 The 8th residue from the end of the APE motif.
APE9 The 9th residue from the end of the APE motif.
APE10 The 10th residue from the end of the APE motif.
APE11 The 11th residue from the end of the APE motif.
APE12 The 12th residue from the end of the APE motif.

Row 9: HRD_bbDihedrals

Backbone (φ, ψ) dihedral angles of the HRD loop (also called "catalytic loop").

Nomenclature Description
HRD φ,ψ of HRD-His in A region of Ramachandran map for active kinases.
Arg φ,ψ of HRD-Arg in L region of Ramachandran map for active kinases.

Row 10: XDFG_bbDihedrals

Backbone (φ, ψ) dihedral angles of the XDFG (X-Asp-Phe-Gly) motif at the N-terminus of the activation loop.

Nomenclature Description
XDFG φ,ψ of X of XDFG motif. B region for BLAminus state of active kinases.
DFGAsp φ,ψ of Asp of DFG motif. L region for BLAminus state of active kinases.
DFGPhe φ,ψ of Phe of DFG motif. A region for BLAminus state of active kinases.
DFGGly φ,ψ of Gly of DFG motif. A region for BLA(A)minus state of active kinases.

Row 11: APE_bbDihedrals

Backbone (φ, ψ) dihedral angles of the Activation Loop C-terminal segment (ActLoopCT).

Nomenclature Description
APE6 φ,ψ of APE6 residue (6th residue from end of activation loop: X in XxxAPE). APE7,APE6 == AA or BL for active kinases.
APE7 φ,ψ of APE7 residue (6th residue from end of activation loop: X in XxxxAPE). APE7,APE6 == AA or BL for active kinases.
APE8 φ,ψ of APE8 residue (6th residue from end of activation loop: X in XxxxxAPE). B region for active kinases.
APE9 φ,ψ of APE9 residue (6th residue from end of activation loop: X in XxxxxxAPE). B region for active TYR kinases.
APE10 φ,ψ of APE10 residue (6th residue from end of activation loop: X in XxxxxxxAPE). B region for active TYR kinases.

Row 12: scDihedrals

Sidechain dihedral angles of select residues involved in conformational assignments (χ1 and, for certain residues, χ2).

Nomenclature Description
DFGAsp χ12 of Asp of DFG motif. trans χ1 rotamer for active kinases.
DFGPhe χ12 of Phe of DFG motif. gauche-minus χ1 rotamer for active kinases.
APE8 χ1 of APE8 residue (6th residue from end of activation loop: X in XxxxxAPE). gauche-minus χ1 rotamer for active non-TYR kinases.

Row 13: APE_Distances

Distances involving ActLoopCT residues used for conformational assignments of non-TYR kinases.

Nomenclature Description
APE9_Arg APE9-Cα / hRd-Arg O for ActLoopCT-in/ActLoopCT-out calculation for nonTYR kinases.
APE10_DFG4 APE10-Cβ / DFG4-Cα for ActLoopCT-in/ActLoopCT-out calculation for nonTYR kinases.
APE11_DFG4 APE10-Cβ / DFG4-Cα for ActLoopCT-in/ActLoopCT-out calculation for nonTYR kinases.
APE12_DFG4 APE10-Cβ / DFG4-Cα for ActLoopCT-in/ActLoopCT-out calculation for nonTYR kinases.

Row 14: Other_Distances

Distances involving the DFG motif, ActLoopNT, and C-helix residues used for conformational assignments.

Nomenclature Description
Glu4_Phe Glu4-Cα / DFG-Phe Cζ distance for DFGin/DFGout/DFGinter calculation. Glu4 is 4 residues after the salt-bridge Glu.
Lys_Phe Lys-Cα / DFG-Phe Cζ distance for DFGin/DFGout/DFGinter calculation. Lys is the salt-bridge Lys.
Lys_Glu Lys-Cβ / Glu-Cβ distance for Chelix-in/Chelix-out calculation.
SaltBr Lys-Nζ / Glu OE1,OE2 distance for SaltBr-in/SaltBr-out calculation. Minimum of distance to OE1 and OE2.
DFG6_XHRD DFG6-N/O / Xhrd O/N distance for ActLoopNT-in/ActLoopNT-out calculation. Minimum of two backbone-backbone hydrogen bonds distances.

Row 15: Spine_Distances

Distances used to measure the state of the regulatory spine (Spine-in/Spine-out). | Spine1 | Nearest sidechain-atom distance between HRD-His and DFG-Phe.| | Spine2 | Nearest sidechain-atom distance between DFG-Phe and Glu4.| | Spine3 | Nearest sidechain-atom distance between Glu4 and HPN7.| | MaxSpine | Maximum value of the three spine distances to determine if spine is broken (Spine-out when MaxSpine>4.5 Å).|

Row 16: Ligands

List of ligands and their types (3 or 5 letter codes from PDB, residue numbers, and types

Nomenclature Description
ATPlike Any ATP-like PDB ligand (ATP, ACP, ANP, ADP, AGS).
Type1 Ligand occupies ATP-binding site.
Type1.5 Ligand occupies ATP-binding site and part of Chelix site.
Type2 Ligand occupies both ATP-binding site and Chelix site.
Type3 Ligand occupies Chelix site.
Allosteric Ligand is elsewhere.

Row 17: Actloop

Minimum, maximum, and average of B-factors of Ca atoms of activation loop. Useful for calculating min(pLDDT) of activation loop of AlphaFold/Boltz models.

Row 18: Autoinhibit

Present if there is any Ser, Thr, or Tyr in activation loop in hydrogen bonding distance of HRD-Asp

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