Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

DHODH (Q02127) - Overview - Molecular Target Synopsis

Protein


DHODH, Dihydroorotate dehydrogenase (quinone), mitochondrial
Enzyme Classification 1.3.5.2
UniProt Q02127

Also Known as PYRD_HUMAN, DHODH

Catalyzes the conversion of dihydroorotate to orotate with quinone as electron acceptor. Monomer.

5ZF9
STRUCTURE OF HUMAN DIHYDROOROTATE DEHYDROGENASE IN COMPLEX WITH 280-12
RCSB/PDB
Inspect Structure
See all 3D Structures for DHODH

Isoforms / Transcripts (Protein Coding)


Drugs


DHODH is targeted by Approved Drugs Leflunomide, Teriflunomide. (see details)
Leflunomide
Teriflunomide

Sub-cellular localization


UniProt: DHODH is active in the following subcellular-locations: mitochondrion inner membrane.
GO terms: DHODH is active in the following subcellular-locations: cytosol, integral component of membrane, mitochondrial inner membrane, mitochondrion, neuronal cell body, nucleoplasm, plasma membrane.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project DHODH has gain in 1 cell-lines, loss in 2 cell-lines and no signal in 1002 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: SN12C, SNB_19, SW_620

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: SW 620, NCI-H520, SKM-1

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: K562, A549, NHLF

(see details)

3D Structures


For DHODH there are:
62 structures (63 chains) solved
61 are solved in complex with at least one small molecule ligand
60 are solved with an approved drug

DHODH is solved in complex with the approved drug(s):

FMN/RIBOFLAVIN 5'-PHOSPHATE (1D3G_A, 1D3H_A, 2B0M_A, 2BXV_A, 2FPT_A, 2FPV_A, 2FPY_A, 2FQI_A, 2PRH_A, 2PRL_A, 2PRM_A, 2WV8_A, 3F1Q_A, 3FJ6_A, 3FJL_A, 3G0U_A, 3G0X_A, 3KVJ_A, 3KVK_A, 3KVL_A, 3KVM_A, 3U2O_A, 3W7R_A, 3ZWS_A, 3ZWT_A, 4IGH_A, 4JGD_A, 4JS3_A, 4JTS_A, 4JTT_A, 4JTU_A, 4LS0_A, 4LS1_A, 4LS2_A, 4OQV_A, 4RK8_A, 4RKA_A, 4RLI_A, 4RR4_A, 4YLW_A, 4ZL1_A, 4ZMG_A, 5H2Z_A, 5H73_A, 5HIN_A, 5HQE_A, 5MUT_A, 5MVC_A, 5MVD_A, 5ZF4_A, 5ZF7_A, 5ZF8_A, 5ZF9_A, 5ZFA_A, 5ZFB_A, 6CJF_A, 6CJF_B, 6CJG_A, 6ET4_A, 6FMD_A),
CE9/POLIDOCANOL (5K9D_A).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


DHODH has been screened with 1147 compounds (1386 bioactivities), 384 compounds have bioactivities that show binding affinity of <= 500nM (481 bioactivities). (see details)