Protein mono-ADP-ribosyltransferase TIPARP (TIPARP)

Protein mono-ADP-ribosyltransferase TIPARP (commonly abbreviated TIPARP, also known as PARP7 or ARTD14) is a member of the poly(ADP-ribose) polymerase (PARP) family with mono-ADP-ribosyltransferase activity, functioning primarily as a nuclear enzyme that modifies itself and multiple target proteins, including core histones, α-tubulin, and transcription factors such as the aryl hydrocarbon receptor (AHR)[1][2][3][4][6]. TIPARP is a key transcriptional repressor of AHR and modulates gene expression by mono-ADP-ribosylating specific residues on substrates, forming part of a negative feedback loop for AHR signaling[1][3][4]. Its biological roles extend to regulating cell adhesion, cytoskeletal dynamics, immune responses, and potentially cancer development and progression[2][4][6]. TIPARP can be induced by TCDD (2,3,7,8-tetrachlorodibenzo-p-dioxin) and is implicated as a therapeutic target in cancer immunotherapy, with development of small molecule inhibitors such as RBN-2397 to activate anti-tumor immunity by blocking its immunosuppressive effects[4][6].

Other names

TCDD inducible poly(ADP-ribose) polymerasePARP7ARTD14TiPARPPoly(ADP-ribose) polymerase 7pART14ADP-ribosyltransferase diphtheria toxin-like 14DDF1RM1

Inhibition of enzymatic mono-ADP-ribosylation activity[6] Modulation of immune response through increased expression of pro-inflammatory cytokines upon inhibition[6]