FT-4202, a selective pyruvate kinase R activator for sickle cell disease

Authors: Ericsson, Anna ^a, Richard, David J. ^a, Wilker, Erik ^a, Lancia, David R., Jr. ^a, Fessler, Shawn ^a, Troccolo, Paul ^a, Zheng, Xiaozhang ^a, Toms, Angela ^a, Dinsmore, Christopher ^a, Yao, Lili ^a, Kuypers, Frans A. ^b, Larkin, Sandra ^b, Marcotte, Douglas ^a, Fulzele, Keertik ^a, Ribadeneira, Maria ^a, Guichard, Sylvie M. ^{c, ⁎}, Marshall, Gary ^a

Source: In Experimental Hematology January 2025 141

Discovery of KT-474a Potent, Selective, and Orally Bioavailable IRAK4 Degrader for the Treatment of Autoimmune Diseases.

Authors: Zheng, Xiaozhang, Ji, Nan, Campbell, Veronica, Slavin, Anthony, Zhu, Xiao, Chen, Dapeng, Rong, Haojing, Enerson, Brad, Mayo, Michele, Sharma, Kirti, Browne, Chris M., Klaus, Christine R., Li, Haoran, Massa, Ginny, McDonald, Alice A., Shi, Yatao, Sintchak, Mike, Skouras, Stephanie, Walther, Dirk M., Yuan, Karen

Source: Journal of Medicinal Chemistry; 10/24/2024, Vol. 67 Issue 20, p18022-18037, 16p

HDAC11 deficiency disrupts oncogene-induced hematopoiesis in myeloproliferative neoplasms

Authors: Yue, Lanzhu ^{1, 2, *}, Sharma, Vasundhara ^{2, *}, Horvat, Nathan P. ², Akuffo, Afua A. ^{2, 3}, Beatty, Matthew S. ², Murdun, Cem ^{2, 4}, Colin, Christelle ², Billington, Julia M.R. ^{2, 3}, Goodheart, William E. ², Sahakian, Eva ², Zhang, Ling ⁵, Powers, John J. ², Amin, Narmin E. ⁶, Lambert-Showers, Que T. ⁴, Darville, Lancia N. ⁷, Pinilla-Ibarz, Javier ², Reuther, Gary W. ⁶, Wright, Kenneth L. ², Conti, Chiara ⁸, Lee, Jennifer Y. ⁸, Zheng, Xiaozhang ⁸, Ng, Pui Yee ⁸, Martin, Matthew W. ⁸, Marshall, C. Gary ⁸, Koomen, John M. ⁶, Levine, Ross L. ⁹, Verma, Amit ¹⁰, Grimes, H. Leighton ¹¹, Sotomayor, Eduardo M. ¹², Shao, Zonghong ¹, Epling-Burnette, Pearlie K. ^{1, 2, 13}

Source: In Blood 16 January 2020 135(3):191-207

Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B‑Cell Lymphoma.

Authors: Weiss, Matthew M., Zheng, Xiaozhang, Ji, Nan, Browne, Chris M., Campbell, Veronica, Chen, Dapeng, Enerson, Brad, Fei, Xue, Huang, Xin, Klaus, Christine R., Li, Haoran, Mayo, Michele, McDonald, Alice A., Paul, Atanu, Rong, Haojing, Sharma, Kirti, Shi, Yatao, Slavin, Anthony, Walther, Dirk M., Yuan, Karen

Source: Journal of Medicinal Chemistry; 7/11/2024, Vol. 67 Issue 13, p10548-10566, 19p

Discovery of novel biaryl sulfonamide based Mcl-1 inhibitors

Authors: Follows, Bruce, Fessler, Shawn, Baumeister, Timm, Campbell, Ann-Marie, Zablocki, Mary Margaret, Li, Hongbin, Gotur, Deepali, Wang, Zhongguo, Zheng, Xiaozhang, Molz, Lisa, Nguyen, Cokey, Herbertz, Torsten, Wang, Liann, Bair, Kenneth

Source: Bioorganic & medicinal chemistry letters. 29(16):2375-2382

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100090307112.0x000001&indx=1&recIds=ETOCvdc_100090307112.0x000001

