Reference Detail

Request Content

Contact

Missing content? – Request curation!

Request curation for specific Genes, Variants, or PubMed publications.

Have questions, comments, or suggestions? - Let us know!

Email us at : ckbsupport@genomenon.com

Ref Type

Journal Article

PMID

(36661329)

Authors

Qi J, Endres S, Yosifov DY, Tausch E, Dheenadayalan RP, Gao X, Müller A, Schneider C, Mertens D, Gierschik P, Wist M, Jebaraj BMC, Stilgenbauer S

Title

Acquired BTK mutations associated with resistance to noncovalent BTK inhibitors.

Journal	Vol	Issue	Date	Pages	Journal Short Title
Blood advances	7	19	2023 Oct 10	5698-5702	Blood Adv

URL

Abstract Text

Filtering

Case insensitive filtering will display rows if any text in any cell matches the filter term
Use simple literal full or partial string matches
Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

Sorting

Generally, the default sort order for tables is set to be first column ascending; however, specific tables may set a different default sort order.
Click on any column header arrows to sort by that column
Hold down the Shift key and click multiple columns to sort by more than one column. Be sure to set ascending or descending order for a given column before moving on to the next column.

Filter rows:

Showing 1 to 5 of 5 entries

Gene	Variant	Impact	Protein Effect	Variant Description	Associated with drug Resistance
BTK	G409R	missense	loss of function	BTK G409R lies within the protein kinase domain of the Btk protein (UniProt.org). G409R results in loss of kinase activity and reduced Btk and Plcg2 phosphorylation, increased Akt phosphorylation, and a greater sustained calcium influx upon IgM stimulation, and demonstrates resistance to BTK inhibitors in culture (PMID: 36661329).	Y
BTK	V416L	missense	loss of function - predicted	BTK V416L lies within the protein kinase domain of the Btk protein (UniProt.org). V416L retains Akt and Erk phosphorylation in culture (PMID: 35196427, PMID: 36661329), but results in decreased Btk autophosphorylation and loss of kinase activity in culture (PMID: 38301010), decreased Btk and Plcg2 phosphorylation and increased calcium ion flux in culture, and demonstrates resistance to BTK inhibitors in culture (PMID: 35196427, PMID: 36661329), and therefore, is predicted to lead to a loss of Btk protein function.	Y
BTK	G480R	missense	loss of function	BTK G480R lies within the protein kinase domain of the Btk protein (UniProt.org). G480R results in loss of kinase activity and reduced Btk and Plcg2 phosphorylation, increased Akt phosphorylation, and a greater sustained calcium influx upon IgM stimulation, and demonstrates resistance to BTK inhibitors in culture (PMID: 36661329).	Y
BTK	L528S	missense	loss of function	BTK L528S lies within the protein kinase domain of the Btk protein (UniProt.org). L528S results in loss of kinase activity and reduced Btk and Plcg2 phosphorylation, increased Akt phosphorylation, and a greater sustained calcium influx upon IgM stimulation, and demonstrates resistance to BTK inhibitors in culture (PMID: 36661329).	Y
BTK	D539H	missense	loss of function	BTK D539H lies within the protein kinase domain of the Btk protein (UniProt.org). D539H results in loss of kinase activity and reduced Btk and Plcg2 phosphorylation, increased Akt phosphorylation, and a greater sustained calcium influx upon IgM stimulation, and demonstrates resistance to BTK inhibitors in culture (PMID: 36661329).	Y

Showing 1 to 5 of 5 entries

Filter rows:

Filter rows:

Showing 1 to 15 of 15 entries

Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
BTK A428D	mantle cell lymphoma	sensitive	ARQ 531	Preclinical - Cell culture	Actionable	In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK A428D in culture (PMID: 36661329).	36661329
BTK A428D	mantle cell lymphoma	resistant	Pirtobrutinib	Preclinical - Cell culture	Actionable	In a preclinical study, a mantle cell lymphoma cell line developed resistance to Jaypirca (pirtobrutinib) after prolonged exposure in culture, and was subsequently found to have acquired BTK A428D (PMID: 36661329).	36661329
BTK C481F	mantle cell lymphoma	resistant	Ibrutinib	Preclinical - Cell culture	Actionable	In a preclinical study, a mantle cell lymphoma cell line developed resistance to Imbruvica (ibrutinib) after prolonged exposure in culture, and was subsequently found to have acquired BTK C481F (PMID: 36661329).	36661329
BTK C481F	mantle cell lymphoma	sensitive	ARQ 531	Preclinical - Cell culture	Actionable	In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK C481F in culture (PMID: 36661329).	36661329
BTK D539H	mantle cell lymphoma	sensitive	ARQ 531	Preclinical - Cell culture	Actionable	In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK D539H in culture (PMID: 36661329).	36661329
BTK D539H	mantle cell lymphoma	resistant	Fenebrutinib	Preclinical - Cell culture	Actionable	In a preclinical study, a mantle cell lymphoma cell line developed resistance to Fenebrutinib (GDC-0853) after prolonged exposure in culture, and was subsequently found to have acquired BTK D539H (PMID: 36661329).	36661329
BTK G409R	mantle cell lymphoma	sensitive	ARQ 531	Preclinical - Cell culture	Actionable	In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK G409R in culture (PMID: 36661329).	36661329
BTK G409R	mantle cell lymphoma	resistant	Vecabrutinib	Preclinical - Cell culture	Actionable	In a preclinical study, a mantle cell lymphoma cell line developed resistance to Vecabrutinib (SNS-062) after prolonged exposure in culture, and was subsequently found to have acquired BTK G409R (PMID: 36661329).	36661329
BTK G480R	mantle cell lymphoma	resistant	Fenebrutinib	Preclinical - Cell culture	Actionable	In a preclinical study, a mantle cell lymphoma cell line developed resistance to Fenebrutinib (GDC-0853) after prolonged exposure in culture, and was subsequently found to have acquired BTK G480R (PMID: 36661329).	36661329
BTK G480R	mantle cell lymphoma	sensitive	ARQ 531	Preclinical - Cell culture	Actionable	In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK G480R in culture (PMID: 36661329).	36661329
BTK G480R	mantle cell lymphoma	resistant	RN486	Preclinical - Cell culture	Actionable	In a preclinical study, a mantle cell lymphoma cell line developed resistance to RN486 after prolonged exposure in culture, and was subsequently found to have acquired BTK G480R (PMID: 36661329).	36661329
BTK L528S	mantle cell lymphoma	resistant	Fenebrutinib	Preclinical - Cell culture	Actionable	In a preclinical study, a mantle cell lymphoma cell line developed resistance to Fenebrutinib (GDC-0853) after prolonged exposure in culture, and was subsequently found to have acquired BTK L528S (PMID: 36661329).	36661329
BTK L528S	mantle cell lymphoma	sensitive	ARQ 531	Preclinical - Cell culture	Actionable	In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK L528S in culture (PMID: 36661329).	36661329
BTK V416L	mantle cell lymphoma	resistant	RN486	Preclinical - Cell culture	Actionable	In a preclinical study, a mantle cell lymphoma cell line developed resistance to RN486 after prolonged exposure in culture, and was subsequently found to have acquired BTK V416L (PMID: 36661329).	36661329
BTK V416L	mantle cell lymphoma	sensitive	ARQ 531	Preclinical - Cell culture	Actionable	In a preclinical study, ARQ 531 inhibited viability of a mantle cell lymphoma cell line harboring BTK V416L in culture (PMID: 36661329).	36661329

Showing 1 to 15 of 15 entries

Filter rows: