| Id: | acc1203 |
| Group: | 2sens |
| Protein: | Rb |
| Gene Symbol: | RB1 |
| Protein Id: | P06400 |
| Protein Name: | RB_HUMAN |
| PTM: | phosphorylation |
| Site: | Ser795 |
| Site Sequence: | PRSPYKFPSSPLRIPGGNIYI |
| Disease Category: | Cancer |
| Disease: | Colorectal Cancer |
| Disease Subtype: | |
| Disease Cellline: | LoVo |
| Disease Info: | |
| Drug: | adapalene |
| Drug Info: | "Adapalene is a topical retinoid medication primarily used for the treatment of mild to moderate acne vulgaris, including comedones, papules, and pustules, by modulating keratinocyte differentiation and reducing inflammation. " |
| Effect: | modulate |
| Effect Info: | Adapalene (ADA) can significantly increase the phosphorylation of CDK2 (at Thr - 160) and Rb (at Ser - 795) and inhibit tumors. |
| Note: | |
| Score: | 4.0 |
| Pubmed(PMID): | 26398439 |
| Sentence Index: | 26398439_4-5 |
| Sentence: | "Among them, adapalene (ADA; CD271,6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphtoic acid) exhibited the highest anti-proliferative effects in LOVO and DLD1 human colon cancer cell lines. Consistent with the expected properties of CDK2 inhibitors, the present study demonstrated that ADA significantly increased the G1-phase population and decreased the expression of CDK2, cyclin E and retinoblastoma protein (Rb), as well as the phosphorylation of CDK2 (on Thr-160) and Rb (on Ser-795)." |
Sequence & Structure:
MPPKTPRKTAATAAAAAAEPPAPPPPPPPEEDPEQDSGPEDLPLVRLEFEETEEPDFTALCQKLKIPDHVRERAWLTWEKVSSVDGVLGGYIQKKKELWGICIFIAAVDLDEMSFTFTELQKNIEISVHKFFNLLKEIDTSTKVDNAMSRLLKKYDVLFALFSKLERTCELIYLTQPSSSISTEINSALVLKVSWITFLLAKGEVLQMEDDLVISFQLMLCVLDYFIKLSPPMLLKEPYKTAVIPINGSPRTPRRGQNRSARIAKQLENDTRIIEVLCKEHECNIDEVKNVYFKNFIPFMNSLGLVTSNGLPEVENLSKRYEEIYLKNKDLDARLFLDHDKTLQTDSIDSFETQRTPRKSNLDEEVNVIPPHTPVRTVMNTIQQLMMILNSASDQPSENLISYFNNCTVNPKESILKRVKDIGYIFKEKFAKAVGQGCVEIGSQRYKLGVRLYYRVMESMLKSEEERLSIQNFSKLLNDNIFHMSLLACALEVVMATYSRSTSQNLDSGTDLSFPWILNVLNLKAFDFYKVIESFIKAEGNLTREMIKHLERCEHRIMESLAWLSDSPLFDLIKQSKDREGPTDHLESACPLNLPLQNNHTAADMYLSPVRSPKKKGSTTRVNSTANAETQATSAFQTQKPLKSTSLSLFYKKVYRLAYLRLNTLCERLLSEHPELEHIIWTLFQHTLQNEYELMRDRHLDQIMMCSMYGICKVKNIDLKFKIIVTAYKDLPHAVQETFKRVLIKEEEYDSIIVFYNSVFMQRLKTNILQYASTRPPTLSPIPHIPRSPYKFPSSPLRIPGGNIYISPLKSPYKISEGLPTPTKMTPRSRILVSIGESFGTSEKFQKINQMVCNSDRVLKRSAEGSNPPKPLKKLRFDIEGSDEADGSKHLPGESKFQQKLAEMTSTRTRMQKQKMNDSMDTSNKEEK
Select PDB:
No data.