Chemically Induced Degradation of the Oncogenic Transcription Factor BCL6

Authors: Kerres, Nina, Steurer, Steffen, Schlager, Stefanie, Bader, Gerd, Berger, Helmut, Caligiuri, Maureen, Dank, Christian, Engen, John R., Ettmayer, Peter, Fischerauer, Bernhard, Flotzinger, Gerlinde, Gerlach, Daniel, Gerstberger, Thomas, Gmaschitz, Teresa, Greb, Peter, Han, Bingsong, Heyes, Elizabeth, Iacob, Roxana E., Kessler, Dirk, Kölle, Heike, Lamarre, Lyne, Lancia, David R., Lucas, Simon, Mayer, Moriz, Mayr, Katharina, Mischerikow, Nikolai, Mück, Katja, Peinsipp, Christoph, Petermann, Oliver, Reiser, Ulrich, Rudolph, Dorothea, Rumpel, Klaus, Salomon, Carina, Scharn, Dirk, Schnitzer, Renate, Schrenk, Andreas, Schweifer, Norbert, Thompson, Diane, Traxler, Elisabeth, Varecka, Roland, Voss, Tilman, Weiss-Puxbaum, Alexander, Winkler, Sandra, Zheng, Xiaozhang, Zoephel, Andreas, Kraut, Norbert, McConnell, Darryl, Pearson, Mark, Koegl, Manfred

Source: In Cell Reports 19 September 2017 20(12):2860-2875

Prediction of pharmacokinetics and pharmacodynamics in human for IRAK4 targeted protein degrader

Authors: Chen, Dapeng, Rong, Haojing, Mayo, Michele, McDonald, Alice, Campbell, Veronica, Zheng, Xiaozhang, Agarwal, Sagar, Weiss, Matt, Slavin, Anthony

Source: In Drug Metabolism and Pharmacokinetics April 2024 55 Supplement

Discovery of novel N-hydroxy-2-arylisoindoline-4-carboxamides as potent and selective inhibitors of HDAC11

Authors: Martin, Matthew W., Lee, Jennifer Y., Lancia, David R., Ng, Pui Yee, Han, Bingsong, Thomason, Jennifer R., Lynes, Maureen S., Marshall, C. Gary, Conti, Chiara, Collis, Alan, Morales, Monica Alvarez, Doshi, Kshama, Rudnitskaya, Aleksandra, Yao, Lili, Zheng, Xiaozhang

Source: Bioorganic & medicinal chemistry letters. 28(12):2143-2147

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100114643689.0x000001&indx=1&recIds=ETOCvdc_100114643689.0x000001

Compounds and compositions for the inhibition of NAMPT

Novel HDAC11 inhibitors suppress lung adenocarcinoma stem cell self-renewal and overcome drug resistance by suppressing Sox2

Authors: Bora-Singhal, Namrata, Mohankumar, Durairaj, Saha, Biswarup, Colin, Christelle M., Lee, Jennifer Y., Martin, Matthew W., Zheng, Xiaozhang, Coppola, Domenico, Chellappan, Srikumar

Source: Scientific reports. 10(1)

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100164298505.0x000001&indx=1&recIds=ETOCvdc_100164298505.0x000001

Piperidine derivatives and compositions for the inhibition of nicotinamide phosphoribosyltransferase (NAMPT)

Pyridinyl and pyrimidinyl sulfoxide and sulfone derivatives

Compounds and compositions for the inhibition of NAMPT

Substituted biaryl piperazinyl-pyridine analogues

SUBSTITUTED BIARYL PIPERAZINYL-PYRIDINE ANALOGUES

Substituted biaryl piperazinyl-pyridine analogues

CIS-CYCLOHEXYL SUBSTITUTED PYRIMIDINONE DERIVATIVES

Biaryl piperazinyl-pyridine analogues

IRAK4 degrader in hidradenitis suppurativa and atopic dermatitis: a phase 1 trial

Authors: Ackerman, Lindsay, Acloque, Gerard, Bacchelli, Sandro, Schwartz, Howard, Feinstein, Brian J., La Stella, Phillip, Alavi, Afsaneh, Gollerkeri, Ashwin, Davis, Jeffrey, Campbell, Veronica, McDonald, Alice, Agarwal, Sagar, Karnik, Rahul, Shi, Kelvin, Mishkin, Aimee, Culbertson, Jennifer, Klaus, Christine, Enerson, Bradley, Massa, Virginia, Kuhn, Eric, Sharma, Kirti, Keaney, Erin, Barnes, Randy, Chen, Dapeng, Zheng, Xiaozhang, Rong, Haojing, Sabesan, Vijay, Ho, Chris, Mainolfi, Nello, Slavin, Anthony, Gollob, Jared A.

Source: Nature Medicine; 20230101, Issue: Preprints p1-10, 10p

Carboxylic acid, phosphate or phosphonate substituted quinazolin-4-ylamine analogues as capsaicin receptor modulators