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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 6 lines, with different data listed on each line:

1OL5      0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Labels    family CAMK  hmm CAMK     score  273.7   Active   DFGin    BLAminus Chelix-in   Saltbr-in   ActLoopNT-in   ActLoopCT-in   Spine-in   APE10-dihe-na APE9-dihe-na APE8-dihe-in APE8-rot-in APE67-dihe-in APE12-dist-in APE11-dist-in APE10-dist-in APE9-dist-in HRD-in
1OL5      0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Residues  APEp3.E302 APEp2.I301 APE.E299  APE6.D294 APE7.L293 APE8.T292 APE9.G291 APE10.C290 APE11.L289 APE12.T288 XDFG.A273  Asp.D274  Phe.F275  Gly.G276  DFG4.W277 DFG6.V279 Lys.K162  Glu.E181  Glu4.Q185 HPN7.L196  XHRD.I253  HRD.H254  Arg.R255  HRDAsp.D256 aFasp.D311
1OL5      0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Distances Glu4_Phe   5.58 Lys_Phe  15.10 Lys_Glu   9.45 SaltBr   2.91 DFG6_XHRD   2.93 APE9_Arg   3.68 APE3_aFasp3   6.13 APE10_DFG4   5.27 APE11_DFG4  10.96 APE12_DFG4   8.17 Spine    3.59   3.51   3.91   3.91
1OL5      0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Dihedrals HRD  -63.28  -60.88 Arg   73.60    1.59 XDFG -139.20 -172.08 DFG   52.22   80.16 -163.54   -3.74 DFG2  -90.83   24.66  282.61   72.55 DFG3  -49.87  -44.18 APE6  -62.23  -14.30 APE7  -43.16  -62.50 APE8 -110.77  140.24  313.06 APE9  119.45 -153.19 APE10 -153.42  162.50
1OL5      0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Ligands   ADP:1388,MG:1389,MG:1390,MG:1394    ATPlike,Allosteric,Allosteric,Allosteric
1OL5      0 A    Active_DFGin_BLAminus_SBin_NTin_CTin          Actloop     26    17.70   12.06   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: Labels

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.
A Chain ID
score 273.7 HMM score of the chain A sequence for CAMK.hmm
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 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
Spine-in The regulatory spine is formed.
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.
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.
HRD-in Backbone dihedral states for the HRD His and HRD Arg residues are active-like.

Row 2: Residues

List of residues used for conformational assignments. Kincore nomenclature followed by the residue type and number in the sequence (separated by ".").

Nomenclature Description
APE The end of the APE motif / the "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.
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.
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).
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 3: Distances

List of distances 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.
APE9_Arg APE9-Cα / hRd-Arg O for ActLoopCT-in/ActLoopCT-out calculation.
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
Spine Spine1-Spine2-Spine3-MaxSpine distances. All between side-chain atoms of residue pairs. Spine1 = (HRD-His, DFG-Phe), Spine2 = (DFG-Phe, Glu4), Spine3 (Glu4, HPN7). MaxSpine = max(Spine1, Spine2, Spine3) to determine if spine is broken (MaxSpine>4.5 Å)

Row 4: Dihedral angles

List of dihedral angles used for conformational assignments.

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
XDFG φ,ψ of X of XDFG motif. B region for BLAminus state of active kinases
DFG φ,ψ,χ12 of Asp of DFG motif. L region for BLAminus state of active kinases
DFG2 φ,ψ,χ12 of Phe of DFG motif. A region for BLAminus state of active kinases
DFG3 φ,ψ of Gly of DFG motif. A region for BLA(A)minus state of active kinases
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,χ1 of APE8 residue (6th residue from end of activation loop: X in XxxxxAPE). B region for active kinases. χ1 in (-120°,0°).
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 5: 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 6: 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 6: Autoinhibit

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

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