Protein Tractability:
source: Open TargetsPTM Intensity:
source: CPTAC| RB1-Ser795 | |
|---|---|
| Cancer | Intensity |
| BRCA | 1 |
| COAD | |
| HGSC | 1.314 |
| ccRCC | 0.252 |
| GBM | |
| HNSC | -0.957 |
| LUAD | -0.782 |
| LUSC | -0.826 |
| non_ccRCC | |
| PDAC | |
| UCEC | |
PTM-Disease Association:
source: PTMD| Residue | Position | State | Disease | Class | PMID |
|---|---|---|---|---|---|
| S | 795 | D | Skin cancer | Phosphorylation | 23888052 |
| S | 795 | U | Melanoma | Phosphorylation | 15502804 ; 15502804 ; 15502804 |
State Note: Based on the distinct PTM states in diseases, PTMD classified all disease-associated PTMs into six classes, including whether the up-regulation (U) or down-regulation (D) of PTM levels, the absence (A) or presence (P) of PTMs, and the creation (C) or disruption (N) of PTM sites are associated with diseases.
PTM-Drug Perturbation Response:
source: DecryptM| Protein | Gene | PTM | Position | Modified sequence | Cell | Drug | pEC50 | Regulation | Experiment |
|---|---|---|---|---|---|---|---|---|---|
| P06400 | RB1 | P | Ser795 | SPYKFPSS(ph)PLR | A549 | Staursporin | 5.9515 | up | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A549 | Dasatinib | 6.6663 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Gefitinib | 8.5113 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Gefitinib | 6.2793 | - | |
| P06400 | RB1 | P | Ser795 | SPYKFPSS(ph)PLR | A431 | Gefitinib | 5.3028 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Gefitinib | 13.2099 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Gefitinib | 7.2478 | - | |
| P06400 | RB1 | P | Ser780;Ser788;Ser795 | TNILQYASTRPPTLS(ph)PIPHIPRS(ph)PYKFPSS(ph)PLR | A431 | Gefitinib | 5.3441 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Gefitinib | 7.2524 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Gefitinib | 6.187 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A549 | AZD8055 | 7.7331 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A549 | Dactolisib | 8.783 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A549 | Dasatinib | 15 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Gefitinib | 2 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A549 | Dasatinib | 6.0533 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A549 | Nintedanib | 7.6768 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A549 | Pictilisib | 10.9236 | - | |
| P06400 | RB1 | P | Ser795 | SPYKFPSS(ph)PLR | A549 | Pictilisib | 6.309 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A549 | Refametinib | 15 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A549 | Refametinib | 9.4401 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A549 | Staursporin | 8.3624 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A549 | Staursporin | 6.3712 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A549 | Tideglusib | 8.7826 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Dasatinib | 12.9897 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Afatinib | 6.5269 | - | |
| P06400 | RB1 | P | Ser780;Ser788;Ser795 | TNILQYASTRPPTLS(ph)PIPHIPRS(ph)PYKFPSS(ph)PLR | A431 | Afatinib | 6.4091 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Afatinib | 6.6331 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Afatinib | 5.4604 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Afatinib | 8.7521 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Afatinib | 8.2796 | - | |
| P06400 | RB1 | P | Ser780;Tyr790;Ser795 | TNILQYASTRPPTLS(ph)PIPHIPRSPY(ph)KFPSS(ph)PLR | A431 | Afatinib | 4.641 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Afatinib | 8.7822 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Afatinib | 6.2606 | - | |
| P06400 | RB1 | P | Ser780;Ser788;Ser795 | TNILQYASTRPPTLS(ph)PIPHIPRS(ph)PYKFPSS(ph)PLR | A431 | Afatinib | 5.5726 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Afatinib | 9.3058 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Dasatinib | 5.4737 | - | |
| P06400 | RB1 | P | Ser795 | SPYKFPSS(ph)PLR | A431 | Dasatinib | 9.9229 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Dasatinib | 5.3155 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Dasatinib | 5.2464 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Dasatinib | 7.2486 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Dasatinib | 5.2098 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Dasatinib | 9.7313 | - | |
| P06400 | RB1 | P | Ser788;Ser795 | S(ph)PYKFPSS(ph)PLR | A431 | Dasatinib | 9.141 | - | |
| P06400 | RB1 | P | Ser780;Ser788;Ser795 | TNILQYASTRPPTLS(ph)PIPHIPRS(ph)PYKFPSS(ph)PLR | A431 | Gefitinib | 8.0046 | - | |
| P06400 | RB1 | P | Ser795 | FPSS(ph)PLR | A431 | Gefitinib | 5.4001 | - |
pEC50 Note: pEC50 is the negative logarithm of EC50 (half-maximal effective concentration, dosage unit Mol), calculated as pEC50 = -log10(EC50), which quantifies the potency of a drug or compound.
Function score:
source: funscoRNo data.
